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Formulation and optimization of effervescent tablet containing bismuth sub-citrate
Somayeh Taymouri, Abolfazl Mostafavi, Mohamad Javanmardi
July-December 2019, 8(2):236-244
Objective: The objective of this study was to design, evaluate and optimize effervescent tablets containing bismuth sub-citrate with sufficient hardness and friability in treatment of peptic ulcer. Materials and Methods: Effervescent tablets were prepared by direct compression method and were optimized using irregular factorial design. Amount of citric acid, sodium bicarbonate to citric acid molar ratio, polyvinyl pyrrolidone K 30 (PVP k30), polyethylene glycol 6000 (PEG 6000) were selected as independent variables, whereas disintegration time, amount of carbon dioxide (CO2), friability, pH, and hardness were selected as dependent variables. All the batches were assessed for various pre and post compression characteristics such as flowability, hardness, friability, effervescent time, pH, and content uniformity. For the enhancement of tablets’ palatability, the components of optimized formulation were mixed with same amounts of different flavoring agents. Results: The best results obtained from effervescent tablets prepared by 500 mg citric acid, 5% PEG 6000 and 3% PVP k30 while the molar ratio of the sodium bicarbonate to citric acid was 3. The disintegration time, amount of CO2, friability, pH, and hardness of optimized formulation were confirmed to be 95.33 ± 1.15sec, 398.73 ± 1.46 mg, 0.73%, 6.0 ± 0.06 and 72.3 ± 5.5 N, respectively. The most pleasant taste according to volunteers’ acceptability was the taste of cherry. Conclusion: These results suggest that developed effervescent tablets may be promising for delivery of bismuth sub-citrate in peptic ulcers therapy.
  15,141 1,261 4
Effect of sodium benzoate on liver and kidney lipid peroxidation and antioxidant enzymes in mice
Forouzan Khodaei, Hossein Kholghipour, Masood Hosseinzadeh, Marzieh Rashedinia
July-December 2019, 8(2):217-223
Introduction: Sodium benzoate (SB), as a chemical preservative, is used in many kinds of foodstuff. Some studies reported toxicity effects of SB in food products and suggested to limit its usage. The aim of this study was to evaluate the effects of oral administration of SB on antioxidant enzymes and lipid peroxidation in the liver and kidney of mice. Materials and Methods: A total of 24 animals were divided into four groups: Control group and three treated groups that received 150, 300, and 600 mg/kg/day of SB, respectively, in drinking water for 4 weeks. The malondialdehyde level, glutathione (GSH) content, superoxide dismutase (SOD), and catalase (CAT) activities of the liver and kidney were measured and the results of the treated groups were compared with those of the control group (one-way analysis of variance). Results: Results showed that SB caused histological alterations in the liver and kidney tissues. Moreover, SB significantly increased lipid peroxidation and GSH content in the kidney tissues (P < 0.05). Also, CAT activity significantly declined in the kidney (P < 0.05), without changing the SOD activity, but SB did not have any effect on the biochemical parameter of the liver tissue. Conclusion: The results of this study showed that SB caused kidney injury more than liver injury, but as a food preservative, which is consumed for a long period of life, it may cause liver damage additionally. For that reason, the excessive SB intake in the food is disturbing.
  10,684 609 14
A review on solubility enhancement methods for poorly water-soluble drugs
Ahmad Ainurofiq, David Sarono Putro, Dhea Aqila Ramadhani, Gemala Mahendra Putra, Laura Da Costa Do Espirito Santo
January-June 2021, 10(1):137-147
One of the most important parameters in pharmacy is drug solubility. Solubility affects the efficacy of a drug. Drug solubility has an important role in determining the concentration of a drug to achieve the necessary pharmacological response, as all drugs absorbed by the body must be in the form of a solution. Drug solubility is quite a common issue and affects the bioavailability of a drug in the body. Drugs with low solubility are poorly absorbed, resulting in poor bioavailability. Many methods have been developed for increasing the solubility of a drug. In this review, we will describe possible efforts for improving the solubility of a drug, e.g., reducing particle size, surfactants, the use of nanosuspension technology, solid dispersion, salt formation, pH adjustment, hydrotropy, cocrystal, amorphous compound formation, and inclusion complexes. The main objective of this review was to focus on efforts that can increase the solubility of a drug to obtain good drug efficacy.
  10,008 966 13
Formulation and evaluation of Neem (Azadirachta indica A. Juss) seed oil suppositories
Olusola I Aremu, Kokonne E Ekere, Yetunde C Isimi, Victoria C Nwaogu, Olawale G Agbaje, Olubunmi J Olayemi, Musiliu O Adedokun, Martins O Emeje
July-December 2019, 8(2):245-252
Background: Neem seed is very vital because of its rich lipid content and bitter constituents. Aims: This study was designed to provide a scientific rationale for the preparation and use of Neem seed oil as suppositories using dika fat (DF), and macrogol (MG), as bases. Materials and Methods: The suppositories which were prepared by fusion method using a pre-calibrated mould, were characterized using parameters like appearance, crushing strength, weight variation, melting point, pH, liquefaction time and in-vitro release according to standard procedures. Results: Results show that, the suppository strengths were in the order; bland, MG (25.00 ± 1.50N) > DF (12.90 ± 0.72 N), while those containing medicaments were NSM1 (20.00 ± 1.92) > NSD1 (12.90 ± 0.94) > NSM2 (12.70 ± 1.24 N) > NSD2 (10.00 ± 1.35 N). The pH of medicated formulations were NSM1 (6.50 ± 0.01), NSM2 (6.54 ± 0.03) > NSD1 (5.73 ± 0.04) and NSD2 (5.07 ± 0.03). Melting point values show that, macrogol base had mean values of 36.80 °C ± 0.62 and 36.40 °C ± 0.46 for NSM1 and NSM2 respectively, whereas, those with DF gave an average melting point values of 32.10 °C ± 0.87 and 30.90 °C ± 0.79 for NSD1 and NSD2 respectively. Conclusion: Results obtained showed that suppositories prepared with Macrogol (MG) base exhibited better physicochemical properties than Dika fat (DF) base suppositories, therefore water soluble bases may be bases of choice in the delivery of neem seed oil.
  7,496 517 -
Green peas protein hydrolyzed by bromelain in simple procedure to improve kidney function in cisplatin-induced rats
Meilinah Hidayat, Sijani Prahastuti, Teresa Liliana Wargasetia, Kirana Nugraha, Andreanus Andaja Soemardji, Siti Farah Rahmawati, Nova Suliska, Khomaini Hasan
January-June 2019, 8(1):68-77
Context: Chronic kidney disease (CKD) can lead to terminal kidney failure. Previous study has shown that protein hydrolysate in yellow peas (Pisum sativum L.) can be used as a natural remedy for CKD. Aims: To obtain hydrolysate protein that is most effective in improving kidney function of cisplatin (CP)-induced Wistar rats, based on urea, creatinine, atrial natriuretic peptide (ANP), cyclooxygenase-1 (COX-1), and renin levels of CP-induced nephrotoxicity Wistar rats. Materials and Methods: Methods of Kjeldahl, Bradford, Kunitz, and sodium dodecyl sulfate-polyacrylamide gel electrophoresis were used to determine the content of the eight types of protein hydrolysates. In in vivo experiment, the samples were administered to CP-induced nephrotoxicity Wistar rats, with urea, creatinine, ANP, COX-1, and renin as parameters. Results: Total neutrase activity was 40.65 U/mg, and bromelain was 35.77 U/mg. Total specific activities of both enzymes were almost identical. Protein hydrolyzed using bromelain had small fractions (<14.4 kDa). On the 30th day of treatment, urea and creatinine levels of all groups of treatment were significantly different from CP control (P < 0.01). The lowest level was shown by the group which was treated with bromelain-hydrolyzed green pea protein. Among ANP, COX-1, and renin measurements, only the result of COX-1 showed the promising result. Conclusions: Green peas protein hydrolysate hydrolyzed by bromelain are suggested as the most effective in improving kidney function based on urea, creatinine, and COX-1 levels of CP-induced nephrotoxicity Wistar rats.
  7,191 543 3
Pharmacognostic standardization and chromatographic fingerprint analysis on triterpenoidal constituents of the medicinally important plant Artocarpus heterophyllus by high-performance thin layer chromatography technique
Gunja Srivastava, Manjul Pratap Singh
January-June 2019, 8(1):1-12
Background: Artocarpus heterophyllus commonly known as Kathal in Hindi and Jackfruit in English has a wide horizon of medicinal possessions. The plant is found in India and in its tropical regions. Objective: Although the plant and its extracts are renowned for its ethnic medicinal values diversely in India, yet organized data somewhere lack in reverse pharmacognostical approach of this plant that shows that plant have not been completely explored for its therapeutic potency. Materials and Methods: In the present study, the folklore potential of this plant has been explored by generating down its pharmacognostical standards along with measurement of its active therapeutic constituent ursolic acid and lupeol via. High-performance thin layer chromatography (HPTLC), evidence from organized data search says that ursolic acid and lupeol is ubiquitous to A. heterophyllus. The plant was also subjected to spectroscopic-based estimation of tannins (gallic acid and tannic acid) and flavonoids (quercetin and rutin). Antimicrobial testing was also performed. Results: Microscopic features revealed the presence of anomocytic type of stomata, collateral open type vascular bundle in which fascicular cambium is present, calcium oxalate crystal and covering trichomes were key features in leaves. Methanolic extract of leaves of the plant was subjected to HPTLC. HPTLC studies revealed that both ursolic acid and lupeol are present in appreciable amount. Plant showed good antibacterial activity which may be due to the high amount of tannins as the tannins has the ability to disintegrate the bacterial cell wall. Conclusion: The data generated could be significantly used as a reference for the authentication and quality control of A. heterophyllus.
  5,958 783 1
Comparative phytochemical screening, in vivo antioxidant and nephroprotective effects of extracts of cassava leaves on paracetamol-intoxicated rats
Israel O Okoro, Helen E Kadiri, Eferhire Aganbi
July-December 2019, 8(2):188-194
The phytochemical screening, antioxidant, and nephroprotective effects of methanol and acetone extracts of cassava (Manihot esculenta Crantz) leaves were comparatively investigated using standard procedures. Fifty-four male Wistar rats (albino) were divided into nine groups of six rats each. Group 1 = negative control (normal untreated rats + normal saline); group 2 = positive control (rats + 2g/kg bw acetaminophen + normal saline), groups 3, 4, and 5 = 200 mg/kg bw, 100 mg/kg bw, and 50 mg/kg bw of methanol extract, respectively, + 2g/kg bw acetaminophen; groups 6, 7, and 8 = 200 mg/kg, 100 mg/kg bw, and 50 mg/kg bw of acetone extract, respectively, + 2g/kg bw acetaminophen; and group 9 = 100 mg/kg silymarin + 2g/kg bw acetaminophen. The phytochemical screening of the methanol and acetone leaves extracts showed the presence of flavonoids, alkaloids, saponins, anthocyanins, tannins, and triterpene, whereas, cardiac glycoside, steroids, and anthraquinone were absent in both extracts. Acetaminophen administration significantly elevated the levels of serum urea, creatinine, sodium, and potassium with a corresponding decrease in the levels of total protein, albumin, and calcium in the group 2 rats compared with that in the group 1 rats. Similarly, the levels of superoxide dismutase, catalase, glutathione peroxidase, glutathione, and glutathione S-transferase were significantly less in the acetaminophen-intoxicated group than that in the negative control group. However, pretreatment with either extracts, dose dependently prevented the acetaminophen-induced derangement of the aforementioned parameters. The extracts showed antioxidant activity similar to the reference drug (silymarin). Comparatively, the methanol extract gave higher in vivo antioxidant and nephroprotective effects than the acetone extract. The results suggest the extracts of cassava leaves have high nephroprotective potential and may be based on their phytoconstituents and antioxidant activity.
  6,077 471 2
Antioxidant activity and phytochemical screening of Ficus benghalensis aerial roots fractions
Zeinab Etratkhah, Seyed Esmaeil Sadat Ebrahimi, Nafiseh Khosravi Dehaghi, Yousef Seifalizadeh
January-June 2019, 8(1):24-27
Context: Ficus benghalensis (Moraceae) is an evergreen tree found in south and southeast of Iran as wild and cultivated plants. Different parts of this plant have different effects such as antitumor, antipyretic, analgesic and anti-inflammatory. Aims: The aim of this study was investigated the phytochemical screening and antioxidant activities of different fractions of plant roots. Materials and Methods: Phytochemical investigation was done by different methods in references. Antioxidant activity was evaluated by DPPH and FRAP assay. All chemical materials and solvents were prepared from Sigma-Aldrich, Scharlau and Merk. Statistical Analysis: All measurements were carried out in triplicate and the data were expressed as mean ± SD. Statistical analysis was performed using one-way analysis of variance (ANOVA) and tukey test. Results: Phytochemical screening showed steroids, flavonoids, tannins, phenolic compounds, and anthraquinone glycoside are F. benghalensis constituents. This plant had antioxidant activity, but it was lower than the Indian kinds. Conclusion: This study elucidated Ficus benghalensis could be useful plant with antioxidant activity. Further investigation needs for details.
  5,573 731 3
New insights into the therapeutic effects of phenolic acids from sorghum seeds
Reda Ben Mrid, Youssef Bouargalne, Redouane El Omari, Mohamed Nhiri
January-June 2019, 8(1):91-101
This paper reviewed the beneficial effects of the major phenolic acid compounds of Sorghum bicolor seeds. Different studies were reviewed to determine the major phenolic acid components of sorghum seeds. Several kinds of literature were then analyzed to discuss the different beneficial effects of these molecules. S. bicolor is an important source for food and feed. It is among the top five crops regarding its production and consumption throughout the world. Till date, many studies highlighted different aspects of the biochemical and physiological properties of sorghum grain. However, studies concerning the pharmacological properties of sorghum grain are scarce. The predominant phenolic acids of sorghum seeds are ferulic, p-coumaric, and protocatechuic acids. The bioactive effects of these phenolic acids are mainly related to their antioxidant, antitumor, antidiabetic, antimicrobial, cardiovascular, and gastrointestinal activities. The data collected from recent studies indicate that these molecules have a promising future as natural agents for the treatment of various diseases, and this is particularly due to their strong antioxidant properties. This review provides evidence for the importance of sorghum seeds and their phenolic compounds in the prevention and treatment of several diseases. This work showed that sorghum grains are a good source of beneficial and therapeutic molecules. It also recommended the addition of sorghum grains to human diet as other cereals because of its high nutritional value.
  5,345 612 7
Investigation on the effects of Bactenecin on POPC membrane in atomistic details using molecular dynamics simulation
Seyran Saeidi, Elham Esmaeili, Mohabbat Ansari, Sajad Moradi, Mohsen Shahlaei
January-June 2019, 8(1):13-17
Background: Traditional antimicrobial agents are losing their efficiency as microbial resistance increases. Thus, developing antimicrobial peptides (AMPs) can assist as an alternative approach. For AMPs, the hypothesis mode of action is involved in pore formation within the lipid membrane, thereby leading to cell death. In this study, interaction between Bactenecin and 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphatidylcholine (POPC) was studied. Methods: For this purpose, two systems, Bactenecin in water and Bactenecin in POPC were treated by 50 ns of molecular dynamic simulation and data were compared with those of free POPC. Results: The results suggest that the interaction between Bactenecin and bilayer membrane cause some disorder and more instability along with little compactness of bilayer. The hydrogen bond between peptide and heads of lipid components may is main reason of membrane compactness. The results can provide some information on how to Bactenecin or other such peptides affect bio-membranes.
  5,179 522 -
Cocrystallization: An innovative route toward better medication
Braham Dutt, Manjusha Choudhary, Vikaas Budhwar
July-December 2020, 9(2):256-270
Nowadays, poor solubility, lower bioavailability, and hindered physical, chemical, and biopharmaceutical properties of active pharmaceutical ingredients (APIs) become a very important matter of discussion for pharmaceutical scientists. It is a challenging task for pharmaceutical researchers and industry to develop a suitable formulation with improved physicochemical properties. The process of cocrystallization is long known; however, in the recent times, this approach has gained enormous importance in pharmaceuticals as a relatively new method for enhancement of solubility, bioavailability, stability, thermal properties, permeability, tablet ability, and other related physicochemical properties. Cocrystals are multicomponent systems in which two components, an API and a coformer, were present in stoichiometric ratio and bonded together with non-covalent interactions in the crystal lattice. Cocrystallization offers better optimization of not only physicochemical properties but also therapeutic response and pharmacological properties of APIs. The design of a cocrystallization experiment is based on robustness, hydrogen bonding rules, and potential intermolecular interactions. Various theoretical and experimental approaches increase the chances for selection of a suitable coformer, the most challenging step during the design of cocrystal formation. The present review covers classification of cocrystals, drug selection criteria for cocrystals, chemistry involved in cocrystal formation, methods of preparation, their characterizations, and various applications in pharmaceutical and biomedical fields.
  5,101 550 3
Development of docetaxel-loaded folate-modified Poly(lactic-co-glycolic acid) particles
Yuri I Poltavets, Vasilisa V Zavarzina, Sergey L Kuznetsov, Anna A Krasheninnikova, Danil O Dronov, Nadezhda V Gukasova, Valentina G Shuvatova, Vadim Yu Balabanyan
July-December 2019, 8(2):253-261
Background: Poly(lactic-co-glycolic acid) (PLGA) particles with small vector molecules are used for targeted delivery of anticancer agents. To be effective, they must be small, noncytotoxic, sterile, and stable. Aim: The aim of this study was to prepare docetaxel-loaded folate-modified PLGA-based nanoparticles (FD-Dtx-NPs) and to assess their as parenteral folate-receptor targeted delivery systems during γ-sterilization and long-term storage. Materials and Methods: NPs were prepared by oil/water single emulsion-solvent evaporation method and simultaneous loading of polymer particles with docetaxel and folic acid derivative. NPs’ physicochemical characteristics and antitumor activity were assessed. Findings: FD-Dtx-NPs presented uniform characteristics over repeated measurements: ~250 nm size, <0.100 polydispersity index, and >2.5% docetaxel content in the finished lyophilizate. The observed slow docetaxel release from FD-Dtx-NPs was acceptable for proposed usage. γ-irradiated NPs were sterile under all tested protocols and maintained their physicochemical properties at a 10-kGy cumulative dose, 0.500 Gy/s dose rate, and 5.57-h exposure. No significant differences were observed in physicochemical characteristics of FD-Dtx-NPs over 12 months. Finally, FD-Dtx-NPs showed a high anticancer activity in vitro. Conclusion: The proposed method generates FD-Dtx-NPs with reproducible characteristics, high activity, and elevated stability during the long-term storage. Results of γ-sterilization and stability studies may be valuable for the development of polymer-based drugs.
  5,114 331 2
Quantitative structure–activity relationship analysis of thiophene derivatives to explore the structural requirements for c-Jun NH2-terminal kinase 1 inhibitory activity
Ashima Nagpal, Monika Chauhan
July-December 2019, 8(2):115-123
Background: With an aim to design a validated two-dimensional quantitative structure–activity relationship (2D QSAR) model, a probe was executed on a series of reported c-Jun NH2-terminal kinase-1 (JNK1) inhibitors, exhibiting selectivity toward JNKs (and not other members of MAPK family). Objective: The present work focused on obtaining valuable insights from the structural architecture of the selected compounds and their effects on JNK1 inhibitory activity. The present work deciphers the importance of descriptive variables, namely Verloop L (Subst. 1), Bond Dipole Moment (Subst. 2), LogP (Subst. 1), Balaban Topological index (Subst. 1), and  VAMP Total Dipole (whole molecule), in molecules possessing JNK1 inhibitory profile. Results: These explanatory variables, obtained after iteratively reducing the data, did not only provide us with the substantial evidence pertaining to the dependence of bioactivity on the structural features of molecules, but also suggested the measures to optimize the selected compounds so as to obtain potent JNK1 inhibitors with good selectivity profile. Based on these distinct descriptors, exhibiting no apparent intercorrelation and manifesting good correlation with biological activity, a 2D QSAR model was generated. Conclusion: Robustness of the developed model was evaluated by performing multiple linear regression, partial least square, and artificial neural network studies. The reliability and predictive ability of the developed model was ascertained through the values of standard statistical parameters, such as s = 0.38, F = 97.22, r = 0.95, r2 = 0.90, and r2cv = 0.88, for the training set compounds. The generated model was validated through the test set compounds, as well as by leave one out method.
  4,578 616 -
Synthesis and evaluation of thiadiazole-based antileishmanial agents
Farshid Hassanzadeh, Elham Jafari, Mozhgan Saeedi, Sedigheh Saberi
July-December 2020, 9(2):189-195
Background and Objectives: The 1, 3, 4-thiadiazole scaffold is one of the principal structural components, in a variety of drug categories such as antimicrobial, anti-inflammatory, antineoplastic, and antileishmanial agents. Considering the reported antileishmanial effects of thiadiazole derivatives and the importance of this disease, some of the thiadiazole derivatives with modifications at sulfur atom or amine group attached to the 2-position were synthesized and evaluated for antileishmanial activity. Materials and Methods: Derivatives of 1,3,4-thiadiazole including 2-substituted-thio-1,3,4-thiadiazoles bearing (5-(4-nitrobenzylideneamino) or 5-amino (II, IV, V) and one derivative of 2-substituted-amino-1,3,4-thiadiazole bearing (5- (4-nitrophenyl) (VII) were synthesized and evaluated for their in vitro antileishmanial activity against promastigote and amastigote forms of the Leishmania major. Results: The most active compound was found to be compound II after 24-h incubation against promastigotes and amastigotes with the half maximal inhibitory concentration (IC50) values of 44.4 µM and 64.7 µM, respectively. Conclusion: All of the synthesized compounds showed good antileishmanial activity against both forms of L. major after 48 and 72h incubation.
  4,707 404 1
Antibacterial effect of combination of cinnamon essential oil and thymol, carvacrol, eugenol, or geraniol
Yassine El Atki, Imane Aouam, Amal Taroq, Fatima El Kamari, Mohammed Timinouni, Badiaa Lyoussi, Abdelfattah Abdellaoui
January-June 2020, 9(1):104-109
Bacterial resistance to classic antibiotics is an alarming rate to put this into control with the use of natural products of plant derivatives. The objective of this study was to determine the phytochemical of cinnamon essential oil (EO) and to evaluate its antibacterial activity alone and in combination with some main components of EOs such as thymol, carvacrol, eugenol, or geraniol against three bacterial strains (Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa). The phytochemical analysis of cinnamon EO was evaluated using gas chromatography-flame ionization detector and gas chromatography-mass spectrometer analysis. The antibacterial activity of tested compounds was determined by agar disk diffusion and minimum inhibitory concentration (MIC) assays. The checkerboard method was used to quantify the efficacy of cinnamon EO in combination with those compounds. The results showed that the major compound in the cinnamon EO was trans-cinnamaldehyde (91.01%). Cinnamon oil was the highest antibacterial activity with MIC of 0.005, 0.005, and 0.02 mg/mL against E. coli, S. aureus, and P. aeruginosa, respectively. Synergistic activity was shown only against S. aureus by the combination of cinnamon EO and thymol. The additive effect was found against E. coli when cinnamon EO was combined with thymol or carvacrol, and against S. aureus when cinnamon EO was combined with carvacrol. However, the combination of EO and thymol or carvacrol showed an indifference action against P. aeruginosa. The combination of cinnamon EO with thymol or carvacrol can be used as an alternative therapeutic agent for medical application and as a natural preservative.
  4,600 472 3
Preparation and pharmaceutical evaluation of ferrous sulfate and ascorbic acid floating matrix tablet for prevention of anemia
Rahim Najafi Bahri, Lotfollah Saghaei, Taher Babaeimehr
July-December 2012, 1(2):72-80
For prolonging the time that drug remains in stomach, new methods used as floating drug delivery systems, that available in various forms such as floating tablets. These systems enhance drug absorption and decrease plasma concentration fluctuations. Iron deficiency and its inadequate absorption in diet are of community health problems. Common forms of iron available in the market have little bioavailability and due to greater excretion of drugs from the gastrointestinal tract has many complications such as constipation. Using floating systems to enhance drug absorption can reduce the dose required and drug side effects. In this study, preparation of floating tablets of ferrous sulfate plus ascorbic acid is considered since it has proven that vitamin C enhances iron absorption. Tablets were prepared with swollen polymers like HPMC K4M and carbopol934 by direct compression method. Sodium bicarbonate and citric acid was used to create the CO2 then drug properties such as buoyancy, release percentage and physical properties were tested on that. Tablet formulation No. 10, started to float in 27 seconds and floating state lasts 18 hours in environments like stomach. According to the great drug release and long floating state (12 h), tablet formulation 10 is recommended as a drug supplement to prevent anemia.
[ABSTRACT]   Full text not available  [PDF]
  4,325 650 -
Drug delivery through nose: A noninvasive technique for brain targeting
Abhishek Thakur, Pankaj K Singh, Swadhin S Biswal, Navneet Kumar, Chandan B Jha, Gurvinder Singh, Charanjit Kaur, Sheetu Wadhwa, Rajesh Kumar
January-June 2020, 9(1):168-175
Majority of drugs are usually introduced through oral or intra-venous route for fast action, better patient compliance and ease of drug administration. However, the low bioavailability and limited brain exposure of orally administered drugs pose a huge challenge to treat neurodegenerative and psychiatric disorders. So, the situation demands for targeting the drug to brain. For brain targeting, a number of factors are considered viz. molecular weight, route of administration, lipophilic character of drug and blood brain barrier (BBB). These factors limit the movement of drug into brain tissue through BBB. To overcome these problems, intranasal drug administration is one of the promising routes that bypasses BBB and cuts down the dose to be administered with better brain exposure to drug. Nasal route has been used for the administration of antihistamines, local analgesics and corticosteroids intended for local drug delivery in nasal allergy, nasal congestion and nasal infection. However, systemic drug delivery through this route has also been explored in recent times. For nose to brain drug delivery, olfactory and respiratory region are utilized which also enable delivery of larger molecules to reach brain tissues. Such delivery systems are generally pH or temperature dependent. Certain diseases of nervous system like migraine, dementia, parkinsonism, epilepsy and Alzheimer’s disease can be successfully treated through this route. This review attempts to highlight the anatomy of nose, mechanisms of drug delivery from nose to brain, critical factors in the formulation of delivery systems, nasal formulations and applications of nasal route for delivery of various drugs.
  4,492 440 4
Differential expression levels of agglutinin-like sequence, lipase, and secreted aspartyl protease genes in Candida tropicalis treated with fluconazole alone and in combination with clotrimazole
Alireza Khodavandi, Fahimeh Alizadeh, Maedeh Abdolahi, Mohammad Jahangiri
January-June 2019, 8(1):28-33
Background: The frequency of opportunistic fungal infections in immunocompromised patients, especially by Candida species, has sharply increased in the last few decades. As the number of antifungal drugs available for the treatment of candidiasis is limited, combination therapy has been employed as one of the most commonly used techniques to alleviate this problem. Aims: The main aim of this study was to explore the antifungal activity of fluconazole in combination with clotrimazole on expression levels of virulence genes, agglutinin-like sequences (ALS1 and ALS2), lipases (LIP1 and LIP4) and secreted aspartyl proteases (SAP2 and SAP4) in Candida tropicalis. Methods: Ten infected clinical isolates obtained from recurrent vulvovaginal candidiasis patients were used in this study. The broth microdilution assay was utilized to investigate antifungal susceptibilities to fluconazole alone and in combination with clotrimazole and the synergistic effects were interpreted with reference to the fractional inhibitory concentration (FIC) index model. The expression levels of ALS1, ALS2, LIP1, LIP4, SAP2 and SAP4 genes were quantified by real-time RT–PCR. Results: Antifungal susceptibility results showed that isolates were resistant to at least one type of azole antifungals. The combination of fluconazole with clotrimazole revealed synergistic effects against C. tropicalis isolates with FIC90 index ranging from 0.011 to 0.43. The results indicated that combination of fluconazole with clotrimazole could cause a down-regulation of gene expression of ALS1, SAP2, LIP4, SAP4, LIP1 and ALS2 genes, respectively. Conclusions: Fluconazole in combination with clotrimazole may diminish the virulence properties of C. tropicalis.
  4,419 449 2
A review on novel topical formulations of vitamins
Juhi Desai, Rashmi Mallya
July-December 2021, 10(2):159-170
Cosmeceuticals are cosmetic products with biologically active ingredients purporting to have drug-like benefits. Cosmeceuticals are one of the fastest-growing segments of the personal care industry as their use has drastically increased over the years. Vitamins being one of the popular ingredients in cosmeceuticals have numerous skin benefits. Vitamins are organic micronutrients essential for the proper functioning of the body. The popular vitamins used in cosmetics are vitamin A, vitamin B3, vitamin C, vitamin E, and vitamin K. These vitamins play an important role in treating skin conditions like acne, hyperpigmentation, and photoaging, protecting from UV, deactivating free radicals, and improving skin moisture retention levels of the skin. This review article emphasizes on the novel formulation of the vitamins-based cosmeceuticals. The novel carriers system has gained importance in cosmetic delivery due to its advantages such as enhanced skin penetration, sustained and controlled drug release profile, maintenance of the concentration within the therapeutic range, with greater safety and targeted delivery of active to the desired tissues.
  4,229 622 1
Analysis of phenolics in Calligonum polygonoides in vitro cultured roots
Asmaa I Owis, Nada S Abdelwahab, Adel A Abul-Soad
July-December 2019, 8(2):124-127
Background: Calligonum polygonoides L. subsp. Comosum (L’Hér.) Sosk. is an endangered plant species belonging to family Polygonaceae. Although the plant is rich in phytoconstituents and has multipurpose medicinal applications, but in vitro root culture studies and phytochemical investigations of these cultures are rare. Objectives: To establish in vitro root, callus and cell suspension cultures from in vitro germinated fruits of C. polygonoides to investigate the production of phenolics through root, callus and cell suspension cultures and attempt to enhance cell capacity to accumulate phenolics. Materials and Methods: Modified Murashige and Skoog medium supplemented with 1 mg l-1 indole-3-butyric acid was used to establish the root culture. Elicitation of cell suspension culture was performed using salicylic acid and yeast extract. The phenolic compounds in root, callus and cell suspension cultures were evaluated using reversed phase high performance liquid chromatography technique. Results: The unorganized cell suspension culture contained fewer amounts of phenolic compounds than the differentiated roots tissue. Elicitation produced quantitative reprogramming of phenolic content. Conclusion: The present study provides a chance to improve secondary metabolite yield from this valuable natural plant.
  4,271 530 -
Acetyl glycyrrhetinic acid methyl ester as a promising glycyrrhizin derivative against the breast cancer cells (MCF-7)
Mohamed G Ibrahim, Fardous F El-Senduny, Magdy M Youssef, Diaaeldin M Elimam, Fatma M Abdel Bar, Farid A Badria
July-December 2019, 8(2):161-171
Background: Breast cancer remains the most potent threat to women’s life worldwide. So far, no ideal drug for treatment of breast cancer, all available drugs exhibit severe side effects, poor therapeutic index, and high cost. Objective: Therefore, this study aimed to investigate the potential use of the natural pentacyclic triterpenoids such as Boswellic, Betulinic (BA), Urosolic, Oleanolic acids, Glycyrrhizin and their derivatives for treatment of breast cancer. Materials and methods: The cell viability was firstly determined after treatment with 50 µM of each compound. The effect of the treatment on cell cycle, apoptosis, cell migration and colony formation was evaluated. The ability of the new glycyrrhizin derivative to activate p53 was investigated by flow cytometry. Results: The cytotoxicity assay revealed that glycyrrhizin derivative AM-GA (3-acetyl-18β-glycyrrhetinic-30-methyl ester) and BA were the most cytotoxic against breast cancer cell line MCF-7 with IC50 values 4.5±0.1 and 4±0.1 µM, respectively. Both AM-GA and BA were selective towards breast cancer cells rather than the normal lung fibroblast cell line WI-38. Both AM-GA and BA were able to inhibit the cancer cell migration in the wound healing assay and inhibited colony formation. Studying the mechanism of action revealed that AM-GA inhibited the growth of the breast cancer cells via cell cycle arrest at sub-G1 phase, induction of apoptosis and activation of the tumor suppressor protein p53. Conclusion: This work highlights the unique role of AM-GA against breast cancer via different mechanisms and will be the gate for new potent analogues and fights different cancer types.
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Design and development of transdermal drug delivery of nonsteroidal anti-inflammatory drugs: Lornoxicam
HN Shivakumar, Ruchira S Kotian
July-December 2019, 8(2):277-283
Background: Conventional route, the most common route of administration, has drawbacks such as hepatic first-pass metabolism, poor bioavailability, and ability to alter drug concentrations in the blood. These problems can be overcome by a controlled-release drug delivery system, which can be accomplished with the development of transdermal drug delivery system. Objective: The objective of this study was to design and develop a lornoxicam-loaded matrix-type transdermal films with different permeation enhancers and determine their physicochemical characteristics. Materials and Methods: Lornoxicam-loaded transdermal films were prepared by the solvent evaporation technique. The Fourier transform infrared spectroscopic studies were performed to determine the drug–excipient interactions. Six formulations were prepared with different permeation enhancers such as propylene glycol, dimethylformamide, dimethyl sulfoxide (DMSO), sodium lauryl sulfate, Span 20, and TWEEN 80 by using 500 mg of sodium alginate as the polymer and 60% w/w glycerin as the plasticizer. The prepared formulations were evaluated for thickness, uniformity of weight, moisture loss, moisture uptake, drug content, and tensile strength. The effect of different permeation enhancers on diffusion was determined through a shed snakeskin by using Franz diffusion cells. Results: The preformulation studies conducted were fulfilled to design a matrix-type transdermal film. In vitro diffusion 24 h indicated that the steady state flux were in the order of F3 > F2 > F1 > F6 > F5 > F4. It was observed that the film prepared with DMSO showed higher diffusion than the formulations with other permeation enhancers. Conclusion: It was concluded that permeation enhancer to prepare lornoxicam-loaded matrix-type transdermal film to improve patient compliance.
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Ethanol extract of jati belanda (Guazuma ulmifolia L.) as therapy for chronic kidney disease in in vitro model
Sijani Prahastuti, Meilinah Hidayat, Stella Tinia Hasiana, Wahyu Widowati, Annisa Amalia, Rismawati Laila Qodariah, Rizal Rizal, Hanna Sari W Kusuma, Zakiyatul Khoiriyah
July-December 2019, 8(2):229-235
Background: People with diabetes mellitus in Indonesia are predicted to increase until 2035. High glucose in body (hyperglycemia) leads to increased fibronectin synthesis. Fibronectin that gets accumulated in glomerulus (mesangial cells), at the end, will lead to diabetic glomerulosclerosis. Jati belanda (Guazuma ulmifolia L.) leaf is well known as an Indonesian traditional medicine to have effects as antidiabetic by the presence of its secondary metabolites such as alkaloid, tannin, saponin, flavonoid, and terpenoid, which are very important in health recovery. Objectives: To evaluate the activity of ethanol extract of jati belanda (EEJB) as a protection agent on induced-glucose mesangial cells of SV40 MES 13 cell line (glomerular mesangial kidney, Mus musculus). Materials and Methods: EEJB (3.125 and 6.25 µg/mL) was extracted based on maceration method using ethanol (70%) as the solvent. Proliferation and viability were performed based on (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) (MTS) method. The level of transforming growth factor β1 (TGF-β1) and fibronectin in glucose-induced mesangial cells was assayed and determined using enzyme-linked immunosorbent assay kit. Reactive oxygen species (ROS) level was measured using flow cytometer. Results: EEJB (3.125 and 6.25 µg/mL) increased cell proliferation and viability in glucose-induced mesangial cells and significantly reduced the level of TGF-β1, fibronectin, and ROS compared to that in positive control (glucose-induced cells). Conclusion: Our study suggests that EEJB is able to reduce TGF-β1, fibronectin, and ROS levels in glucose-induced mesangial cells, which correlate to diabetic glomerulosclerosis condition and increase the mesangial cell proliferation and viability.
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Phytochemical analysis and evaluation of purified extract of Tinospora crispa stem for in vivo antihyperuricemic effect
Harwoko Harwoko, Warsinah Warsinah
January-June 2020, 9(1):46-51
Background: Tinospora crispa is used in folk medicines for the treatment of gout, rheumatoid arthritis, and internal inflammation. The presence of flavonoids, polyphenols, glycosides, and alkaloids in T. crispa stem is supposed to contribute to these therapeutic effects. This study aimed to analyze qualitative and quantitative phytochemical of purified extract of T. crispa stem (PETS) and to evaluate the in vivo antihyperuricemic effect. Materials and Methods: First, total flavonoid and total alkaloid contents of PETS were determined by colorimetric and gravimetric methods. After that, potassium oxonate-induced hyperuricemic mice were treated with three doses of PETS at 50, 100, and 200 mg/kg, and hydroalcoholic extract at 500 mg/kg. Moreover, allopurinol at 10 mg/kg and sodium carboxymethylcellulose 0.5% were orally administered as positive and negative controls, respectively. Serum uric acid levels were measured by ultraviolet–visible spectrophotometry. Results: The high flavonoids content (31.08% ± 1.77% rutin equivalent) in T. crispa stem possesses a potential as uricostatic in the treatment of gout. The purified extract of T. crispa stem at a dose of 100 mg/kg revealed a significant uric acid–lowering effect compared with negative control (P < 0.05). Conclusion: This study indicates the potential of T. crispa purified extracts in the treatment of hyperuricemia and gout.
  4,268 398 3
The effect of ibuprofen on expression of Cox-1/2-related miRNAs in MKN- 45 -derived cancer stem-like cells
Hassan Akrami, Behnam Karimi, Zohreh Salehi, Sajjad Sisakhtnezhad
January-June 2019, 8(1):18-23
Context: Ibuprofen is an anti-inflammatory drug that non-selectively blocks cyclooxygenases-1/2 (COX-1/2) enzymes and thus reduces the risk tumorigenesis. This study was designed to detect microRNAs (miRNAs) that target Cox-1/2 mRNA and to investigate the effect of ibuprofen on the expression of the miRNAs in MKN-45-derived gastric cancer stem-like cells (CSLCs). We were also aimed to find signaling pathways modulated by the miRNAs. Subjects and Methods: The miRWalk database was used to recognize miRNAs that targeted Cox-1/2 genes. CSLCs were derived from MKN-45 cell line and were then treated with ibuprofen. Consequently, the effect of ibuprofen was evaluated on the expression of the miRNAs by quantitative real-time polymerase chain reaction (qRT-PCR). Finally, DIANA tools were used to identify signaling pathways that modulated by the miRNAs. Results: Our bioinformatic investigation showed that hsa-mir-16-5p, hsa-mir-483-5p, and hsa-mir-4669 targeted both Cox-1 and Cox-2 mRNAs. The qRT-PCR results indicated that hsa-mir-16-5p and hsa-mir-4669 were overexpressed 2.34 and 9.47 folds, respectively, while hsa-mir-483-5p under-expressed (2.08 folds) in ibuprofen-treated CSLCs relative to untreated cells. Moreover, it found that these miRNAs are involved in PI3K-Akt, P53, transforming growth factor-beta, phosphatidylinositol and insulin signaling pathways, cell cycle, extracellular matrix receptor interaction, gap junction, small cell lung cancer, prostate cancer, and chronic myeloid leukemia. Conclusions: We suggest that ibuprofen may reduce the risk of gastric cancer by affecting the expression of miRNAs that target Cox-1/2. however, further research is necessary to unravel its exact effects.
  4,102 541 2