|
 
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| REVIEW ARTICLE |
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| Year : 2021 | Volume
: 10
| Issue : 2 | Page : 171-181 |
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Herbal nanoemulsion in topical drug delivery and skin disorders: Green approach
Chanchal Chaurasiya1, Jitendra Gupta2, Sachin Kumar1
1 Department of Pharmaceutics, NKBR College of Pharmacy and Research Centre, Meerut, India
2 Department of Pharmaceutics, GLA University, Mathura, Uttar Pradesh, India
| Date of Submission | 15-May-2020 |
| Date of Acceptance | 28-Jul-2021 |
| Date of Web Publication | 17-Dec-2021 |
Correspondence Address:
Mrs. Chanchal Chaurasiya
Department of Pharmaceutics, NKBR College of Pharmacy and Research Centre, L-342, Shastri Nagar, Meerut, Uttar Pradesh
India
 Source of Support: None, Conflict of Interest: None  | Check |
DOI: 10.4103/jrptps.JRPTPS_64_20
A topical drug delivery system can be a future trend for drug delivery because of the availability of the largest surface area of skin than any other organ. Although the skin has some advantages such as ease of application, patient compliance, and safety, it has many disadvantages such as permeability and bioavailability via first-pass metabolism and others. Nanoemulsion can be a future trend for topical delivery of drugs because of its very fine droplet size range, lipophilic and/or hydrophilic nature, and suitability for various administration routes such as parenteral, oral, topical, intranasal, ocular, and pulmonary. The contents of nanoemulsions make them suitable for human use because the oil/lipid, water, surfactants, and co-surfactants used in the formulation of nanoemulsion are relatively safe and nontoxic. Nowadays, people are more attracted to natural preparations as of their inherited qualities and fewer side effects. Due to herbal drugs’ compatibility in nanoemulsion, it is considered the best technology for the green approach of the medicine system. The article presented the foundation for the above statement by different literature surveys on the herbal nanoemulsion formulations. Keywords: Co-surfactant, greens, nanoemulsion, surfactant, topical delivery
How to cite this article:
Chaurasiya C, Gupta J, Kumar S. Herbal nanoemulsion in topical drug delivery and skin disorders: Green approach. J Rep Pharma Sci 2021;10:171-81 |
| Introduction | |  |
Human skin is a stratified epithelium, covering 1.6 m2 of surface region and representing roughly 16% of a grown-up’s body weight and consist of a different cell type that performs a distinct function. In direct contact with the outside condition, the skin assists with keeping up four basic body functions: (1) maintenance of dampness and counteraction of pervasion or loss of different molecules, (2) maintenance of body temperature, (3) assurance of the body from organisms and destructive outer impacts, and (4) sensation.[1]
The skin may be comprehensively partitioned into the outer epidermis, dermis, and undermost hypodermis [Figure 1]. In addition, the epidermis can be divided from outside to within into stratum corneum (horny layer), stratum granulosum (granular layer), stratum spinosum (prickle cell layer), and stratum basale (Stratum germinativum). The stratum basale and spinosum are considered known as the malpighian layer. The additional layer stratum lucidum can be seen on the part of the body with thickened skin example, the palm and bottom of the foot. The hair follicle and sweat glands cross different skin layers.[2]
Skin is the primary course of the topical drug delivery system. Skin disease affects the population and has been cited as one of the top 15 ailments for which prevalence and medical service expanded in the most recent decade.[4] Improvement in the biological sciences with an increasing dermatological market increases the advent of batter topical formulations. Topical drug delivery systems include a wide range of pharmaceutical dosage forms such as solid powders, semisolids, liquids, and sprays preparations. Gels, creams, and ointments are mostly used in semisolid preparation for topical drug delivery. There are the following advantages associated with topical drug delivery systems:[5]
Patient acceptance and compliance,
Ease of application,
Noninvasive and painless method of administration,
Improved drug bioavailability,
Good pharmacological and physiological responses
Minimum systemic toxicity
Minimum exposure of the drug to non-infectious tissue sites.
In addition to the advantages elucidated here, the major challenge in topical delivery is the permeability of the drug across skin and bioavailability profile. Nanoemulsions have been developed to defeat debilitated drug permeation following the topical application as shown in [Figure 2].[6],[7] | Figure 2: Topical absorption of conventional dosage form and nanoemulsion
Click here to view |
In addition, as an emulsion, either o/w or w/o is scattering of two liquids that are immiscible, stabilized by using a suitable surface active agent, the nano suffixed for its mean droplet size radius achieved in normally less than 500 nm.[8],[9]
Nanoemulsions may be formulated in a variety of delivery forms, such as oils, creams, sprays, gels, aerosols, foams, and may be administered uniformly through different routes, such as topical, dental, intravenous, intranasal, pulmonary, and ocular.[10],[11]
[TAG:2]Advantages of Nanoemulsions[12][/TAG:2]
Because of the nanosize and wide interfacial area of the droplets, there is an improvement in solubility, dissolution, absorption, permeation, and bioavailability.
The physical stability of herbal bioactive can be improved by encapsulation into the nanoemulsion matrix.
As oils/lipids are compatible with the body, quickly metabolized, and nontoxic, the nanoemulsions are safe for human health.
Allows a targeted and sustained transfer of active molecules.
Toxic effects of the drug can be minimized due to a reduction in dose and provide better therapeutic effects.
Due to their solubilization and transportation ability of both hydrophobic and hydrophilic active compounds with unusual physical properties, nanoemulsion has been the subject of extensive research globally.[13]
It improves plasma drug concentration because it avoids first-pass metabolisms.
Provides value-added nutraceutical and dietary supplement distribution system.
Improve patient compliance.
| Formulation of Nanoemulsion | | |
- Oils: O/W nanoemulsions consist of 5%–20% oil/lipid as disperse phase, even sometimes it may be more significant up to 70%. Lipids/oil used in nanoemulsions is usually based on the solubility of the drug.[14] It helps to facilitate emulsification to increase the solubility of the water-insoluble drug in the oil droplets. It also improves the absorption of the oral drug by increasing the gastrointestinal drug permeation through the intestinal lymphatic. For topical formulations, it functions as a penetration enhancer that facilitates drug permeation in the skin.[15],[16]
- Surfactants: Surfactants are the agent that minimizes the interfacial tension of oil and water and act as the emulsifier in the formulation of nanoemulsion. They rapidly adsorb on the oil and water interface and provides steric or electrostatic, or double electro-steric stability. HLB value plays an integral part in the selection of appropriate surfactants. 30–60% v/v concentration of surfactant is used to produce a stable emulsion.[17],[18] Lecithin (phosphatidylcholine) is derived from egg yolk or soybean and is used as a common surfactant used in nanoemulsions.[19]
- Cosurfactants: Cosurfactants are used to increase the effectiveness of surfactants. It should be used in smaller concentrations owing to its adverse side effects at greater concentrations.[20],[21]
- Stabilizers: Different kind of stabilizers is used to overcome the instability issues of nanoemulsion such as flocculation, coalescence, Ostwald ripening, and gravitational separation.[21] The contents of nanoemulsion are summarized in [Figure 3].
| Green Approach | | |
The importance of herbal drugs and formulations is increased worldwide for all sorts of diseases. People are well aware of the ingredients, therapeutic and medicinal properties of the ingredients of their daily diet. Plants have a no. of very beneficial bioactive compounds, which work as a backbone of the conventional medicine system. Numerous sorts of diseases have been known to be treated with natural cures. This action is because of the presence of phytochemical components such as glycosides, tannins, alcohols, and aldehydes. People are attracted to the herbal medicine system because of its fewer side effects and low-toxicity profile.
Because of the quick staged way of life and polluted environment, individuals are presented with numerous ways of life, particularly skin diseases.[22]
Examples of few herbs that are effective in some diseases are given in [Table 1].[21],[22]
| Importance of Nanoemulsion in Delivery of Herbal Drugs | | |
Either the most recent decades, it has become a pushed region of research for some specialists and trailblazers all through the world because of their medical advantages; however, the pharmaceutical use of natural bioactive and phytopharmaceuticals is restricted with low solubility, permeability, and bioavailability. It has become the most significant obstacle for the effective use of natural bioactive against different health complications. These hurdles can be solved with the formulation of nanoemulsion of herbal drugs.[23] Nanoemulsion is considered the best technology because of its:[24]
Damp or smooth behavior,
Eminent interaction with the skin cells,
Small droplet dimension,
Efficient permeability,
Protection
Capability to convey volatile, irritant, and high molecular weight drugs evenly.
Nanoemulsions easily associate with the skin cells due to their fluidic behavior and emulsifier properties at the interface.
Nanoemulsion leads to provide better efficacy and interaction due to surface charge over nanoemulsion.
| Formulation and Development of Herbal Nanoemulsion | | |
Prior to the production of a quality nanoemulsion product, it is necessary to note the choice of ingredients, their correct concentration, an order of addition, proper preparation method, optimum stirring speed, and shear stress. There are several techniques that are used for the preparation of nanoemulsion [Figure 4]:[25]
| High-Energy Methods | | |
The method is called high energy because it uses high mechanical energy using no mechanical devices such as ultrasonicators, microfluidizers, and high-pressure homogenizers to provide strong disruptive forces, which breaks large size droplets into nanosized droplets and produce nanoemulsions with high kinetic energy.[26],[27] High-energy methods provide better control of particle size with a choice of formulation composition, stability, rheology, and color of the emulsion.[28] High-energy methods contain a no of methods that are given below.
High-pressure homogenization
High-pressure homogenization creates intense turbulence and shear flow to the nanoemulsion mixture under very high pressure, resulting in the breakage of the dispersed phase into small droplets, that is, less than 100–1 nm. The relative flux between the droplets governs the dynamic equilibrium between breakage and coalescence, due to which homogenous droplets with better shelf life and texture characteristics are produced.[29]
Microfluidization
Microfluidization is a high-pressure homogenization technique used to develop a highly dispersed system. A microfluidizer co-existently uses hydraulic shear, impact, attrition, impingement, intense turbulence, and cavitation for effective size reduction. It forces feed material through an interaction chamber consisting of microchannels under the influence of a high-pressure displacement pump (500–50,000 psi), which results in the formation of very fine droplets.[30],[31] Precarious and finest nanoemulsion particles are produced in microfluidizers than homogenizers and produce stable nanoemulsions at low surfactant concentrations.[32],[33]
Ultrasonication
Ultrasonicator is used in this method to convert macroemulsion into nanoemulsion. Ultrasonicator is consists of a probe that emits ultrasonic waves. The desired particle size and stability of nanoemulsion is achieved by varying ultrasonic energy input and time. In ultrasonication, the acoustic cavitation process is used to provide physical shear. Cavitation is a process of the development and growth of microbubbles, accompanied by the collapsing of microbubbles, caused by pressure changes in the acoustic wave. The formation of nanosized droplets results from the intense turbulence caused by the collapse of microbubbles.[34],[35]
| Low-Energy Methods | | |
Low-energy emulsification methods use the system’s intrinsic chemical energy and require delicate mixing for the preparation of the nanoemulsions.[36],[37]
Phase inversion emulsification method
spontaneous surfactant curvature occurs by changes in variables such as temperature and composition induces phase transition in the process of emulsification.[38] Phase inversion emulsification methods are of two types: transitional phase inversion (TPI) methods, which involve phase inversion temperature (PIT) method and phase inversion composition (PIC), and continuous phase inversion (CPI) methods, which involve emulsion inversion point (EIP).
TPI happens due to the changes in random curvature or orientation of the surfactant due to variation in the variables such as temperature and composition.[39],[40] However, CPI occurs when the scattered phase is gradually inserted as the scattered phase droplets are collated together to create bicontinuous/lamellar structural phases.[36] In the PIT method, the curvature of the surfactant is reversed by altering temperature. The PIC method is identical to the PIT method; however, in PIC, inversion is accomplished by adjusting the system composition instead of the system temperature.[37] In PIC, one element such as water is introduced to the mixture, and oil/lipid -surfactant or oil/lipid is added to the water-surfactant mixture. In the EIP method, phase inversion occurs through CPI mechanisms. The catastrophic phase inversion is caused due to change in the fractioned volume of the dispersed phase instead of the properties of the surfactant.[38]
Self-nanoemulsification method
Formation of nanoemulsion formation without changing the spontaneous curvature of the surfactant is achieved in the self-emulsification method. Surface active agents and/or co-solvent molecules are quickly diffuse from the scattered phase to the continuous phase, which triggers turbulence and generates nanosized emulsion droplets.[35],[36]
| Successful Topical Herbal Nanoemulsion Formulations | | |
With the help of literature, numbers of successful herbal nanoemulsion formulations were found and presented, as shown in [Table 2].{Table 2}
| Conclusion | | |
With a number of skin functions, there are a few significant challenges in drug delivery through the topical route. Nanoemulsion defeats these limitations and is found to be one of the best formulations for topical drug delivery, and nanoemulsion can also be formulated in a variety of delivery forms. In the era of allopathic medicines, people are attracted to green approaches because of varying and favorable qualities to use in many pathological and physiological health conditions. The study results and exemplifies that an herbal drug’s nanoemulsions can become the future fashion for both therapeutic and non-therapeutic applications[69].
Financial support and sponsorship
Nil.
Conflicts of interest
There are no conflicts of interest.
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[Figure 1], [Figure 2], [Figure 3], [Figure 4]
[Table 1], [Table 2]JRepPharmaSci_2021_10_2_171_332786_t6.jpg
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