Therapeutic benefits of natural oils along with permeation enhancing activity.

The skin is the largest organ of the integumentary system with a multifunctional purpose to protect the body from heat and microbes, regulate body temperature, and act as a sensory organ. A topical dosage form applied on the skin will have to cross the stratum corneum, which would then allow the dosage form to traverse the subsequent layers of the skin. The drug with poor solubility and short half-life would serve as an ideal candidate for its delivery via the transdermal route. This review reports the role of natural oils in enhancing the permeation of drugs through skin as they possess different features like natural origin, favorable penetration enhancement, and partitioning action in the skin. Chemical penetration enhancers have been used widely but are associated with toxicities. Thus, more research should be channelized in the area of extraction of oils from natural sources, along with their active constituents, which can serve as therapeutic alternatives to various disorders and diseases. Natural oils are obtained from leaves, fruits, flowers, seeds, bark, and roots, which have a therapeutic potential as well as penetration enhancing activity. The demerits of oral drug delivery include degradation of drugs in the gastrointestinal tract, addition of taste masking, and coating of tablets, which can be overcome by delivering the drug via the transdermal route. Natural oil contains lipids, flavonoids, and terpenes, which play a significant role in anti-inflammatory and penetration enhancing activity.

Formulation evaluation of ketoconazole microemulsion-loaded hydrogel with nigella oil as a penetration enhancer.

BACKGROUND: Onychomycosis is an opportunistic fungal infection often infecting people with compromised immune system. Currently available treatment interventions such as physical, surgical, and chemical-based approaches are successful in treating the condition, however, are painful and nonpatient complaint. Moreover, dermal creams with antifungal agents do not penetrate nail plate as required; hence, there is a necessity of developing a novel formulation with enhanced penetration. AIMS: The aim of the present research work was to develop ketoconazole microemulsion-loaded hydrogel formulation containing nigella oil as permeation enhancer for the treatment of onychomycosis. METHODS: Screening of oils, surfactants, and cosurfactants were done based on solubility studies followed by the construction of pseudo-ternary phase diagrams with 2% ketoconazole. The microemulsion was characterized for globule size, zeta potential, viscosity, and thermodynamic stability. Ex-vivo studies were carried out using Franz diffusion cells using porcine skin membrane. The antifungal activity of microemulsion-loaded hydrogel was evaluated using cup plate method using Candida albicans and Aspergillus niger. RESULTS: The optimized microemulsion had a composition of 54.97% Capryol:Nigella (2:1), 36.07% Transcutol:Propylene glycol (2:1), and 7.13% water and was later incorporated into polymeric gel base. The microemulsion-loaded hydrogel exhibited a 10 hours sustained release profile as compared to the marketed cream and an enhanced activity against marketed ketoconazole cream and compared with marketed ketoconazole formulation. CONCLUSION: The thermodynamic stability, sustained drug release with greater permeation, and enhanced activity due to the presence of nigella oil in microemulsion-loaded hydrogel warrant its application as an excellent vehicle for treating fungal infections.

Polymeric Lipid Hybrid Nanoparticles: Properties and Therapeutic Applications.

Some of the criteria for selection of a viable nanocarrier formulation currently being explored are the development of a site-specific and bioavailable formulation. Although the literature reports a variety of techniques for fabrication of nanocarrier systems, their stability and scale-up issues are a concern for their prominence in the pharmaceutical industry. The other widely recognized drawbacks of nanoparticulates, i.e., polymeric nanoparticles and lipid vesicular nanoparticles (liposomes), are low circulatory half-lives due to reticuloendothelial system (RES) uptake and leaky architecture leading to burst kinetics. Polymeric lipid hybrid nanoparticles (PLHNs) or lipomers are the recent advancement in nanodrug delivery systems composed of a polymeric core and lipid shell which imparts physicochemical stability and biocompatibility to the nanoparticles. The lipomers are a blend of positive attributes of both liposomes and polymeric nanoparticles wherein their individual innate flaws are negated. An extensive study of PLHN was engineered using single/two or multiple methods carried out for encapsulation efficiency, physicochemical properties, and stability. The influence of shape and composition of PLHN has also shown promising results in terms of reticuloendothelial uptake. These PLHNs have shown to hold a promising place in designing drug delivery systems for the treatment of cancer and infectious diseases as well as for theranostic purposes. The present review article encompasses various types of PLHNs, their physicochemical characteristics, and their applications as future perspectives in strategizing drug delivery to their desired sites of action.