Novel drug delivery systems are now a days is creating a new interest in development of drug deliveries. Vesicular drug delivery system is also a part of these novel drug delivery systems. TDDS is the permeability of the skin, it is permeable to small molecules, lipophilic drug and highly impermeable to the macromolecules and hydrophilic drugs. Recent approaches have resulted in design of two vesicular carriers, ethosomes and ultra flexible lipid based elastic vesicles, transferosomes. Transferosomes have recently been introduced, which are capable of transdermal delivery of low as well as high molecular weight drugs. This offers several potential advantages over conventional routes like avoidance of first pass metabolism, predictable and extended duration of activity, minimizing undesirable side effects, utility of short half life drugs, improving physiological and pharmacological response and have been applied to increases the efficiency of the material transfer across the intact skin, by the use of penetration enhancers, iontophoresis, sonophoresis and use of colloidal carriers such as lipid vesicles (liposomes & proliposomes) and non-ionic surfactant vesicles (niosomes & proniosomes). It is suitable for controlled and targeted drug delivery and it can accommodate drug molecules with wide range of solubility. Due to its high deformability it gives better penetration of intact vesicles. They are biocompatible and biodegradable as they are made from natural phospholipids and have high entrapment efficiency. The preparation variables are depending upon the procedure involved for manufacturing of formulation and the preparation procedure was accordingly optimized and validated. Characterization of transferosomes can be done to know the vesicle size, morphology, drug content, entrapment efficiency, penetration ability, occlusion effect, surface charge, in vitro drug release, in vitro skin penetration etc., It increases stability of labile drugs and provides control release. Transferosomes thus differs from such more conventional vesicles primarily by its softer, more deformable, better adjustable artificial membrane.
Transfersomes are particularly optimized, ultradeformable (ultraflexible) lipid supramolecular aggregates, which are able to penetrate the mammalian skin intact. Transfersome is a type of carrier system which is capable of transdermal delivery of low as well as high molecular weight drugs. Transfersomes penetrate through the pores of stratum corneum which are smaller than its size and get into the underlying viable skin in intact form. Acne vulgaris is a disease of the pilosebaceous follicle characterized by non-inflammatory (open and closed comedones) and inflammatory lesions (papules, pustules, and nodules). In such situation transdermal drug delivery remains the most preferential mode of administration. But, stratum corneum forms the most formidable barrier for the penetration of drug through skin. To overcome the stratum corneum barrier, the use of lipid vesicles like transfersomes in delivery systems has involved increasing attention in recent years. The aim of the present study was to statistically optimize the vesicular formulations (Transfersomes) for enhanced skin delivery of a model drug Clindamycin Phosphate. Keywords: Transfersomes, Acne vulgaris, Clindamycin Phosphate
Delivery across skin is striking due to its easy convenience. However, drug delivery across skin is still a confront in biomedical sciences. Over the past few decades, various successful narrative devices and techniques have emerged to optimize drug delivery across skin whose barricading behaviour constricts entry of most of the therapeutic agents. Ethosomes are non-invasive delivery transporter that enables drugs to reach the deep skin layers and/or the systemic circulation. Although ethosomal systems are theoretically sophisticated, they are characterized by simplicity in their preparation, efficacy and safety. A combination that can highly inflate their application. Ethosomes are soft, malleable vesicles adapted for enhanced delivery of active agents. This article reviews work carried out method of preparation, application and characterization of ethosomal systems. Because of their exceptional structure, ethosomes are able to encapsulate and deliver through the skin highly lipophilic molecules such as testosterone, cannabinoids and minoxidil as well as cationic drugs such as trihexyphenidil and propranolol. Results obtained in a double-blind two-armed randomized clinical study showed that treatment with the ethosomal acyclovir formulation appreciably improved all the evaluated parameters. In further work, the ethosomal expertise was broadened to introduce agents into cultured cells and microorganisms. Enhanced delivery of bioactive molecules through the skin and cellular membranes by means of an ethosomal transporter opens numerous confronts and prospects for the research and future development of novel improved therapies. Keywords: Ethosomes, Skin layers, Characterization
Curcumin (diferuloylmethane) is a natural polyphenolic compound with potent anti-inflammatory, anticancer and antioxidant activities. However, its bioavailability is low as it is poorly absorbed in the gastrointestinal tract. Microemulsions offer the potential to improve the solubility and bioavailability of bioactive compounds; the present work investigated the topical delivery potential of microemulsion gel loaded with curcumas. Curcumin microemulsion was prepared by spontaneous emulsification method using oil (Oleic acid), surfactant:cosurfactant (Smix) (Ethanol and Tween 80, Span 80 and n Butanol) and water. The optimized formulations of microemulsions were subjected to thermodynamic stability tests. After stability study, stable formulation was characterized for droplet size, pH determination, centrifugation, % drug content in microemulsion, zeta potential and vesicle size measurement and then microemulsion gel were prepared and characterized for spreadability, measurement of viscosity, drug content, In-vitro diffusion, in-vitro release data. Tween 80, Span 80 was selected as surfactant, ethanol, n Butanol as co surfactant and Oleic acid as oil component based on solubility study. The optimized formulation contained Curcumin (10 mg). The in vitro drug release from curcumin microemulsion gel was found to be considerably higher in comparison to that of the pure drug. The in-vitro diffusion of microemulsion gel was significantly good. Based on this study, it can be concluded the solubility and permeability of curcumin can be increased by formulating into microemulsion gel. Keyword: Curcumin, Microemulsion, In-vitro diffusion, Spreadability, Zeta potential, Stability, span 40
Acyclovir has low bioavailability mainly due to low solubility. This study aimed to formulate an optimized acyclovir (ACV) nanoemulsion gel for the slow, variable and incomplete oral drug absorption in patient suffering from herpes simplex viral infection. The dispersion solubility of acyclovir was studied in various oils, surfactants and co-surfactants and by constructing pseudo phase ternary diagram nanoemulsion area was identified. The optimized formulations of nanoemulsions were subjected to thermodynamic stability tests. After stability study, stable formulation was characterized for droplet size, pH determination, centrifugation, % drug content in nanoemulsion, Zeta Potential and Vesicle size measurement and than nanoemulsion gel were prepared and characterized for spreadability, measurement of viscosity, drug content, In-vitro diffusion, in-vitro release data. Span 40 was selected as surfactant, PEG 400 as co surfactant and castor oil as oil component based on solubility study. The in vitro drug release from acyclovir nanoemulsion gel was found to be considerably higher in comparison to that of the pure drug. The in-vitro diffusion of nanoemulsion gel was significantly good. Based on this study, it can be concluded the solubility and permeability of acyclovir can be increased by formulating into nanoemulsion gel. Keywords: Acyclovir, Nanoemulsion, In-vitro diffusion, Zeta potential, Stability
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