Formulation Development and In-Vitro Evaluation of Glycerosomes Containing Mionoxidil for Topical Application

Background and Objective: Novel vesicular systems provide an alternative to improve drug delivery into and through the skin. Glycerosomal vesicles have shown their ability to increase dermal drug delivery. More over, glycerosomes offer a promising avenue to fulfill the need for a transdermal drug delivery system, can act as drug containing reservoir and the modification of the vesicular compositions or surface properties can adjust the drug release rate and the affinity for the target site. Androgenetic alopecia is the most common form of alopecia in men and women. Topical minoxidil (ROGAINE 2%) became first FDA-approved medication for stimulating hair growth. In the present study an attempt has been made to improve the skin penetration of minoxidil by encapsulating it in Glycerosomes. Method : Minoxidil glycerosomes were prepared using soya lecithin, cholesterol with different concentration of glycerol(20%, 30% and 40%) by lipid thin film hydration. Design expert 13 version has been used for the optimization of formulation. Nine formulations of minoxidil loaded glycerosomes were prepared based on 32 factorial designs. The prepared systems were characterized for size, zeta potential, shape, entrapment efficiency and in vitro drug release. Results:Among the nine formulations F1 was selected as optimized formulation. Glycerosomes showed spherical morphology, smooth, vesicular in nature morphologically same without clusters and size range was found to be 120.63 and 186.4 nm. The entrapment efficiency was found in the range of 70.47 to 89.58% and drug release extended upto 13 hours. The kinetics of in vitro drug release of glycerosomes follow zero order and non- fickian diffusion mechanism. Interpretation and conclusion: Minoxidil glycerosomes containing 40% of glycerol were found to be the effective formulation on the basis of optimization using DOE among all the other formulations and were incorporated into HPMC K100 M gel. The formulated gel was evaluated for appearance, pH, drug content, viscosity and in vitro drug release. The study has demonstrated the potential of minoxidil glycerosomes incorporated in gel, for the enhancement of topical absorption, which will be beneficial for topical application in androgenetic alopecia.