title: Formulation of niosomal gel for enhanced transdermal lopinavir delivery and its comparative evaluation with ethosomal gel.
abstract: The aim was to develop niosomal gel as a transdermal nanocarrier for improved systemic availability of lopinavir. Niosomes were prepared using thin-film hydration method and optimized for molar quantities of Span 40 and cholesterol to impart desirable characteristics. Comparative evaluation with ethosomes was performed using ex vivo skin permeation, fluorescence microscopy, and histopathology studies. Clinical utility via transdermal route was acknowledged using in vivo bioavailability study in male Wistar rats. The niosomal formulation containing lopinavir, Span 40, and cholesterol in a molar ratio of 1:0.9:0.6 possessed optimally high percentage of drug entrapment with minimum mean vesicular diameter. Ex vivo skin permeation studies of lopinavir as well as fluorescent probe coumarin revealed a better deposition of ethosomal carriers but a better release with niosomal carriers. Histopathological studies indicated the better safety profile of niosomes over ethosomes. In vivo bioavailability study in male Wistar rats showed a significantly higher extent of absorption (AUC(0→∞), 72.87 h × μg/ml) of lopinavir via transdermally applied niosomal gel as compared with its oral suspension. Taken together, these findings suggested that niosomal gel holds a great potential of being utilized as novel, nanosized drug delivery vehicle for transdermal lopinavir delivery.
authors.affiliation: Centre for Research in Pharmaceutical Sciences, The M.S. University of Baroda, Shri G.H. Patel Pharmacy Building, Vadodara, 390002, India.
authors.forename: Ketul K
authors.initials: KK
authors.lastname: Patel
authors.forename: Praveen
authors.initials: P
authors.lastname: Kumar
authors.forename: Hetal P
authors.initials: HP
authors.lastname: Thakkar
mesh_terms: D000279:Administration, Cutaneous; D000284:Administration, Oral; D000818:Animals; D019380:Anti-HIV Agents / Q000008:administration & dosage / Q000737:chemistry; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002784:Cholesterol / Q000737:chemistry; D003374:Coumarins / Q000008:administration & dosage / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D005782:Gels / Q000008:administration & dosage / Q000737:chemistry*; D008081:Liposomes / Q000008:administration & dosage / Q000737:chemistry*; D061466:Lopinavir / Q000008:administration & dosage* / Q000737:chemistry*; D008297:Male; D010316:Particle Size; D010539:Permeability; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D013535:Suspensions / Q000008:administration & dosage / Q000737:chemistry
chemical_list: D019380:Anti-HIV Agents; D003374:Coumarins; D004337:Drug Carriers; D005782:Gels; D008081:Liposomes; D013535:Suspensions; D061466:Lopinavir; D002784:Cholesterol; C030123:coumarin