Bosentan Monohydrate Vesicles Loaded Transdermal Drug Delivery System: In Vitro In Vivo Evaluation

Revathi M., Indira Y.


This study elucidates the enhancement of the permeation of bosentan monohydrate through skin by encapsulating it in
vesicles loaded transdermal delivery system. Niosomal vesicles were formulated by ether injection method. Formulation
FN7 (span 60: cholesterol: poloxamer 401, 1.25:1:0.25) showed maximum entrapment efficiency of 96.7±0.037% and
was optimized for loading in to transdermal system. Transdermal systems were formulated using both hydrophilic and
hydrophobic polymers like HPMC, HEC and EC. Formulation F1 with HPMC was optimized based on in vitro release
(99.21±1.45 %) and was further evaluated for ex-vivo permeation. The results indicate that the ex vivo release
(98.13±1.65%) was as par with in vitro release and followed zero order super case- II transport mechanism. The in vivo
studies were done on New Zealand male rabbits for oral and transdermal route. The results inferred no significant change
in half-life of drug but a substantial difference in Tmax, AUC and MRT was observed in transdermal systems. A two fold
increase in AUC was observed in transdermal route (18.609±7.251µg/ml/h) when compared to oral route
(9.644±5.621µg/ml/h). A controlled release was attained up to 35h and reservoir effect was observed and this may be due
to the barrier properties of skin. Drug encapsulated niosomes were released in to the skin by loosening the lipid layers
and the surfactant acted as penetration enhancer. The study infers that niosomes loaded transdermal patches of bosentan
monohydrate can enhance the bioavailability and provided controlled release for better therapeutic efficacy and safety of drug.


Bosentan monohydrate, niosomes, transdermal drug delivery, ex vivo permeation studies, in vivo kinetic studies.

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