Nanosized ethanol based malleable liposomes of cytarabine to accentuate transdermal delivery: formulation optimization,in vitroskin permeation andin vivobioavailability

Abstract

Cytarabine is a pyrimidine nucleoside analog used predominantly for acute myeloid leukemia (AML) and also for other indications, including acute lymphocytic leukemia, chronic myelogenous leukemia, and lymphoma by parenteral route due to its low oral bioavailability. Parenteral administration requires constant plasma level, monitoring for its fluctuation and poor patients compliances. Hence the objective of this work is to construct optimized nanosized malleable liposomes of cytarabine to accentuate transdermal delivery of drug to circumvent previously mentioned drawbacks. We also investigated its characteristics and therapeutic efficiency and attempted to systematically explore the penetration enhancing property. Well characterized ethanolic liposomes were also biologically tested for dermatological safety and systemic bioavailability. Ethanolic liposomes were found to be spherical having nanometric size with low polydispersity and high encapsulation efficiency. Skin permeation and deposition studies revealed significant enhancement. In vivo, skin irritation study of developed formulation showed no erythema or scaling vis-à-vis the liposomes. Blood profile of this novel formulation indicated lower lag time with the high amount of drug within 3-12 h after transdermal administration demonstrating the enhanced percutaneous penetration of cytarabine with no erythema, thus leading to patient's compliance by alternative delivery of drug for the treatment of leukemia.

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