Nano-transfersomal Formulations for Transdermal Delivery of Asenapine Maleate: In Vitro and in Vivo Performance Evaluations

Shreya, AB and Managuli, Renuka S and Menon, Jyothsna and Kondapalli, Lavanya and Hegde, Aswathi R and Avadhani, Kiran and Shetty, Pallavi K and Amirthalingam, Muthukumar and Kalthur, Guruprasad and Mutalik, Srinivas (2016) Nano-transfersomal Formulations for Transdermal Delivery of Asenapine Maleate: In Vitro and in Vivo Performance Evaluations. Journal of Liposome Research, 26 (3). pp. 221-232. ISSN 0898-2104

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Context: Asenapine maleate (ASPM) is an antipsychotic drug for the treatment of schizophrenia and bipolar disorder. Extensive metabolism makes the oral route inconvenient for ASPM.Objective: The objective of this study is to increase ASPM bioavailability via transdermal route by improving the skin permeation using combined strategy of chemical and nano-carrier (transfersomal) based approaches.Materials and methods: Transfersomes were prepared by the thin film hydration method using soy-phosphatidylcholine (SPC) and sodium deoxycholate (SDC). Transfersomes were characterized for particle size, polydispersity index (PDI), zeta potential (ZP), entrapment efficiency,surface morphology, and in vitro skin permeation studies. Various chemical enhancers were screened for skin permeation enhancement of ASPM. Optimized transfersomes were incorporated into a gel base containing suitable chemical enhancer for efficient transdermal delivery. In vivo pharmacokinetic study was performed in rats to assess bioavailability by transdermal route against oral administration.Results and discussion: Optimized transfersomes with drug:SPC:SDC weight ratio of 5:75:10 were spherical with an average size of 126.0 nm, PDI of 0.232, ZP of�43.7 mV, and entrapment efficiency of 54.96%. Ethanol (20% v/v) showed greater skin permeation enhancement. The cumulative amount of ASPM permeated after 24 h (Q24) by individual effect of ethanol and transfersome, and in combination was found to be 160.0, 132.9, and 309.3 mg, respectively,indicating beneficial synergistic effect of combined approach. In vivo pharmacokinetic study revealed significant (p50.05) increase in bioavailability upon transdermal application compared with oral route.Conclusion: Dual strategy of permeation enhancement was successful in increasing the transdermal permeation and bioavailability of ASPM.

Item Type: Article
Uncontrolled Keywords: Asenapine maleate; Bioavailability; Ethanol; Transdermal; Transfersomes
Subjects: Medicine > KMC Manipal > Clinical Embryology
Pharmacy > MCOPS Manipal > Pharmaceutics
Depositing User: KMC Library
Date Deposited: 01 Jul 2016 09:10
Last Modified: 17 Aug 2021 09:28

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