Nano-transfersomal formulations for transdermal delivery of asenapine maleate: in vitro and in vivo performance evaluations

A. B. Shreya, Renuka S. Managuli, Jyothsna Menon, Lavanya Kondapalli, Aswathi R. Hegde, Kiran Avadhani, Pallavi K. Shetty, Muthukumar Amirthalingam, Guruprasad Kalthur, Srinivas Mutalik

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

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 μg, respectively, indicating beneficial synergistic effect of combined approach. In vivo pharmacokinetic study revealed significant (p < 0.05) 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.

Original languageEnglish
Pages (from-to)221-232
Number of pages12
JournalJournal of Liposome Research
Volume26
Issue number3
DOIs
Publication statusPublished - 02-07-2016

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Biological Availability
Skin
Deoxycholic Acid
Phosphatidylcholines
Ethanol
Pharmacokinetics
Bipolar Disorder
Particle Size
Antipsychotic Agents
Oral Administration
In Vitro Techniques
Asenapine
Schizophrenia
Gels
Weights and Measures
Pharmaceutical Preparations
Therapeutics

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Cite this

Shreya, A. B. ; Managuli, Renuka S. ; Menon, Jyothsna ; Kondapalli, Lavanya ; Hegde, Aswathi R. ; Avadhani, Kiran ; Shetty, Pallavi K. ; Amirthalingam, Muthukumar ; Kalthur, Guruprasad ; Mutalik, Srinivas. / Nano-transfersomal formulations for transdermal delivery of asenapine maleate : in vitro and in vivo performance evaluations. In: Journal of Liposome Research. 2016 ; Vol. 26, No. 3. pp. 221-232.
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Nano-transfersomal formulations for transdermal delivery of asenapine maleate : in vitro and in vivo performance evaluations. / Shreya, A. B.; Managuli, Renuka S.; Menon, Jyothsna; Kondapalli, Lavanya; Hegde, Aswathi R.; Avadhani, Kiran; Shetty, Pallavi K.; Amirthalingam, Muthukumar; Kalthur, Guruprasad; Mutalik, Srinivas.

In: Journal of Liposome Research, Vol. 26, No. 3, 02.07.2016, p. 221-232.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Nano-transfersomal formulations for transdermal delivery of asenapine maleate

T2 - in vitro and in vivo performance evaluations

AU - Shreya, A. B.

AU - Managuli, Renuka S.

AU - Menon, Jyothsna

AU - Kondapalli, Lavanya

AU - Hegde, Aswathi R.

AU - Avadhani, Kiran

AU - Shetty, Pallavi K.

AU - Amirthalingam, Muthukumar

AU - Kalthur, Guruprasad

AU - Mutalik, Srinivas

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N2 - 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 μg, respectively, indicating beneficial synergistic effect of combined approach. In vivo pharmacokinetic study revealed significant (p < 0.05) 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.

AB - 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 μg, respectively, indicating beneficial synergistic effect of combined approach. In vivo pharmacokinetic study revealed significant (p < 0.05) 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.

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