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Formulation Development of a Transdermal Self-Microemulsifying Drug Delivery System of Bosutinib

Kalpesh Patel
,
Nirav Patel

Published in December 2022 Issue 6 (Vol. 12, Issue 6, 2022)

Formulation Development of a Transdermal Self-Microemulsifying Drug Delivery System of Bosutinib - Issue cover

Keywords

Self-microemulsifyingBosutiniboleic acidLabrasoltopical gel.

Abstract

Tyrosine kinase inhibitors treat chronic myeloid leukemia but have many negative effects. These BCS Class II or IV medicines have low oral bioavailability due to poor solubility, permeability, or both. As P-glycoprotein substrates and hepatic presystemic metabolism inactivators, these medicines have another drawback. The present work sought to overcome the limitations of tyrosine kinase inhibitor bosutinib. A transdermal system with the medication put into a SMEDDS was created. The investigation began with solubility and emulsification studies to choose the proper oil (oleic acid), surfactant (Tween 20), and cosurfactant (Transcutol® P). The microemulsion zone was identified using ternary phase diagrams. The resultant SMEDDS exhibited a narrow polydispersity index and a droplet size of 45.66 ± 2.4 nm. The formulation's zeta potential prevented aggregation during storage, as shown by thermodynamic stability investigations under physical and thermal stress. Dispersibility and dilution experiments showed that the formulation formed the microemulsion instantly in vivo. BOS-loaded liquid SMEDDS was gelled with 2% HPMC K15M to make G-SNEDDS. The liquid SMEDDS and G-SMEDDS had similar properties. In vitro dissolution showed that near to 100% drug release could be achieved in 30 mins, compared to 5–6% for the simple medication. The formulation's in vitro permeability testing employing an artificial membrane demonstrated a 2.18-fold increase in drug penetration compared to the basic drug suspension.

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Authors (2)

Kalpesh Patel

B K Mody Government Pharmacy C...

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Nirav Patel

Department of Pharmaceutics, S...

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Article Information

Published in:

December 2022 Issue 6 (Vol. 12, Issue 6, 2022)

AJPTR6120012

AJPTR-02-002462

191-210

2022-12-25

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How to Cite

Patel & Patel (2022). Formulation Development of a Transdermal Self-Microemulsifying Drug Delivery System of Bosutinib. American Journal of PharmTech Research, 12(6), 191-210. https://ajptr.com/articles/AJPTR6120012

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