Investigations in Transdermal Delivery of Lacidipine

Author: Lalan M.S., Patel F.T., Patel R.D., Chauhan P., Gamit R. and Patel B.K.

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Abstract

Lacidipine is a calcium channel blocker which exhibits limited oral bioavailability. This study sought to formulate and assess lacidipine-loaded bigels for hypertension management by transdermal administration, resulting in lower doses, controlled drug delivery and improved patient compliance. Box-Behnken design was employed to optimize bigels by studying the effect of independent variables i.e. organogelator concentration, hydrogelator concentration, mixing proportion of Hydrogel:Organogel on dependent variables viscosity, time for 80% drug release. Bigels were characterized for physical appearance, pH, spreadability, extrudability, gel sol transition temperature, drug content, in vitro and ex vivo skin permeation, stability. Compatibility studies showed drug’s compatibility with excipients. Carbopol 940, Span 60 were used as hydrogelator, organogelator respectively and mixing proportion of hydrogel:organogel was 1:1. Statistical model indicated that higher amount of hydrogelator and organogelator increased viscosity is increased. The higher proportion of hydrogel in bigel reduced the time for 80% drug release decreased. Optimized formula was found to show 86% drug release in 8 hours and stable in the accelerated stability study. Thus the novel formulation can be a commercially viable dosage form for efficient management of hypertension.

Keywords

lacidipine, bigel, hydrogel, organogel, transdermal, hypertension

Conclusion

Bigel of the antihypertensive drug lacidipine was formulated by dispersion of hydrogel and drug loaded organogel. The successful formulation was indicated by absence of phase separation and desirable consistency. The microstructure revealed uniform globular dispersion. Box Behnken design aided in optimization of the formulation’s critical independent variables on the basis of desirable responses. Drug release studies through the dialysis membrane and ex vivo skin permeation suggested sustained drug release for a duration of 8 hours. The prepared formulation displayed desirable physiochemical characteristics in terms of pH, gel-sol transition, spreadability and stability in accelerated studies. The Bigel is a patient friendly dosage form for transdermal drug delivery that can be scaled up easily during large scale manufacturing.

References

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How to cite this article

Lalan M.S., Patel F.T., Patel R.D., Chauhan P., Gamit R. and Patel B.K. (2023). Investigations in Transdermal Delivery of Lacidipine. Biological Forum – An International Journal, 15(5a): 481-491.