Novel nano spanlastic carrier system for buccal delivery of lacidipine

Cleona Elizabeth Mary DCruz, Prashant Jivaji Bhide, Lalit Kumar, Rupesh Kalidas Shirodkar

Research output: Contribution to journalArticlepeer-review

Abstract

Lacidipine, a calcium channel antagonist with its highly lipophilic and poorly water-soluble nature (BCS Class II Drug), when administered via the conventional oral route undergoes extensive hepatic metabolism by Cytochrome P450 3A4 (CYP3A4), results in low bioavailability (∼10%) and summons a challenge to anti-hypertensive therapy. This present research study aimed to override this drug delivery obstacle by formulating lacidipine loaded spanlastic orally dissolving films. A 23 factorial design model was employed in the spanlastics development process to examine the influence of the formulation variables over the response variables. Spanlastics composed of Span 60 and Tween 80 were prepared by modified ethanol injection method and developed into an orally dissolving film using hypromellose E5, polyvinyl alcohol and polyethylene glycol 400 by the solvent casting technique. The characterization results of the formulation showed that the spanlastics possessed nano-sized vesicles and good entrapment efficiency (86.84%). Optical microscopy and high resolution transmission electron microscopy displayed lamellar, circularly shaped, and uniformly dispersed nanovesicles. Evaluation studies revealed that the oral film possessed considerable flexibility, good mechanical strength, disintegrated within 35 s and revealed a drug release of 92.96% within 5 min. The scanning electron microscopy displayed a smooth, uniform surface of the film with pores. Stability studies of the films at 25 ± 2 °C and 60 ± 5% RH for 3 months showed no alteration in physical appearance or mechanical properties. The developed spanlastic vesicles, owing to their nano size have an enhanced barrier permeation profile while the oral films offer better bioavailability of the drug by absorption through the oro-mucosal tissue. In combination with the increased permeability, the circumvention of hepatic metabolism, improved dissolution and fast onset of action, this new drug delivery approach makes lacidipine efficiently available for antihypertensive therapy.

Original languageEnglish
Article number103061
JournalJournal of Drug Delivery Science and Technology
Volume68
DOIs
Publication statusPublished - 02-2022

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

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