Next generation of buccadhesive excipient: Preactivated carboxymethyl cellulose

International Journal of Pharmaceutics
Flavia LaffleurIjaz Muhammad

Abstract

Assessment of preactivated carboxymethyl cellulose as potential excipient for buccal drug delivery. Firstly, carboxymethyl cellulose (CMC) and cysteine (SH) were covalently coupled via amide bond formation to obtain thiolated carboxymethyl cellulose (CMC-SH). Further, preactivated carboxymethyl cellulose (CMC-S-S-MNA) was obtained by preactivation with 2-mercaptonicotinic acid (MNA). Sulforhodamine 101 (SRH101) was used as a model drug for permeation study through buccal mucosa. CMC-S-S-MNA was evaluated with respect to mucoadhesive and permeation enhancing effect and cytotoxicity. Thiolated carboxymethyl cellulose exhibited a total amount of 112.46 ± 0.46 thiol groups. CMC-S-S-MNA exhibited around 50% of preactivated thiol groups. The preactivated polymer showed no toxic effect. Furthermore, compared to unmodified CMC, CMC-S-S-MNA revealed 3.0-fold improved mucoadhesive properties according to the rotating cylinder method and 8.8-fold enhancement in mucoadhesiveness by tensile assay, respectively. Preactivated carboxymethyl cellulose fulfills the requirements as potential excipient of being mucoadhesive and permeation enhancing for the buccal drug delivery.

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Citations

Jul 5, 2017·Drug Development and Industrial Pharmacy·Flavia LaffleurClaudia Menzel
Aug 23, 2016·Expert Opinion on Drug Delivery·Kifayat Ullah ShahStéphane Gibaud
Apr 9, 2020·Pharmaceutical Development and Technology·Amresh KumarGoutam Rath
May 1, 2019·Molecular Pharmaceutics·Randi Angela BausAndreas Bernkop-Schnürch
Aug 27, 2021·International Journal of Pharmaceutics·Amina Ahmady, Nor Hayati Abu Samah

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