Development of pre-activated α-cyclodextrin as a mucoadhesive excipient for intra-vesical drug delivery

Publication date: 20 December 2017 Source:International Journal of Pharmaceutics, Volume 534, Issues 1–2 Author(s): Muhammad Ijaz, Maximilian Prantl, Noemi Lupo, Flavia Laffleur, Mulazim Hussain Asim, Barbara Matuszczak, Andreas Bernkop-Schnürch The study was designed to synthesize and characterize pre-activated α-cyclodextrin (α-CD) derivatives as mucus adhering excipients for intra-vesical drug delivery. Sodium periodate (NaIO4) was used to oxidize α-CD and subsequently cysteamine was covalently attached to carbonyl groups of oxidized α-CD via reductive amination to produce thiolated α-CD. l-cysteine-2-mercaptonicotinic acid conjugate (Cys-MNA) was covalently attached to carbonyl groups of oxidized α-CD to produce pre-activated α-CD having enhance stability against oxidation at higher pH. Thiolated and pre-activated α-CD derivatives were quantitatively assayed for the attached thiol groups and MNA groups, respectively. Cell viability and tolerability was evaluated via resazurin assay and via red blood cells (RBC) lysis assay, respectively. Mucoadhesive properties were evaluated on porcine bladder mucosa. Trimethoprim (TMP) was encapsulated into thiolated and pre-activated α-CD derivatives and the dissolution behavior was evaluated in vitro. Thiol groups attached to thiolated α-CD derivatives α-CD-SH780 and α-CD-SH1426 were 780±68μmol/g and 1426±66μmol/g, respectively. For the entirely pre-activated α-CD derivatives, α-CD-MNA3609 and α-CD-MNA42...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research