Buccoadhesive gel of carvedilol nanoparticles for enhanced dissolution and bioavailability

Abstract

The aim of the work was to improve carvedilol bioavailability through preparation of nanoparticles to be formulated as a buccoadhesive gel. Physicochemical compatibility of drug was studied. The ionic gelation technique was used for nanoparticles preparation based on 31 × 41 factorial design using Eudragit® RS100 as a complexing agent. Particle size, entrapment efficiency and dissolution parameters were measured and the formula of choice was prepared into two nanoparticles gel formulae to study the effect on bioavailability. The nanoparticles appearance was spherical and uniform. The tested formula variables significantly affected all the parameters (P value < 0.05). The particle size of the prepared formulae ranged from 150 to 225 nm and entrapment efficiency varied from 73.3 to 98.8%. The prepared gel formulae showed an acceptable bioadhesion force which is required for buccal application. Regarding pharmacokinetics parameters, both gel formulae shorten the Tmax from 1.5 h to 1 h compared to the market product. Carvedilol nanoparticles were successfully formulated using the ionic gelation technique with low particle size and high entrapment efficiency. The prepared nanoparticles gel contains both sodium carboxymethyl cellulose and hydroxypropyl methylcellulose K4M polymers showed two fold increase in relative bioavailability.