Ultrasonic atomization and polyelectrolyte complexation to produce gastroresistant shell–core microparticles

Abstract

In this study ultrasound-assisted atomization technique was combined with two-stages polyelectrolyte complexation to produce enteric shell-core microparticles encapsulating a non-steroidal, anti-inflammatory gastrolesive active ingredient indomethacin. In particular, a solution of the anionic biopolymer alginate, containing indomethacin, was sprayed in fine droplets which were complexed with a cationic (meth)acrylate copolymer, Eudragit V R E 100, which, in turn, was complexed by the anionic copolymer Eudragit V R L30D-55. The first complexation stage was applied to achieve a high drug encapsulation efficiency; the second one to assure good gastroresistance feature. The novel protocol has been found more effective in terms of loading, encapsulation efficiency, and enteric properties during in vitro release tests, than conventional procedures which involved alginate cross-linking by charged ions. Furthermore ultrasonic atomization-polyelectrolytes complexation preparation approach was performed using mild conditions, aqueous solutions, in the absence of organic solvents and chemical cross-linkers.

An Engineering Point of View on the Use of the Hydrogels for Pharmaceutical and Biomedical Applications

“…Optimization of manufacturing parameters allowed to obtain high encapsulation efficiency (nearly 92%); good gastro-resistance properties (less than 10% release at pH of 1.0, nearly 100% release at pH of 6.8 and 240 min of dissolution); limited ergocalciferol degradation after 5 months of storage, reduction of D2 degradation during microwave-assisted stabilization process compared to the convective one. Another modification of the process, that is, the coupling of the ultrasonic atomization technique with the polyelectrolyte complexation, allowed to produce enteric shell-core HMPs encapsulating an anionic gastrolesive drug, indomethacin (Figure 3) [59]. Again, both the solutions, core and shell feed (with unchanged features), were sent to the coaxial ultrasonic atomizer where they were nebulized and placed in contact with the cross-linking solution.…”

“…Structure of the HMPs produced by ultrasonic-atomization-two stage polyelectrolyte complexation. From Dalmoro et al[59], Copyright © (2016).…”

Development of new potential drugs with psychotropic activity among phosphorylacetohydrazides and other phosphorylated carboxylic acids derivatives - priority area of Kazan school of psychopharmacologists

“…Эти сополимеры широко применяют в фармацевтической промышленности, а ИПЭК на основе различных марок эудрагитов способны, в зависимости от состава комплексов, обеспечивать направленную доставку ЛВ в определённые отделы желудочно-кишечного тракта или пролонгировать его действие, обеспечивая постепенное высвобождение ЛВ [44]. Описаны также композиции с использованием микро-и наночастиц ИПЭК, обладающие улучшенными фармако-технологическими и биофармацевтическими характеристиками [43].…”

Modern Methods for Studying Polymer Complexes in Aqueous and Organic Solutions

“…. ИПЭК также находят применение в других областях фармацевтики, например, как вспомогательные вещества при создании твердых лекарственных форм [8,9] и капсул [10,11]. [16][17][18], а также стереотактических полилактонов [19].…”