Colonic delivery of indometacin loaded PGA-co-PDL microparticles coated with Eudragit L100-55 from fast disintegrating tablets

Abstract

The aim of this work was to investigate the efficient targeting and delivery of indometacin (IND), as a model anti-inflammatory drug to the colon for treatment of inflammatory bowel disease. We prepared fast disintegrating tablets (FDT) containing IND encapsulated within poly(glycerol-adipate-co-ɷ-pentadecalactone), PGA-co-PDL, microparticles and coated with Eudragit L100-55 at different ratios (1:1.5, 1:1, 1:0.5). Microparticles encapsulated with IND were prepared using an o/w single emulsion solvent evaporation technique and coated with Eudragit L-100-55 via spray drying. The produced coated microparticles (PGA-co-PDL-IND/Eudragit) were formulated into optimised FTD using a single station press. The loading, in vitro release, permeability and transport of IND from PGA-co-PDL-IND/Eudragit microparticles was studied in Caco-2 cell lines. IND was efficiently encapsulated (570.15±4.2μg/mg) within the PGA-co-PDL microparticles. In vitro release of PGA-co-PDL-IND/Eudragit microparticles (1:1.5) showed significantly (p<0.05, ANOVA/Tukey) lower release of IND 13.70±1.6 and 56.46±3.8% compared with 1:1 (89.61±2.5, 80.13±2.6%) and 1:0.5 (39.46±0.9 & 43.38±3.12) after 3 and 43h at pH 5.5 and 6.8, respectively. The permeability and transport studies indicated IND released from PGA-co-PDL-IND/Eudragit microparticles had a lower permeability coefficient of 13.95±0.68×10cm/s compared to free IND 23.06±3.56×10cm/s. These results indicate the possibility of targeting anti-inflammatory drugs to the colon using FDTs containing microparticles coated with Eudragit.

Formulation of Ethyl Cellulose Microparticles Incorporated Pheophytin A Isolated from Suaeda vermiculata for Antioxidant and Cytotoxic Activities

“…The encapsulation of pheo-a with EC was used to enhance the solubility and spreadability of the final product, and hence to decrease its side effects on the stomach due to ethyl cellulose requires a pH above 7 for release. Furthermore, this ethyl cellulose polymer is cheap, safe, and available [21,22].…”

Novel sublingual tablets of Atorvastatin calcium/Trimetazidine hydrochloride combination; HPTLC quantification, in vitro formulation and characterization

“…Different diluents were used including soluplus®, anhydrous lactose and Avicel pH101. Ac-Di-Sol (Croscarmellose sodium), Crospovidone and Explotab (Sodium starch glycolate) were used as superdisintegrants to promote fast disintegration of tablets and they were incorporated in different concentrations ranged from 4.0 to 9.6 %w/w of the final tablet weight of 250 mg (Sheshala et al, 2011, Tawfeek et al, 2015, Tawfeek et al, 2017, Tawfeek et al, 2018). Magnesium stearate was used as a lubricant in a concentration of 1% (w/w).…”

Design of Sustained Action Dosage Forms; Mini-Review

“…For this situation, the impact of excipients and pressure ought to be considered. The position of a typified item into tablet or case must be done precisely to limit fracture or combination of the particles and to keep up the respectability of the coat [22][23][24][25].…”

“…The ability of drugs to diffuse through membranes is influenced by molecular size. Drugs with high molecular weights usually possess a very low diffusion coefficient and hence a low permeability through many polymeric films [22,48].…”

“…A properly designed sustained-release drug delivery system can be an important advance toward solving these two problems. The science and technology is a useful development of sustained-release pharmaceuticals and still continue to be the focusing of a great deal of care in both industrial and educational laboratories [1]. The term sustained-release drug product has been utilized to explain several types of oral prolonged release rate dosage forms, involving sustained-release, controlled-action, long-action, and retarded-release [2,3].…”