Eudragit S-100 coated sodium alginate microspheres of naproxen sodium: Formulation, optimization and in vitro evaluation / Alginatne mikrosfere naproksen natrija obložene Eudragitom S-100: Priprava, optimizacija i in vitro vrednovanje

Abstract

The aim of the study was to prepare site specific drug delivery of naproxen sodium using sodium alginate and Eudragit S-100 as a mucoadhesive and pH-sensitive polymer, respectively. Core microspheres of alginate were prepared by a modified emulsification method followed by cross-linking with CaCl 2 , which was further coated with the pH dependent polymer Eudragit S-100 (2.5 or 5 %) to prevent drug release in the upper gastrointestinal environment. Microspheres were characterized by FT-IR spectroscopy, X-ray diffraction, differential scanning calorimetry and evaluated by scanning electron microscopy, particle size analysis, drug loading efficiency, in vitro mucoadhesive time study and in vitro drug release study in different simulated gastric fluids. Stability studies of the optimized formulation were carried out for 6 months. SEM images revealed that the surface morphology was rough and smooth for core and coated microspheres, respectively. Core microspheres showed better mucoadhesion compared to coated microspheres when applied to the mucosal surface of freshly excised goat colon. The optimized batch of core microspheres and coated microspheres exhibited 98.42 ± 0.96 and 95.58 ± 0.74 % drug release, respectively. Drug release from all sodium alginate microsphere formulations followed Higuchi kinetics. Moreover, drug release from Eudragit S-100 coated microspheres followed the Korsmeyer-Peppas equation with a Fickian kinetics mechanism. Stability study suggested that the degradation rate constant of microspheres was minimal, indicating 2 years shelf life of the formulation.

Formulation and evaluation of pH-sensitive rutin nanospheres against colon carcinoma using HCT-116 cell line

“…Among several types of Eudragit polymers, Eudragit S100 is pH sensitive anionic copolymers based on methacrylic acid and methyl methacrylate in the ratio 1:2. It does not degrade below pH 7 [10] . In other words, this polymer does not dissolve in stomach and intestinal pH, yet it dissolves in the pH of the colon (pH > 7) due to the ionization of its carboxyl functional groups and consequently the drug can be released in the colon [11] .…”

Mucin-Grafted Polyethylene Glycol Microparticles Enable Oral Insulin Delivery for Improving Diabetic Treatment

“…The coating of the MPs was carried out following the procedure reported in the literature [14,[18][19][20] with slight modifications. In brief, a 2.0% solution of Eudragit ® RS-100 in dichloromethane was freshly prepared, and MPs (5.0 g) were gently dispersed and shaken for about 3 min in the corresponding coating solution.…”

Formulation and Evaluation of Karaya Gum Microspheres of Cromolyn Sodium: Treatment of Ulcerative Colitis

“…About 50mg of microspheres were digested in 10ml Phosphate buffer saline (PBS, pH-7.4) and extracted completely during 24 h. The solution was centrifuged at 6000rpm.The supernatant filtered through 0.22µm membrane filter (Millipore) and the amount of mesalamine was measured spectrometrically (Shimadzu, Double-Beam Spectrophotometer, 150-03, Japan) at 235nm.Each determination was made in triplicate 11,12 .…”