Formulation and evaluation of Bacillus coagulans-loaded hypromellose mucoadhesive microspheres

Abstract

Development of a novel delivery system has been attempted to deliver viable probiotic cells into the gut for a prolonged period of time while maintaining high numbers of viable cells within the formulation throughout the shelf-life of the product and during the gastrointestinal transit. Core mucoadhesive microspheres of Bacillus coagulans were developed employing several grades of hypromellose, a mucoadhesive polymer, following coacervation and phase separation technique and were subsequently enteric-coated with hypromellose phthalate. Microspheres were evaluated for percent yield; entrapment efficiency; in vitro swelling; surface morphology; particle size, size distribution, and zeta potential; flow property, mucoadhesion property by the ex vivo mucoadhesive strength test and the in vitro wash off test; in vitro release profile and release kinetic; in vivo probiotic activity; and stability. The values for the kinetic constant and regression coefficient of model-dependent approaches and the difference factor ( f 1 ), the similarity factor ( f 2 ), and the Rescigno index ( ξ 1 and ξ 2 ) of model independent approaches were determined for comparing in vitro dissolution profiles. Freeze dried B. coagulans cells were successfully formulated as enteric-coated mucoadhesive microspheres with satisfactory physical structure and yield. The viability of B. coagulans was maintained in the simulated gastric conditions and during processing; in simulated intestinal conditions exhibiting mucoadhesion, and controlling and extending the viable cell release following zero-order; and was satisfactorily stable at room temperature. Test results depict statistically significant effects of the hypromellose grade and their concentration on the performance and release profile of formulations.

Aqueous Film Coating the Current Trend

“…• Cellulosics: Examples: Hydroxypropyl Methylcellulose (HPMC) [21][22][23][24][25][26][27] • Glycols: Example, high molecular weight poly ethylene glycols.…”

Preparation of Mangosteen Peel Extract Microcapsules by Fluidized Bed Spray-Drying for Tableting: Improving the Solubility and Antioxidant Stability

“…One of them is HPMC, which is known to be biodegradable, biocompatible, renewable, and low in toxicity [ 21 , 22 ]. HPMC has been used as a mixture with active ingredients to increase solubility and extend drug contact time due to its hydrophilic and mucoadhesive properties [ 23 , 24 , 25 ]. This cellulose derivate has also demonstrated substantial potential to alleviate GI irritation caused by APIs known to induce diarrhea, ulcers, nausea, or vomiting [ 23 ].…”