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Formulation and evaluation of Bacillus coagulans-loaded hypromellose mucoadhesive microspheres.

Alli SM - Int J Nanomedicine (2011)

Bottom Line: 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.Freeze dried B. coagulans cells were successfully formulated as enteric-coated mucoadhesive microspheres with satisfactory physical structure and yield.Test results depict statistically significant effects of the hypromellose grade and their concentration on the performance and release profile of formulations.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Technology, Jadavpur University, Kolkata, West Bengal, India. smatharalli@gmail.com

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.

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Histogram of mean particle size distribution of all formulation batches.
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f2-ijn-6-619: Histogram of mean particle size distribution of all formulation batches.

Mentions: The mean particle size value of all formulation batches lies between 26.61 μm and 49.01 μm (Table 3). Variation in the mean particle size was observed with differences in the grade of hypromellose. The highest mean particle size value was observed with formulations containing Methocel K15M Premium. The effect of the grade of hypromellose on the mean particle size value follows the order of Methocel K15M Premium > Methocel E15 Premium LV > Methocel E5 Premium LV (Figure 2 and Table 3). Variation in B. coagulans-to-hypromellose ratio does not influence the mean particle size value of formulation batches. The zeta potential value (Table 3) of core microspheres was negative as expected due to the methoxy group of hypromellose. Core microspheres prepared with the Methocel E15 Premium LV and the Methocel E5 Premium LV possessed nearly the same zeta potential value as both have the same ratio of methoxy and hydroxypropoxy groups, and are both higher than that prepared with Methocel K15M Premium. This may be due to an increase in the methoxy content of hypromellose polymer. A nearly constant negative zeta potential value (−7.66 ± 0.87) was observed with coated microspheres of all formulation batches, which is lower than that of uncoated microspheres, confirms the presence of hypromellose phthalate on the surface of microspheres. The zeta potential report of uncoated microspheres from formulation-F1 is presented in Figure 3. The flow properties of formulation batches lie between the passable and very poor range.


Formulation and evaluation of Bacillus coagulans-loaded hypromellose mucoadhesive microspheres.

Alli SM - Int J Nanomedicine (2011)

Histogram of mean particle size distribution of all formulation batches.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3107721&req=5

f2-ijn-6-619: Histogram of mean particle size distribution of all formulation batches.
Mentions: The mean particle size value of all formulation batches lies between 26.61 μm and 49.01 μm (Table 3). Variation in the mean particle size was observed with differences in the grade of hypromellose. The highest mean particle size value was observed with formulations containing Methocel K15M Premium. The effect of the grade of hypromellose on the mean particle size value follows the order of Methocel K15M Premium > Methocel E15 Premium LV > Methocel E5 Premium LV (Figure 2 and Table 3). Variation in B. coagulans-to-hypromellose ratio does not influence the mean particle size value of formulation batches. The zeta potential value (Table 3) of core microspheres was negative as expected due to the methoxy group of hypromellose. Core microspheres prepared with the Methocel E15 Premium LV and the Methocel E5 Premium LV possessed nearly the same zeta potential value as both have the same ratio of methoxy and hydroxypropoxy groups, and are both higher than that prepared with Methocel K15M Premium. This may be due to an increase in the methoxy content of hypromellose polymer. A nearly constant negative zeta potential value (−7.66 ± 0.87) was observed with coated microspheres of all formulation batches, which is lower than that of uncoated microspheres, confirms the presence of hypromellose phthalate on the surface of microspheres. The zeta potential report of uncoated microspheres from formulation-F1 is presented in Figure 3. The flow properties of formulation batches lie between the passable and very poor range.

Bottom Line: 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.Freeze dried B. coagulans cells were successfully formulated as enteric-coated mucoadhesive microspheres with satisfactory physical structure and yield.Test results depict statistically significant effects of the hypromellose grade and their concentration on the performance and release profile of formulations.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Technology, Jadavpur University, Kolkata, West Bengal, India. smatharalli@gmail.com

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.

Show MeSH
Related in: MedlinePlus