Formulation and Optimization of Metronidazole and <i>Lactobacillus</i> spp. Layered Suppositories via a Three-Variable, Five-Level Central Composite Design for the Management of Bacterial Vaginosis

• Main Authors: Margaret O. Ilomuanya (Author), Busayo B. Salako (Author), Modupe O. Ologunagba (Author), Omonike O. Shonekan (Author), Kruga Owodeha-Ashaka (Author), Eseosa S. Osahon (Author), Andrew N. Amenaghawon (Author)
• Format: Book
• Published: MDPI AG, 2022-10-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 10.3390/pharmaceutics14112337; 1999-4923
• Keywords: central composite design; bacterial vaginosis; layered suppositories; <i>Lactobacillus</i> spp.; Pharmacy and materia medica; RS1-441
• Source: Pharmaceutics, Vol 14, Iss 11, p 2337 (2022)

Bacterial vaginosis, a polymicrobial clinical syndrome characterized by a shift in healthy vaginal microbiota due to bacterial colonization, is characterized by high recurrence rates after conventional treatment with an antimicrobial agent. This has necessitated the need to develop a formulation that has the potential to ensure <i>Lactobacilli</i> viability and bacterial clearance. This study seeks to develop and optimize a layered suppository using a five-level central composite design to ensure optimized metronidazole release and lactic acid viability. Layered suppositories were formulated using the fusion method using polyethylene glycol blend 1500/4000 and Ovucire^® as suppository bases. <i>Lactobacillus fermentum</i> was incorporated in the molten mass before molding the solid body suppositories into the cavity of hollow-type suppositories and sealing the molten excipients. Artificial neural network model predictions for product optimization showed high predictive capacity, closely resembling experimental observations. The highest disintegration time recorded was 12.76 ± 0.37 min, with the optimized formulations showing lower times of 5.93 ± 0.98 min and an average weight of 1.17 ± 0.07 g. Histopathological observations determined high compatibility of suppositories with vaginal cells with no distortion or wearing of the vagina epithelium. This optimized formulation provides a safe and promising alternative to conventional suppositories in the treatment and prevention of the recurrence of bacterial vaginosis.