Improvement of an encapsulation process for the preparation of pro- and prebiotics-loaded bioadhesive microparticles by using experimental design

• Published in: European journal of pharmaceutical sciences 2011-09, Vol.44 (1), p.83-92
• Main Authors: Pliszczak, D., Bourgeois, S., Bordes, C., Valour, J.P., Mazoyer, M.A., Orecchioni, A.M., Nakache, E., Lantéri, P.
• Format: Article
• Language: English
• Subjects: Adhesiveness; Analytical chemistry; Bioadhesive microparticles; Biological and medical sciences; Chemical Sciences; Drug Carriers - chemistry; Drug Compounding - methods; Drug Compounding - standards; Drug Compounding - trends; Drug Design; General pharmacology; Hyaluronic acid; Hyaluronic Acid - chemistry; Medical sciences; Microscopy, Confocal; Microscopy, Electron, Transmission; Microspheres; Models, Biological; Particle Size; Pectin; Pectins - chemistry; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Prebiotics; Probiotics; Probiotics - administration & dosage; Probiotics - chemistry; Rheology; Solubility; Surface Properties; Vaginal Creams, Foams, and Jellies - administration & dosage; Vaginal Creams, Foams, and Jellies - chemistry; Vaginal delivery system
• ISSN: 0928-0987; 1879-0720
• DOI: 10.1016/j.ejps.2011.06.011

The purpose of this study was to design a new vaginal bioadhesive delivery system based on pectinate–hyaluronic acid microparticles for probiotics and prebiotics encapsulation. Probiotic strains and prebiotic were selected for their abilities to restore vaginal ecosystem. Microparticles were produced by emulsification/gelation method using calcium as cross-linking agent. In the first step, preliminary experiments were conducted to study the influence of the main formulation and process parameters on the size distribution of unloaded microparticles. Rheological measurements were also performed to investigate the bioadhesive properties of the gels used to obtain the final microparticles. Afterwards an experimental design was performed to determine the operating conditions suitable to obtain bioadhesive microparticles containing probiotics and prebiotics. Experimental design allowed us to define two important parameters during the microencapsulation process: the stirring rate during the emulsification step and the pectin concentration. The final microparticles had a mean diameter of 137 μm and allowed a complete release of probiotic strains after 16 h in a simulated vaginal fluid at +37 °C.