Enhanced gastric retention and drug release via development of novel floating microspheres based on Eudragit E100 and polycaprolactone: synthesis and in vitro evaluation

• Main Authors: Umar Farooq, Samiullah Khan, Shahid Nawaz, Nazar Mohammad Ranjha, Malik Salman Haider, Muhammad Muzamil Khan, Eshwa Dar, Ahmad Nawaz
• Format: Article
• Language: English
• Published: Taylor & Francis Group 2017-01-01
• Series: Designed Monomers and Polymers
• Subjects: Floating microspheres; metronidazole benzoate; oil in water (o/w) method; gastric retention and drug release; Eudragit E 100
• Online Access: http://dx.doi.org/10.1080/15685551.2017.1326702

Eudragit E 100 and polycaprolactone (PCL) floating microspheres for enhanced gastric retention and drug release were successfully prepared by oil in water solvent evaporation method. Metronidazole benzoate, an anti-protozoal drug, was used as a model drug. Polyvinyl alcohol was used as an emulsifier. The prepared microspheres were observed for % recovery, % degree of hydration, % water uptake, % drug loading, % buoyancy and % drug release. The physico-chemical properties of the microspheres were studied by calculating encapsulation efficiency of microspheres and drug release kinetics. Drug release characteristics of microspheres were studied in simulated gastric fluid and simulated intestinal fluid i.e., at pH 1.2 and 7.4 respectively. Fourier transform infrared spectroscopy was used to reveal the chemical interaction between drug and polymers. Scanning electron microscopy was conducted to study the morphology of the synthesized microspheres.