Formulation and in-vitro evaluation of pantoprazole loaded pH-sensitive polymeric nanoparticles

• Main Authors: Ahmed Mohammed Nasef, Ahmed Rifaat Gardouh, Mamdouh Moustafa Ghorab
• Format: Article
• Language: English
• Published: SpringerOpen 2017-12-01
• Series: Future Journal of Pharmaceutical Sciences
• Subjects: Acid labile; Nanoprecipitation; Pantoprazole; pH-dependant polymers
• Online Access: http://www.sciencedirect.com/science/article/pii/S231472451630139X

The pH-sensitive polymeric nanoparticles are very efficient delivery systems for acid labile drugs. The main aim of the study was to formulate pantoprazole loaded pH-sensitive polymeric nanoparticles using pH-sensitive polymers to prevent degradation of acid labile drug and evaluate the effect of formation conditions on both nanoparticles characteristics and drug release patterns. Pantoprazole loaded nanoparticles were prepared using nanopercipitation method using pH-sensitive polymers Eudragit S100 or HPMC phthalate HP55. Nanoparticles were characterized for their micromeritic and crystallographic properties, drug content, in-vitro release and the ability to delay pantoprazole release in acidic medium to prevent its degradation. Physicochemical properties of nanoparticles, including particle size, loading capacity (LC), encapsulation efficiency (EE) and in-vitro drug release were significantly affected by formulation conditions. All formulas showed sub micronized size ranging from 299.3 ± 4.62 to 639.7 ± 9.71 nm and achieved delayed release to protect pantoprazole from degradation with different degrees, but generally Hydroxypropyl methyl cellulose phthalate HP55 loaded nanoparticles showed slower drug release than that of Eudragit S100 loaded nanoparticles. Release kinetics and morphological properties of nanoparticles with most delayed release pattern were investigated by Transmission Electron Microscope (TEM) and Compatibility between pantoprazole and polymer was proved by Fourier Transmission Infra Red (FT-IR) and Differential Scanning calorimetry (DSC). The formula stability was evaluated by measuring zeta potential value. Our results suggested that nanoprecipitation method is effective to produce pH-sensitive polymeric nanoparticles, which can be used as a delivery system for acid labile drug (Pantoprazole) to avoid its degradation in acidic medium of the stomach.