5–4.5 h) It also eliminated rapidly through urine (∼90%) and faeces (∼20%) within 8–12 h.4 and 5 Therefore repeated administration of high doses are required to maintain effective plasma concentration and thus reducing patient compliance with side effects like PD0325901 clinical trial abdominal discomfort, anorexia, nausea and diarrhea. Metformin HCl is highly water soluble drug therefore here the role of polymer is so
important to control it for maximum time in gastric environment. In present study we developed the metformin HCl loaded nanoparticles by non-aqueous solvent emulsion evaporation technique and characterized it. The challenge in our study was to enhance the encapsulation percentage of metformin in polymeric nanoparticles core and decrease initial burst release. This was achieved by total hydrophobic environment and examines the effect of different viscosity grade ethylcellulose
on drug loading and release profile. All nanoparticle formulations evaluated by particle size, zeta potential, drug content, product recovery, surface morphology, drug-polymer interaction, X-ray diffraction and in vitro dissolution study, etc. Metformin HCl was kindly gifted by Aarti Drugs Pvt. Ltd., Mumbai. ETHOCEL Standard 45 Premium Ethylcellulose (45 cP) (EC45) and ETHOCEL Standard 100 Premium Ethylcellulose (100 cP) (EC100) were gift sample by Colorcorn Asia Pvt. Ltd., Goa. Ethylcellulose (300 cP) Selleck BMS-754807 (EC300) procured from Sigma–Aldrich, USA. In all polymers ethoxyl content was 48–49.5%. Methanol and SPAN 80 were purchased from Merck, Mumbai and Ozone International, Mumbai respectively.
Liquid Paraffin Light procured from Himedia Lab Pvt. Ltd. Mumbai. Dissolution medium was prepared by using triple distilled water filtered with 0.22 μ membrane filter. Nanoparticles were prepared by oil in oil (O/O) solvent evaporation technique.6 Metformin HCl and ethylcellulose polymers (EC45/EC100/EC300) were dissolved in methanol at 1:3, 1:6 and 1:9 ratios by magnetic lab stirrer (Remi, India). After complete soluble in methanol, organic phase was added drop by drop in Liquid Paraffin Light containing 0.4% v/v Span 80. During this addition Terminal deoxynucleotidyl transferase emulsion was stirred by high speed homogenizer (Omni GLH homogenizer) at 25,000 rpm. The temperature of external phase was maintained. Then solution was stirred for 2 h to allow complete evaporation of solvent. After removal of solvent nanoparticles were separated from oil by centrifugation (R243A, Remi) at 18,000 rpm for 30 min. The separated nanoparticles were repeatedly washed with n-hexane until free from oil. The collected nanoparticles were dried at room temperature and subsequently stored in desiccator for 24 h. Viscosities of internal phases at different ratios of all polymers were measured by Brookfield rotational digital viscometer DVLV II at 25 °C. The obtained nanoparticles were suspended in distilled water and sonicate before analysis for 10 s. Particle size determined at 25 °C by using Nano series Malvern Instruments, UK.