Formulation, Solid State Characterization and Enhancement of Dissolution Rate of Olmesartan Medoxomil by Polyvinyl Alcohol-Polyethylene Glycol Graft Copolymer Based Nanoparticles

Abstract

The objectives of present investigation were to prepare and evaluate nanoparticles of Olmesartan medoxomil (OLM) by a precipitation method using polyvinyl alcoholpolyethylene glycol graft copolymer (Kollicoat IR) and to investigate the effect of stirring speed & time on particle size. Particles were characterized for drug content, FTIR, zeta potential (ZP), particle size distribution (Dynamic light scattering), differential scanning calorimeter (DSC), powder X-ray diffraction (PXRD), scanning electron microscopy (SEM), solubility, in vitro release and stability studies. All batches showed drug content in range of 93.24 ± 0.96% to 99.91 ± 0.98%, particle size in range of 136.3-188.9 nm. As stirring speed increased particles of reduced size obtained and vice versa. ZP values of formulations were from -2.28 mV to -17.90 mV & comply with requirement of ZP for stability. Solubility results indicated improvement in solubility of formulations. PXRD analysis showed particles were in same crystalline state as raw OLM. Particle exhibited enhanced dissolution compared to raw material due to reduction in particle size, increased surface area & solubility. When formulated in tablets showed improvement in dissolution, compared to marketed formulation, anti solvent precipitation method is promising tool to prepare OLM particles by using Kollicoat IR as a polymer, for enhancement of solubility, dissolution velocity of OLM.

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“…[9,10] The unabsorbed drug may cause gastrointestinal side effects such as abdominal pain, dyspepsia, gastroenteritis, and nausea. [11] In the literature nanoparticles, [12] nanosuspension [10] and complexation with cyclodextrin [11] have been reported to improve solubility of OLM. Therefore, formulation approaches are being explored to enhance dissolution of OLM using poloxamer 407.…”

“…20 tablets from each batch were crushed and tablet powder equivalent to 40 mg of OLM was weighed and estimated for drug content using earlier reported UV spectrophotometric method. [12] Wetting time and in vitro disintegration test (Electrolab, Mumbai, India) were performed for all the prepared batches as per the procedure laid down in the previously published literature. [18] In vitro drug release…”

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“…of OLM oral dosage form remains unabsorbed in GIT which causes side effects such as abdominal pain, gastroenteritis, nausea, and dyspepsia. [8] To overcome the problem, researchers employed nanonization approach which may result in improved solubility and enhanced oral bioavailability of OLM. The oral fastdissolving strip (OFDS) was developed for the geriatric and bedridden patients who have difficulty in swallowing and to acquire faster onset of action.…”