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(PVA/polysorbate-80) in a fixed concentration (0.5%, w/v) were studied for particle size, drug loading, and entrapment efficiency. Nanoparticles were characterized by differential scanning calorimetry (DSC) and their shapes were observed by scanning electron microscopy (SEM). An aqueous solubility study indicated that the dissolution rates were remarkably increased for nanoparticles compared with the drug alone.The in vitro drug release study of the nanoparticles showed a biphasic release pattern: one initial burst release of 40.56% in the first 4 h which can be helpful to improve the penetration of drug
followed by a second slow-release phase (extended release) consistent with a Higuchi diffusion mechanism.The hypolipidemic activity of nanoparticles was determined in comparison with SV in male Wistar rats for changes in total cholesterol (CH) and triglyceride (TG) levels in blood. Nanoparticles showed a significantly better in vivo performance than SV in reducing total CH and TG levels which is primarily attributed to the improved solubility and dissolution of nanoparticles. Together, these results indicate that nanoparticulate formulations are ideal carriers for oral administration of SV having great potential
to improve the oral bioavailability and sustain the drug release, thereby minimizing the dose-dependent adverse effects and
maximizing the patientâ€™s compliance.
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Lipinski CA. Poor aqueous solubility â€“ an industry wide problem in
drug discovery. Am Pharm Rev 2002;53:82-5.
Vasconcelos T, Sarmento B, Costa P. Solid dispersions as strategy to
improve oral bioavailability of poor water soluble drugs. Drug Discov
Gursoy RN, Benita S. Selfemulsifying drug delivery systems (SEDDS)
for improved oral delivery of lipophilic drug. Biomed Pharmacother
Humberstone AJ, Charman WN. Lipid-based vehicles for the oral delivery
of poorly water soluble drugs. Adv Drug Deliv Rev 1997;25:103-28.
Wong SM, Kellaway LW, Murdan S. Enhancement of the dissolution
rate and oral absorption of a poorly water soluble drug by formation
of surfactant-containing microparticles. Int J Pharm 2006;317:61-8.
Kesisoglou F, Panmai S, Wu Y. Nanosizing â€” Oral formulation
development and biopharmaceutical evaluation. Adv Drug Deliv Rev
Stella VJ, Nti-Addae KW. Prodrug strategies to overcome poor water
solubility. Adv Drug Deliv Rev 2007;59:677-94.
Turk M, Hils P, Helfgen B, Schaber K, Martin H, Wahl MA. Micronization
of pharmaceutical substances by the Rapid Expansion of Supercritical
Solutions (RESS): A promising method to improve bioavailability of
poorly soluble pharmaceutical agents. J Supercrit Fluids 2002;22:75-84.
Rao VM, Nerurka M, Pinnamaneni S, Rinaldi F, Raghavan K.
Co-solubilization of poorly soluble drugs by micellization and
complexation. Int J Pharm 2006;319:98-106.
El-Badry M, Fetih G, Fathy M. Improvement of solubility and dissolution
rate of indomethacin by solid dispersions in Gelucire 50/13 and
PEG4000. Saudi Pharm J 2009;17:217-25.
Saha P, Kou JH. Effect of solubilizing excipients on permeation of poorly water-soluble compounds across Caco-2 cell monolayers. Eur J Pharm Biopharm 2000;50:403-11.
Kumari A, Yadav SK, Yadav SC. Biodegradable polymeric nanoparticles
based drug delivery systems. Colloids and Surf B Biointerfaces
Nishiyama N, Bae Y, Miyata K, Fukushima S, Kataoka K. Smart polymeric
micelles for gene and drug delivery. Drug Discov Today Technol
Shegokar R, Muller RH. Nanocrystals: Industrially feasible multifunctional
formulation technology for poorly soluble actives. Int J Pharm
Muller RH, Jacobs C, Kayser O. Nanosuspensions as particulate drug
formulations in therapy: Rationale for development and what we can
expect for the future. Adv Drug Deliv Rev 2001;47:3-19.
Kohli K, Chopra S, Dhar D, Arora S, Khar RK. Self-emulsifying drug
delivery systems: An approach to enhance oral bioavailability. Drug
Discov Today 2010;15:958-65.
Company literature on ZOCORÂ® (Simvastatin) Tablets. NJ, USA: Merck
and Co., Inc; 2004. p. 1-12.
Nirogi R, Mudigonda K, Kandikere V. Chromatographyâ€“mass
spectrometry methods for the quantitation of statins in biological
samples. J Pharm Biomed Anal 2007;44:379-87.
Kang BK, Lee JS, Chon SK, Jeong SY, Yuk SH, Khang G, et al. Development
of self-microemulsifying drug delivery systems (SMEDDS) for oral
bioavailability enhancement of simvastatin in beagle dogs. Int J Pharm
Margulis-Goshen K, Magdassi S. Formation of simvastatin nanoparticles
from microemulsion. Nanomedicine 2009;5:274-81.
Mao Z, Ma L, Gao C, Shen J. Preformed microcapsules for loading and
sustained release of ciprofloxacin hydrochloride. J Control Release
Gupta H, Aqil M, Khar RK, Ali A, Bhatnagar A, Mittal G. Sparfloxacin-
loaded PLGA nanoparticles for sustained ocular drug delivery.
Bodmeier R, McGinity JW. The preparation and evaluation of drug
containing poly(dl-lactide) microspheres formed by the solvent
evaporation method. Pharm Res 1987;4:465-71.
Muthu MS, Rawat MK, Mishra A, Singh S. PLGA nanoparticle
formulations of risperidone: Preparation and neuropharmacological
evaluation. Nanomedicine 2009;5:323-33.
Budhian A, Siegel SJ, Winey KI. Haloperidol-loaded PLGA nanoparticles: Systematic study of particle size and drug content. Int J Pharm 2007;336:367-75.
Quintanar-Guerrero D, Fessi H, Allemann E, Doelker E. Influence of
stabilizing agents and preparative variables on the formation of poly
(D, L-lactic acid) nanoparticles by an emulsification-diffusion technique.
Int J Pharm 1996;143:133-41.
Mainardes RM, Evangelista RC. PLGA nanoparticles containing
praziquantel: Effect of formulation variables on size distribution. Int
J Pharm 2005;290:137-44.
Lourenco C, Teixeira M, Simees S, Gaspar R. Steric stabilization of
nanoparticles: Size and surface properties. Int J Pharm 1996;138:1-12.
Kohane DS, Tse JY, Yeo Y, Padera R, Shubina M, Langer R. Biodegradable polymeric microspheres and nanospheres for drug delivery in the peritoneum. J Biomed Mater Res A 2006;77:351-61.
Zhanga Z, Bua H, Gaoa Z, Huanga Y, Gaoa F, Li Y. The characteristics
and mechanism of simvastatin loaded lipid nanoparticles to increase
oral bioavailability in rats. Int J Pharm 2010;394:147-53.
Vogel HG, Vogel WH. Drug discovery and evaluation: Pharmacological
assays. Berlin: Springer-Verlag; 1997. p. 604-11.
Elson CE. Tropical oils: Nutritional and scientific issues. Crit Rev Food
Sci Nutr 1992;31:79-102.