Formulation and Characterization of Nateglinide Nanosuspension by Precipitation Method
DOI:
https://doi.org/10.37285/ijpsn.2014.7.4.11Abstract
Poor water solubility and slow dissolution rate are major issues for the majority of upcoming and existing biologically active pharmaceutical compounds. Nateglinide is Biopharmaceutical Classification System Class-II drug that has low solubility and high permeability. The purpose of the present study was to improve the solubility and dissolution rate of Nateglinide by the preparation of nanosuspension by the nanoprecipitation technique. Nateglinide nanosuspension was evaluated for its particle size, in vitro dissolution study, and characterized by differential scanning calorimetry and scanning electron microscopy. The optimized formulation showed an average particle size of 207 nm and zeta potential of -25.8 mV. The rate of dissolution of the optimized nanosuspension was enhanced by 83% in 50 min relative to micronized suspension of nateglinide (37% in 50 min). This improvement was mainly due to the formulation of nanosized particles of Nateglinide. Stability study revealed that nanosuspension was more stable at room temperature and refrigerator condition with no significant change in particle size distribution. These results indicate that the nateglinide loaded nanosuspension may significantly improve in vitro dissolution rate and thereby possibly enhance the onset of therapeutic effect.
Downloads
Metrics
Keywords:
Nateglinide, Nanosuspension, Nanoprecipitation, Solubility, Dissolution rate
Downloads
Published
How to Cite
Issue
Section
References
Agrawal S, Pancholi S, Jain NK and Agrawal GP (2004). Hydrotropic solubilisation of nimesulide for parentral administration. Int J Pharm 274: 149-155.
Chorny M, Fishbein I, Danenberg HD and Golomb G (2002). Lipophilic drug loaded nanospheres prepared by nanoprecipitation: effect of formulation variables on size, drug recovery and release kinetics. J Control Release 83: 389-400.
Das S and Suresh PK (2011). Nanosuspension: a new vehicle for the improvement of the delivery of drugs to the ocular surface. Application to amphotericin B. Nanomedicine 7: 242-247.
Dhapte V and Pokharkar V (2011). Polyelectrolyte stabilized antimalarial nanosuspension using factorial design approach. J Biomed Nanotechnol 7: 139-141.
Dubey R (2006). Impact of nanosuspension technology on drug discovery and development. Drug Delive Technol 4: 65-67.
Fasinu P, Pillay V, Ndesendo VM, Du Toit LC and Choonara YE (2011). Diverse approaches for the enhancement of oral drug bioavailability. Biopharmaceutics and Drug Disposition 32: 185-209.
Fessi H, Puisieux F, Devissaguet JP, Ammoury N and Benita S (1989). Nanocapsule formulation by interfacial polymer deposition following solvent displacement. Int J Pharm 55: R1-4.
Ghosh I, Bose S, Vippagunta R and Harmon F (2011). Nanosuspension for improving the bioavailability of a poorly soluble drug and screening of stabilizing agents to inhibit crystal growth. Int J Pharm 409: 260-268.
Krishna RSM, Shivakumar HG and Gowda DV (2006). Nanoparticles: A novel colloidal drug delivery system. Indian J Pharm Edu Res 40: 15-20.
Lee J, Lee SJ, Choi JY, Yoo JY and Ahn CH (2005). Amphiphilic amino acid copolymers as stabilizers for the preparation of nanocrystal dispersion. Eur J Pharm Sci 24: 441-449.
Lou H, Gao L, Wei X, Zhang Z, Zheng D, Zhang D, Zhang X, Li Y and Zhang Q (2011). Oridonin nanosuspension enhance anti-tumor efficacy in SMMC-7721 cells and H22 tumor bearing mice. Colloid Surface B 87: 319-325.
Maheshwari RK and Shilpkar R (2012). Formulation development and evaluation of injection of poorly soluble drug using mixed solvency concept. Int J pharm Bio Sci 3: 179-189.
Mahmoud KA, Mena JA, Male KB, Hrapovic S, Kamen A and Luong JH (2010). Effect of surface charge on the cellular uptake and cytotoxicity of fluorescent labelled cellulose nanocrystals. ACS Appl Mater Interfaces 2: 2924-2930.
Manju R, Deependra S and Swarnalata S (2006). Nanocarrier: Promising vehicle for bioactive drugs. Biol Pharm Bull 29: 1790-1798.
Merisko-Liversidge E, Liversidge GG and Cooper ER (2003). Nanosizing: a formulation approach for poorly- soluble compounds. Eur j Pharm Sci 18:113-120.
Mittal P, Singh P, Verma A, Khinchi MP, Agarwal D, Gupta MK and Sigh SP (2013). Nanosuspension: Newer approach for drug delivery system. Asian Journal of Pharmaceutical Research and Development 1: 2-12.
Norman P and Rabasseda X (2001). Nateglinide: A structurally novel, short-acting, hypoglycemic agent. Drugs Today 37: 411.
Pavia DL, Gary ML and Gaorge SK (2001). Introduction to spectroscopy A guide for students of organic chemistry, 3rd ed: 26-81.
Quan P, Shi K, Piao HZ, Liang N, Xia DN and Cui FD (2012). A novel surface modified nitrendipine nanocrystals with enhancement of bioavailability and stability. Int J Pharm 430: 336-371.
Rajalakshmi R, Venkataramudu T, Kumar AL, Sree DK and Kiranmayi D (2012). Design and characterization of valsartan nanosuspension. Inter J of Pharmacotherapy 2: 70-81.
Shegokar R and Muller RH (2010). Nanocrystals: Industrially feasible multifunctional formulation technology for poorly soluble actives. Int J Pharm 399: 129-139.
Singh SK, Srinivasan KK, Growthamrajan K, Singare DS, Prakash D and Gaikwad NB (2011). Investigation of preparation parameters of nanosuspension by top-down media milling to improve the dissolution of poorly water-soluble glyburide. Eur J Pharm Biochem 78: 441-446.
Soni LK, Solanki SS and Maheshwari RK (2014). Solubilization of poorly water soluble drug using mixed solvency approach for aqueous injection. British Journal of Pharmaceutical Research 4: 549-568.
Van Eerdenbrugh B, Stuyven B, Froyen L, Van Humbeeck J, Martens JA, Augustijns P and Van den Mooter G (2009). Downscaling drug nanosuspension production: Processing aspects and physicochemical characterization. Aaps Pharm sci tech 10: 44-53.
Van Eerdenbrugh B, Van den Mooter G and Augustijns P (2008). Top-down production of drug nanocrystals:Nanosuspension stabilization, miniaturization and transformation into solid product. Int J Pharm 364: 64-75.
Van Eerdenbrugh B, Vercruysse S, Martens JA, Vermant J, Froyen L, Van Humbeeck J, Van den Mooter G and Augustijns P (2008). Microcrystalline cellulose, a useful alternative for sucrose as a matrix former during freeze-drying of drug nanosuspension- A case study with itraconazole. Eur J Pharm Biopharm 70: 590-596.
Wang YC, Zhang DR, Liu ZP, Liu GP, Duan CX, Jia LJ, Feng FF, Zhang XY, Shi YQ and Zhang Q (2010). In vitro and in vivo evaluation of silybin nanosuspensions for oral and intravenous delivery. Nanotechnology 21: 155104.
Zheng DD, Wang YC, Zhang DR, Liu ZP, Duan CX, Jia LJ, Wanf FH, Liu Y, Liu GP, Hao LL and Zhang Q (2011). In- vitro antitumor activity of silybin nanosuspension in PC-3 cells Cancer Lett 307: 158-164.
