Formulation and Characterization of Glimepiride Nanoparticles for Dissolution Enhancement

Author(s): Reena Siwach, Parijat Pandey, Harish Dureja*

Journal Name: Nanoscience & Nanotechnology-Asia

Volume 10 , Issue 5 , 2020


Become EABM
Become Reviewer
Call for Editor

Graphical Abstract:


Abstract:

Background: The rate-limiting step in the oral absorption of BCS class II drugs is dissolution. Their low solubility is one of the major obstacles in the process of drug development. Dissolution rate can be increased by decreasing the particle size to the nano range, eventually leading to increased bioavailability.

Objective: In the present study, glimepiride loaded nanoparticles were prepared to enhance the dissolution rate. The aim of the work was to examine the effect of polymer-drug ratio, solvent-antisolvent ratio and speed of mixing on in vitro release of glimepiride.

Methods: Glimepiride is an antidiabetic drug belonging to the BCS class II drugs. The polymeric nanoparticles were formulated according to Box-Behnken Design (BBD) using nanoprecipitation technique. The prepared nanoparticles were evaluated for in vitro drug release, loading capacity, entrapment efficiency, and percentage yield.

Results: It was found that NP-8 has maximum in vitro drug release and was selected as an optimized batch. Analysis of Variance (ANOVA) was applied to the in vitro drug release to study the fitness and significance of the model. The batch NP-8 showed 70.34 ± 1.09% in vitro drug release in 0.1 N methanolic HCl and 92.02 ± 1.87% drug release in phosphate buffer pH 7.8. The release data revealed that the nanoparticles followed zero order kinetics.

Conclusion: The study revealed that the incorporation of glimepiride into gelucire 50/13 resulted in enhanced dissolution rate.

Keywords: Dissolution enhancement, antidiabetic, glimepiride, polymeric nanoparticles, in vitro release study, Box-Behnken design.

[1]
Fu, Q.; Kou, L.; Gong, C.; Li, M.; Sun, J.; Zhang, D.; Liu, M.; Sui, X.; Lui, K.; Wang, S.; He, Z. Relationship between dissolution and bioavailability for nimodipine colloidal dispersions: The critical size in improving bioavailability. Int. J. Pharm., 2012, 427(2), 358-364.
[2]
Thorat, A.A.; Dalvi, S.V. Liquid antisolvent precipitation and stabilization of nanoparticles of poorly water-soluble drugs in aqueous suspensions: Recent developments and future perspective. Chem. Eng. J., 2012, 181-182, 1-34.
[3]
Beck, C.; Dalvi, S.V.; Dave, R.N. Controlled liquid antisolvent precipitation using a rapid mixing device. Chem. Eng. Sci., 2010, 65, 5669-5675.
[4]
World Health Organization. Available from: https://www.who.int/diabetes/country-profiles/en/ (Accessed on: 26 March 2019)
[5]
World Health Organization. Available from: https://www.who.int/news-room/fact-sheets/detail/diabetes (Accessed on: 26 March 2019)
[6]
International Diabetes federation. Available from: https://idf.org/52-about-diabetes.html (Accessed on: 26 March 2019)
[7]
Ilic, I.; Dreu, S.V.; Burjak, M.; Homar, M.; Kerc, J.; Srcic, S. Microparticle size control and glimepiride microencapsulation using spray congealing technology. Int. J. Pharm., 2009, 381, 176-183.
[8]
Rajpurohit, V.S.; Rakha, P.; Goyal, S.; Dureja, H.; Aroroac, G.; Nagpal, M. Formulation and characterization of solid dispersions of glimepiride through factorial design. Iran J. Pharm. Sci., 2011, 7(1), 7-16.
[9]
Gupta, M.K.; Goldman, D.; Bogner, R.H.; Tseng, Y.C. Enhanced drug dissolution and bulk properties of solid dispersions granulated with a surface adsorbent. Pharm. Dev. Technol., 2001, 6(4), 563-572.
[10]
Hadri, M.; Achahbar, A.; Khamkhami, J.; Khelifa, B.; Tuyet, C.; Faivre, V.; Abbas, O.; Marssi, M.; Bougrioua, F.; Bresson, S. Vibrational behavior of Gelucire 50/13 by Raman and IR spectroscopies: A focus on the 1800-1000 cm-1 spectral range according to temperature and degree of hydration. J. Mol. Struct., 2015, 1083, 441-449.
[11]
Du, B.; Shen, G.; Wang, D.; Pang, L.; Chen, Z.; Liu, Z. Development and characterization of glimepiride nanocrystal formulation and evaluation of its pharmacokinetic in rats. Drug Deliv., 2013, 20, 25-33.
[12]
Behera, A.; Srikanth, P.; Rao, Y.M.; Sahoo, S.K. Formulation and characterisation of glimepiride loaded biodegradable nanoparticles for the management of type 2 diabetes mellitus. Immunol. Endocrine. Metabol. Agents Med. Chem., 2016, 16(1), 49-60.
[13]
Ahmed, O.A.A.; El-Say, K.M.; Alahdal, A.M. A PLGA-reinforced PEG in situ gel formulation for improved sustainability of hypoglycemic activity of glimepiride in streptozotocin-induced diabetic rats. Sci. Reports., 2017, 7, 16384.
[14]
Upadhyay, P.; Pandit, J.K.; Wahi, A.K. Gelucire: An alternative formulation technological tool for both sustained and fast release of drugs in treating diabetes mellitus type 2 disease. J. Sci. Ind. Res., 2013, 72(12), 776-780.
[15]
Fu, Q.; Kou, L.; Gong, C.; Li, M.; Sun, J.; Zhang, D.; Liu, M.; Sui, X.; Lui, K.; Wang, S.; He, Z. Relationship between dissolution and bioavailability for nimodipine colloidal dispersions: The critical size in improving bioavailability. Int. J. Pharm., 2012, 427(2), 358-364.
[16]
Shah, S.R.; Parikh, R.H.; Chavda, J.R.; Sheth, N.R. Application of Plackett-Burman screening design for preparing glibenclamide nanoparticles for dissolution enhancement. Powder Technol., 2013, 235, 405-411.
[17]
Li, Z.; Tao, W.; Zhang, D.; Wu, C.; Song, B.; Wang, S.; Wang, T.; Hu, M.; Liu, X.; Wang, Y.; Sun, Y.; Sun, J. The studies of PLGA nanoparticles loading atorvastatin calcium for oral administration in vitro and in vivo. Asian J. Pharm. Sci., 2017, 12, 285-291.
[18]
Indian Pharmacopoeia. Government of India, Ministry of Health and Family Welfare; The Indian Pharmacopoeia Commission: Ghaziabad, 2014, p. 1865.
[19]
Shen, J.; Burgess, D.J. In vitro dissolution testing strategies for nanoparticulate drug delivery systems: Recent developments and challenges. Drug Deliv. Transl. Res., 2013, 3(5), 409-415.
[20]
Dong, Y.; Ng, W.K.; Shen, S.; Kim, S.; Tan, R.B.H. Preparation and characterization of spironolactone nanoparticles by antisolvent precipitation. Int. J. Pharm., 2009, 375, 84-88.
[21]
Reven, S.; Grdadolnik, J.; Kristl, J.; Žagar, E. Hyperbranched poly(esteramides) as solubility enhancers for poorly water-soluble drug glimepiride. Int. J. Pharm., 2010, 396(1-2), 119-126.
[22]
Pirooznia, N.; Hasannia, S.; Lotfi, A.S. Encapsulation of alpha-1 antitrypsin in PLGA nanoparticles: In vitro characterization as an effective aerosol formulation in pulmonary diseases. J. Nanobio-technol, 2012, 10(20), 1-15.


Rights & PermissionsPrintExport Cite as

Article Details

VOLUME: 10
ISSUE: 5
Year: 2020
Page: [649 - 663]
Pages: 15
DOI: 10.2174/2210681209666190422160115
Price: $25

Article Metrics

PDF: 9
HTML: 3