Author(s):
A. Anka Rao, Narender. Malothu, A. Narayana Rao, Bandaru Naga Raju, B. Jahasultana. Mohammed
Email(s):
Email ID Not Available
DOI:
10.52711/0974-360X.2023.00370
Address:
A. Anka Rao*, Narender. Malothu, A. Narayana Rao, Bandaru Naga Raju, B. Jahasultana. Mohammed
K L College of Pharmacy, Koneru Lakshmaiah Education Foundation, Vaddeswaram, Andhra Pradesh.
*Corresponding Author
Published In:
Volume - 16,
Issue - 5,
Year - 2023
ABSTRACT:
Gastro retentive dosage forms have potential for use as controlled- release drug delivery systems. Gastro retentive floating drug delivery systems have a bulk density lower than that of gastric fluids and thus increase residence time of drug in stomach and provide controlled delivery of many drugs. The aim of the present study is formulation and characterization of floating microspheres using Sitagliptin as a model drug for the management of type-2 diabetes mellitus. Floating microspheres were prepared by oil-in-water emulsion solvent evaporation technique using ethyl cellulose and eudragit S-100 as release retarding polymers. The floating microspheres were evaluated for percentage yield (%), particle size, drug content, drug entrapment efficiency, in-vitro floating ability and in-vitro drug release studies. The surface morphology of prepared microspheres was characterized by scanning electron microscopy. The microspheres were found to be spherical in shape and porous in nature. Compatibility studies were performed by fourier transform infrared (FTIR) technique. The prepared microspheres showed prolonged drug release of 12 h and remain buoyant for more than 12 h. In-vitro release kinetics were studied in different release kinetics models like zero order, first order, higuchi and korsmeyer peppas model and the best fit model was found to be higuchi plot with release exponent n value less than 0.89. It was concluded that developed floating microspheres of Sitagliptin offers a suitable and practical approach for prolonged release of drug over an extended period of time and thus oral bioavailability, efficacy and patient compliance is improved.
Cite this article:
A. Anka Rao, Narender. Malothu, A. Narayana Rao, Bandaru Naga Raju, B. Jahasultana. Mohammed. Formulation and Evaluation of Floating Microspheres of Sitagliptin. Research Journal of Pharmacy and Technology 2023; 16(5):2251-6. doi: 10.52711/0974-360X.2023.00370
Cite(Electronic):
A. Anka Rao, Narender. Malothu, A. Narayana Rao, Bandaru Naga Raju, B. Jahasultana. Mohammed. Formulation and Evaluation of Floating Microspheres of Sitagliptin. Research Journal of Pharmacy and Technology 2023; 16(5):2251-6. doi: 10.52711/0974-360X.2023.00370 Available on: https://rjptonline.org/AbstractView.aspx?PID=2023-16-5-29
REFERENCES:
1. Li S, Lin S, Daggy, BP, et al. Effect of HPMC and Carbopol on the release and floating properties of gastric floating drug delivery system using factorial design. Int J Pharm. 2003; 253:13–22, https://doi.org/10.1016/S0378-5173(02)00642-7.
2. Singh BN, Kim KH. Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention. J Control Release. 2000; 63:235, https://doi.org/10.1016/S0168-3659(99)00204-7.
3. Jagtap Yogesh Mukund, Bhujbal Rohan Kantilal, Ranpise Nisharani Sudhakar,Flaoting microsphere review. Brizillain Journal of Pharmaceutical Sciences. 2012; 48-1: 17-30, DOI:10.1590/S1984-82502012000100003.
4. H.M.El-Nahas and K.M. Hosny, T Hino, Y Itoh.chitosan based floating microspheres of trimetazidine dihydrochloride. Indian J Pharm Sci. 2011; 73(4): 397-403. doi: 10.4103/0250-474X.95619
5. M Sharma, S Kohli, A Dinda. In vitro and in vivo evaluation of repaglinide loaded floating microspheres prepared from different viscosity grades of HPMC polymer. Saudi Pharmaceutical Journal. 2015; 1-8, doi: 10.1016/j.jsps.2015.02.013
6. S. K. Jain, A. M. Awasthi, N. K. Jain, G. P. Agrawal. Calcium silicate based microspheres of repaglinide for gastroretentive floating drug delivery: preparation and in vitro characterization. Journal of Controlled Release. 2005; 107: 300-309. doi:1010.16/j.jconreol.2005.06.007
7. H Yadav, H Patel. Formulation and evaluation of floating microspheres of etodolac. American Journal of Pharmacy and Health Research. 2013; 1(2): 45-54. doi.org/10.3109/10717544.2013.834414.
8. Awasthi R, Kulkarni G, Pawar V, Garg G. Optimization studies on gastroretentive floating system using response surface methodology. AAPS Pharm Sci Tech. 2012; 13:85–93 , DOI https://doi.org/10.1208/s12249-011-9730-y
9. Bhadouriya P, Kumar M, Pathak K. Floating microspheres – to prolong the gastric retention time in stomach. Curr Drug Deliv. 2012; 9:315–24, http://dx.doi.org/10.2174/156720112800389061.
10. Costa P, Sousa Lobo JM, Modeling and comparison of dissolution profiles. Eur J Pharmaceut Sci. 2001; 13:123–33, https://doi.org/10.1016/S0928-0987(01)00095-1.
11. Dave BS, Amin AF, Patel MM, Gastroretentive drug delivery system of ranitidine hydrochloride: formulation and in vitro evaluation. AAPS Pharm Sci Tech. 2004; 5:77-82, DOIhttps://doi.org/10.1208/pt050234.
12. El-Kamel AH, Sokar MS, Al Gamal SS, Naggar VF, Preparation and evaluation of ketoprofen floating oral delivery system. Int J Pharm. 2001; 220:13–21, https://doi.org/10.1016/S0378-5173(01)00574-9.
13. Goyal P, Gill S, Gupta UD, et al. Development and characterization of rifampicin loaded floating microspheres. Artif Cell Blood Substit Biotechnol. 2011; 39:330–4, https://doi.org/10.3109/10731199.2011.573482.
14. Hoffman A, Stepensky D, Lavy E, etal. Pharmacokinetic and pharmacodynamic aspects of gastroretentive dosage forms. Int J Pharm. 2004; 277:141–53, https://doi.org/10.1016/j.ijpharm.2003.09.047.
15. Yedurkar P, Dhiman MK, Petkar K, Sawant K, Mucoadhesive bilayer buccal tablet of carvedilol-loaded chitosan microspheres: in vitro, pharmacokinetic and pharmacodynamic investigations. J. Microencapsul. 2012; 29:126–37, https://doi.org/10.3109/02652048.2011.630109.