FORMULATION ANDCHARACTERIZATION OF OLANZEPINELOADED MUCOADHESIVE MICROSPHERES
DOI:
https://doi.org/10.22159/ajpcr.2017.v10i4.16659Abstract
Objective: The objective of this research was to formulate and evaluate olanzapine (OLE) mucoadhesive microsphere prepared using carbopol and sodium combination. OLE having extensive hepatic first pass metabolism and low bioavailability problem, determined the need for the development of sustained release formulation.
Methods: OLE mucoadhesive microspheres were prepared by ionic gelation method. OLE mucoadhesive microspheres were prepared by ionic gelation method by using calcium chloride as crosslinking agent. The OLE mucoadhesive microsphere was characterized by particle size measurement, process yield, morphology of microsphere, drug entrapment efficiency, mucoadhesion test, differential scanning calorimetry, powder X-ray diffraction, Fourier transforms infrared (FTIR) study and in-vitro drug release.
Results: The OLE mucoadhesive microsphere having mean particle size ranged from 546.0 µm to 554.3 µm, and the entrapment efficiencies ranged from 73% to 96%. All the olanzapine (OLE) microsphere batches showed good in-vitro mucoadhesive property ranging from 75.89% to 96.47% and in the in-vitro wash off test ranging from 68.12% to 81.3%. FTIR studies indicated the no drug-polymer interactions in the ideal formulation F9. There
were no compatibility issues, and the crystallinity of OLE was found to be reduced shoeing less intense peak in prepared mucoadhesive microspheres, which were confirmed by differential scanning calorimeter and X-ray diffraction studies. Among different formulations, the OLE microspheres of batch F9 had shown the optimum percent drug entrapment of microspheres. Release pattern of OLE from F9 microspheres batch followed Higuchi kinetic model. Stability studies were carried out for F9 formulation at 4°C/ambient, 25±2°C/60±5%, 40±2°C/75±5% relative humidity revealed that the drug entrapment, mucoadhesive behavior, and drug release were within permissible limits.
Conclusion: The results obtained in this work demonstrate the use of carbopol and sodium alginate polymer for preparation of mucoadhesive microsphere.
Keywords: Ionic gelation method, Gastroretentive delivery, Mucoadhesive microsphere, Carbopol.
Downloads
References
Krishnamoorthy V, Nagalingam A, Priya Ranjan Prasad V, Parameshwaran S, George N, Kaliyan P. Characterization of olanzapine-solid dispersions. Iran J Pharm Res 2011;10(1):13-24.
Badshah A, Subhan F, Rauf K. Controlled release matrix tablets of olanzapine: Influence of polymers on the in vitro release and bioavailability. AAPS PharmSciTech 2010;11(3):1397-404.
Das MK, Senapati PC. Evaluation of furosemide-loaded alginate microspheres prepared by ionotropic external gelation technique. Acta Pol Pharm 2007;64(3):253-62.
Nayak BS, Ghosh SK, Patro KT. Preparation and characterization of famotidine microcapsule employing mucoadhesive polymers in combination to enhance gastro retention for oral delivery. Int J Pharm Pharm Sci 2009;2(1):1-9.
Sahu S, Chourasia A, Toppo A, Asati A. Formulation and evaluation of captropril microspheres by ionic gelation technique. Int J Pharm Life Sci 2012;3(1):1377-9.
Velmurugan S, Ali MA. Development and evaluation of ritonavir mucoadhesive microspheres. Asian J Pharm Clin Res 2014;7(5):47-52.
Galgette U, Chaudhari PD. Preparation and evaluation of bioadhesive microspheres prepared by ion gelation method and effect of variables on quality of microspheres. Am J PharmTech Res 2013;3(4):535-46.
Das M, Senapati PC. Evaluation of furosemide loaded alginate microspheres prepared by ionotropic external gelation technique. Acta Pol Pharm 2007;64(3):253-62.
Venkateswaramurthy N, Sambathkumar R, Vijayabaskaran M, Perumal P. Formulation and in-vitro evaluation of furazolidone mucoadhesive microspheres. Int J Pharm Pharm Sci 2010;2(3):104-6.
Patil S, Choudhary B, Rathore A, Roy K, Mahadik K. Enhanced oral bioavailability and anticancer activity of novel curcumin loaded mixed micelles in human lung cancer cells. Phytomedicine 2015;22(12):1103-11.
Velmurugan S, Ali MA. Formulation and evaluation of maraviroc mucoadhesive microsheres by ionotropic gelation method. Int J Pharm Pharm Sci 2013;5(4):294-302.
Kuchekar S, Mohite S. Plackett-burman screening of olmesartan medoxomil liquisolid tablets: Quality by design approach. Asian J Pharm Clin Res 2015;8(3):292-300.
Ararath D, Velmurugan S. Formulation and evaluation of nevirapine mucoadhesive microspheres. madhurideshmukh9@yahoo.com Int J Pharm Sci 2015;7(6):342-8.
Lehr CM, Bowstra JA, Tukker JJ, Junginger HE. Intestinal transit of bioadhesive microspheres in an in situ loop in the rat-a comparative study with copolymers and blends based on poly(acrylic acid). J Control Release 1990;13(1):51-62.
Sonawane S, Bhalekar M, Shimpi S. Preparation and evaluation of microspheres of xyloglucan and its thiolated xyloglucan derivative. Int J Biol Macromol 2014;69:499-505.
Swain S, Behera A, Dinda SC, Patra CN, Jammula S, Beg S, et al. Formulation design, optimization and pharmacodynamic evaluation of sustained release mucoadhesive microcapsules of venlafaxine HCl. Indian J Pharm Sci 2014;76(4):354-63.
Sellappan V, Mohamed A. Development and evaluation of ritonavir mucoadhesive microsphere. Asian J Pharm Clin Res 2014;7(5):47-52.
Velmurugan S, Ali M. Development and evaluation of ritonavir mucoadhesive microspheres. Asian J Pharm Clin Res 2014;7(5):47-52.
Kuchekar S, Mohite S Plackett-burman screening of olmesartan medoxomil liquisolid tablets: quality by design approach. Asian J Pharm Clin Res 2015; 8(3):292-300.
Gudikandula R, Madhavi K, Thakkalapally SR, Veeramalla A, Prasad IR. Enhancement of solubility and dissolution rate of ezetimibe through liquisolid technique. Int J Pharma Sci Res 2013;4(8):3229-38.
Published
How to Cite
Issue
Section
The publication is licensed under CC By and is open access. Copyright is with author and allowed to retain publishing rights without restrictions.
