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Controlled release chitosan microspheres of mirtazapine: in vitro and in vivo evaluation.
Arch Pharm Res. 2011 Nov; 34(11):1919-29.AP

Abstract

The purpose of the study was to formulate and evaluate controlled release chitosan microspheres of mirtazapine (MTZ) to improve the bioavailability by altering the pharmacokinetic profiles of the drug. Chitosan microspheres were prepared to prolong the release of the drug into the systemic circulation. Microspheres were prepared by a single water in oil (w/o) emulsion technique varying the chitosan/drug ratio, stirring speed and concentration of the crosslinking agent (glutaraldehyde). Drug-polymer compatibility studies were carried out using fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC). The microspheres were evaluated for encapsulation efficiency, particle size, surface morphology, swelling index, in vitro release, as well as erosion and in vivo studies in rats. The FT-IR and DSC studies revealed no interaction between drug and polymer. The encapsulation efficiency of different formulation varied from 53 ± 1.2% to 78 ± 1.5%. The mean particle size of the optimized formulation F-14 was 106.4 ± 0.5 μm. Surface morphology revealed that chitosan microspheres were discrete and spherical in shape with a porous surface. The release of MTZ from chitosan microspheres was rapid up to 4 h, and then it was continuously and slowly released up to 48 h. Optimized formulation (F-14) was found to be stable under accelerated storage conditions based on International Conference on Harmonisation guidelines. Pharmacokinetic studies revealed that the optimized formulation showed significant increases in systemic exposure (AUC = 177.70 ± 7.39 μg·h/mL), half-life (4.72 ± 0.46 h) and reduced clearance (0.009 ± 0.0001 L/h) compared to pure drug administration. Hence, the present study demonstrates that controlled release formulation of MTZ microspheres using chitosan can improve pharmacokinetic profiles of MTZ.

Authors+Show Affiliations

Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576104, Karnataka, India.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

22139691

Citation

Ranjan, Om Prakash, et al. "Controlled Release Chitosan Microspheres of Mirtazapine: in Vitro and in Vivo Evaluation." Archives of Pharmacal Research, vol. 34, no. 11, 2011, pp. 1919-29.
Ranjan OP, Shavi GV, Nayak UY, et al. Controlled release chitosan microspheres of mirtazapine: in vitro and in vivo evaluation. Arch Pharm Res. 2011;34(11):1919-29.
Ranjan, O. P., Shavi, G. V., Nayak, U. Y., Arumugam, K., Averineni, R. K., Meka, S. R., & Sureshwar, P. (2011). Controlled release chitosan microspheres of mirtazapine: in vitro and in vivo evaluation. Archives of Pharmacal Research, 34(11), 1919-29. https://doi.org/10.1007/s12272-011-1112-1
Ranjan OP, et al. Controlled Release Chitosan Microspheres of Mirtazapine: in Vitro and in Vivo Evaluation. Arch Pharm Res. 2011;34(11):1919-29. PubMed PMID: 22139691.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Controlled release chitosan microspheres of mirtazapine: in vitro and in vivo evaluation. AU - Ranjan,Om Prakash, AU - Shavi,Gopal Venkatesh, AU - Nayak,Usha Yogendra, AU - Arumugam,Karthik, AU - Averineni,Ranjith Kumar, AU - Meka,Sreenivasa Reddy, AU - Sureshwar,Pandey, Y1 - 2011/12/03/ PY - 2011/03/03/received PY - 2011/04/25/accepted PY - 2011/04/13/revised PY - 2011/12/6/entrez PY - 2011/12/6/pubmed PY - 2012/5/2/medline SP - 1919 EP - 29 JF - Archives of pharmacal research JO - Arch. Pharm. Res. VL - 34 IS - 11 N2 - The purpose of the study was to formulate and evaluate controlled release chitosan microspheres of mirtazapine (MTZ) to improve the bioavailability by altering the pharmacokinetic profiles of the drug. Chitosan microspheres were prepared to prolong the release of the drug into the systemic circulation. Microspheres were prepared by a single water in oil (w/o) emulsion technique varying the chitosan/drug ratio, stirring speed and concentration of the crosslinking agent (glutaraldehyde). Drug-polymer compatibility studies were carried out using fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC). The microspheres were evaluated for encapsulation efficiency, particle size, surface morphology, swelling index, in vitro release, as well as erosion and in vivo studies in rats. The FT-IR and DSC studies revealed no interaction between drug and polymer. The encapsulation efficiency of different formulation varied from 53 ± 1.2% to 78 ± 1.5%. The mean particle size of the optimized formulation F-14 was 106.4 ± 0.5 μm. Surface morphology revealed that chitosan microspheres were discrete and spherical in shape with a porous surface. The release of MTZ from chitosan microspheres was rapid up to 4 h, and then it was continuously and slowly released up to 48 h. Optimized formulation (F-14) was found to be stable under accelerated storage conditions based on International Conference on Harmonisation guidelines. Pharmacokinetic studies revealed that the optimized formulation showed significant increases in systemic exposure (AUC = 177.70 ± 7.39 μg·h/mL), half-life (4.72 ± 0.46 h) and reduced clearance (0.009 ± 0.0001 L/h) compared to pure drug administration. Hence, the present study demonstrates that controlled release formulation of MTZ microspheres using chitosan can improve pharmacokinetic profiles of MTZ. SN - 0253-6269 UR - https://www.unboundmedicine.com/medline/citation/22139691/Controlled_release_chitosan_microspheres_of_mirtazapine:_in_vitro_and_in_vivo_evaluation_ L2 - https://dx.doi.org/10.1007/s12272-011-1112-1 DB - PRIME DP - Unbound Medicine ER -