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Sustained release optimized formulation of anastrozole-loaded chitosan microspheres: in vitro and in vivo evaluation.
J Mater Sci Mater Med. 2011 Apr; 22(4):865-78.JM

Abstract

The purpose of this study was to develop sustained release formulation of anastrozole-loaded chitosan microspheres for treatment of breast cancer. Chitosan microspheres cross-linked with two different cross-linking agents viz, tripolyphosphate (TPP) and glutaraldehyde (GA) were prepared using single emulsion (w/o) method. A reverse phase HPLC method was developed and used for quantification of drug in microspheres and rat plasma. Influence of cross-linking agents on the properties of chitosan microspheres was extensively investigated. Formulations were characterized for encapsulation efficiency (EE), compatibility of drug with excipients, particle size, surface morphology, swelling capacity, erosion and drug release profile in phosphate buffer pH 7.4. EE varied from 30.4 ± 1.2 to 69.2 ± 3.2% and mean particle size distribution ranged from 72.5 ± 0.5 to 157.9 ± 1.5 μm. SEM analysis revealed smooth and spherical nature of microspheres. TPP microspheres exhibited higher swelling capacity, percentage erosion and drug release compared to GA microspheres. Release of anastrozole (ANS) was rapid up to 4 h followed by slow release status. FTIR analysis revealed no chemical interaction between drug and polymer. DSC analysis indicated ANS trapped in the microspheres existed in amorphous form in polymer matrix. The highest correlation coefficients (R (2)) were obtained for Higuchi model, suggesting a diffusion controlled mechanism. There was significant difference in the pharmacokinetic parameters (AUC(0-∞), Kel and t(1/2)) when ANS was formulated in the form of microspheres compared to pure drug. This may be attributed to slow release rate of ANS from chitosan microspheres and was detectable in rat plasma up to 48 h which correlates well with the in vitro release data.

Authors+Show Affiliations

Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka 576104, India. gopalshavi@gmail.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

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

Language

eng

PubMed ID

21431353

Citation

Shavi, Gopal V., et al. "Sustained Release Optimized Formulation of Anastrozole-loaded Chitosan Microspheres: in Vitro and in Vivo Evaluation." Journal of Materials Science. Materials in Medicine, vol. 22, no. 4, 2011, pp. 865-78.
Shavi GV, Nayak UY, Reddy MS, et al. Sustained release optimized formulation of anastrozole-loaded chitosan microspheres: in vitro and in vivo evaluation. J Mater Sci Mater Med. 2011;22(4):865-78.
Shavi, G. V., Nayak, U. Y., Reddy, M. S., Karthik, A., Deshpande, P. B., Kumar, A. R., & Udupa, N. (2011). Sustained release optimized formulation of anastrozole-loaded chitosan microspheres: in vitro and in vivo evaluation. Journal of Materials Science. Materials in Medicine, 22(4), 865-78. https://doi.org/10.1007/s10856-011-4274-y
Shavi GV, et al. Sustained Release Optimized Formulation of Anastrozole-loaded Chitosan Microspheres: in Vitro and in Vivo Evaluation. J Mater Sci Mater Med. 2011;22(4):865-78. PubMed PMID: 21431353.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Sustained release optimized formulation of anastrozole-loaded chitosan microspheres: in vitro and in vivo evaluation. AU - Shavi,Gopal V, AU - Nayak,Usha Y, AU - Reddy,M Sreenivasa, AU - Karthik,A, AU - Deshpande,Praful B, AU - Kumar,A Ranjith, AU - Udupa,N, Y1 - 2011/03/23/ PY - 2010/06/30/received PY - 2011/02/28/accepted PY - 2011/3/25/entrez PY - 2011/3/25/pubmed PY - 2011/10/15/medline SP - 865 EP - 78 JF - Journal of materials science. Materials in medicine JO - J Mater Sci Mater Med VL - 22 IS - 4 N2 - The purpose of this study was to develop sustained release formulation of anastrozole-loaded chitosan microspheres for treatment of breast cancer. Chitosan microspheres cross-linked with two different cross-linking agents viz, tripolyphosphate (TPP) and glutaraldehyde (GA) were prepared using single emulsion (w/o) method. A reverse phase HPLC method was developed and used for quantification of drug in microspheres and rat plasma. Influence of cross-linking agents on the properties of chitosan microspheres was extensively investigated. Formulations were characterized for encapsulation efficiency (EE), compatibility of drug with excipients, particle size, surface morphology, swelling capacity, erosion and drug release profile in phosphate buffer pH 7.4. EE varied from 30.4 ± 1.2 to 69.2 ± 3.2% and mean particle size distribution ranged from 72.5 ± 0.5 to 157.9 ± 1.5 μm. SEM analysis revealed smooth and spherical nature of microspheres. TPP microspheres exhibited higher swelling capacity, percentage erosion and drug release compared to GA microspheres. Release of anastrozole (ANS) was rapid up to 4 h followed by slow release status. FTIR analysis revealed no chemical interaction between drug and polymer. DSC analysis indicated ANS trapped in the microspheres existed in amorphous form in polymer matrix. The highest correlation coefficients (R (2)) were obtained for Higuchi model, suggesting a diffusion controlled mechanism. There was significant difference in the pharmacokinetic parameters (AUC(0-∞), Kel and t(1/2)) when ANS was formulated in the form of microspheres compared to pure drug. This may be attributed to slow release rate of ANS from chitosan microspheres and was detectable in rat plasma up to 48 h which correlates well with the in vitro release data. SN - 1573-4838 UR - https://www.unboundmedicine.com/medline/citation/21431353/Sustained_release_optimized_formulation_of_anastrozole_loaded_chitosan_microspheres:_in_vitro_and_in_vivo_evaluation_ L2 - https://doi.org/10.1007/s10856-011-4274-y DB - PRIME DP - Unbound Medicine ER -