Exemestane loaded polymeric nanoparticles for oral delivery

Document Type: Reasearch Paper

Authors

Department of Pharmaceutics, Sri Venkateshwara College of Pharmacy & Research Centre, Affiliated to Osmania University, Hyderabad, India.

10.7508/ijnd.2015.04.010

Abstract

The aim of the present study was to develop Exemestane loaded polymeric nanoparticles for improved oral bioavailability of Exemestane. Exemestane loaded nanoparticles were prepared by solvent displacement method with Eudragit RL 100 and Eudragit L 100 as polymers and Pluronic® F-68 as surfactant. The influence of various formulation factors (drug: polymer ratio and concentration of surfactant) on particle size, size distribution, zeta potential, encapsulation efficiency, in vitro drug release were investigated. The mean particle size of optimized formulations F5 and F13 were found to be 98.19nm and 48.16nm respectively. Zeta potential of optimized formulations F5 and F13 were found to be +22mV and -25mV respectively. Fourier Transform Infrared Spectroscopy (FT-IR) study indicated that, there was no interaction between drug and polymers. Scanning electron microscopy (SEM) study revealed spherical morphology of the developed NPs. The results of the present investigation indicate that the formulations F5 and F13 can be considered as best among various formulations with respect to particle size, entrapment efficiency and in-vitro drug release. In conclusion, this study indicates the capability of Eudragit nanoparticles in enhancing the oral bioavailability of exemestane.

Keywords

Main Subjects


 

[1]      Bibby D. C., Talmadge J. E., Dalal M. K., Kurz S. G., Chytil K. M., Barry S. E., Shand D. G., Steiert M., (2005), Pharmacokinetics and biodistribution of RGD-targeted doxorubicin loaded nanoparticles in tumor-bearing mice. Int. J. Pharm. 293: 281-290.        

[2]      Sanjoy K. D., Bivash M., Manas B., Lakshmi K. Gh., (2009), Development and in vitro evaluation of Letrozole loaded biodegradable nanoparticles for breast cancer therapy.  Braz. J. Pharm. Sci. 45: 33-36.

[3]      Basudev S., Kousik S., Sumit B., Biswajit Mu., (2010), Development of biodegradable polymer based tamoxifen citrate loaded nanoparticles and effect of some manufacturing process parameters on them: a physicochemical and in-vitro evaluation. Int. J. Nanomed. 5: 621–630.

[4]      Miller W. R., Dixon J. M., (2002), Endocrine and clinical endpoints of exemestane as neoadjuvant therapy. Cancer Cont. 9: 9–15.

[5]      Arbos P, Campanero M. A, Arangoa M. A, Renedo M. J, Irache J. M., (2003), Influence of the surface characteristics of PVM/ MA nanoparticles on their bioadhesive properties. J. Control. Release. 89: 193-201.

[6]      Andrew R., (2009), A review of the use of exemestane in early breast cancer. Therap. Clin. Risk Manag. 5: 91–98.

[7]      Scott L. J., Wiseman L. R., (1999), Exemestane. Drugs. 58: 675–680.

[8]      Lonning P. E., (1998), Pharmacological profiles of exemestane and formestane, steroidal aromatase inhibitors used for treatment of postmenopausal breast cancer. Breast Cancer Res. Treat. 49: 45-50.

[9]      Praveen S., Hiremath K. S., Soppimath G., Betageri V., (2009),  Proliposomes of exemestane for improved oral delivery: Formulation and in vitro evaluation using PAMPA, Caco-2 and rat intestine. Int. J. Pharm. 380: 96–104.

[10]  Ajeet K., Singh A. Ch., Manish S., Satish C., Upadhyay R., Mukherjee,and R., Khar K., (2008),  Exemestane Loaded Self-Microemulsifying Drug Delivery System (SMEDDS): Development and Optimization., AAPS Pharm. Sci. Tech. 2: 628-34.

[11]  Burc Y., Erem B., I˙mran V., Murat S.¸ (2010), Alternative oral exemestane formulation: Improved dissolution and permeation. Int. J. Pharm. 398: 137–145.

[12]  Lobenberg R., Amidon G. L., (2000), Modern bioavailability, bioequivalence and biopharmaceutics classification system. New scientific approaches to international regulatory standards. Eur. J. Pharm. Biopharm. 50: 3–12.

[13]  FDA NDA 20753/S006–Approved Labeling & Clinical Pharmacology and Biopharmaceutics Review(s).

[14]  Naik J. B., Mokale V. J., (2012), Formulation and evaluation of Repaglinide nanoparticles as a sustained release carriers. Novel Sci. Int. J. Pharm. Sci. 1: 259-266.

[15]  Yuyan J., Nathalie U., Monique M.-A., Claude V., Maurice H., Thomas L., Philippe M., (2002), In vitro and in vivo evaluation of oral heparin-loaded polymeric nanoparticles in rabbits. J. Am. Heart Assoc.105: 230-235.

[16]  Ubrich N., Schmidt C., Bodmeier R., Hoffman M., Maincent P., (2005), Oral evaluation in rabbits of cyclosporin-loaded Eudragit RS or RL nanoparticles. Int. J. Pharm. 288: 169–175.

[17]  Prakash B., Hariom U., Sajeev Ch., (2011), Brimonidine Tartrate–Eudragit Long-Acting Nanoparticles: Formulation, Optimization, In Vitro and In Vivo Evaluation. AAPS Pharm. Sci. Tech. 12: 1087–1101.