Preparation and in vitro characterization of poly (epsilon-caprolactone)-based tamoxifen citrate- loaded cylindrical subdermal implant for breast cancer

Jagadeesh G Hiremath, V Kusum Devi

Abstract


In the present study cylindrical poly(epsilon-caprolactone) (PCL)-based biodegradable polymeric tamoxifen citrate-loaded subdermal implants were prepared by laboratory-based modified melt extrusion technique. The prepared implants were evaluated for their physicochemical parameters. Drug content in implants by high-performance liquid chromatographic (HPLC) method, differential scanning calorimetry (DSC), X-ray diffraction (XRD) and scanning electron microscope (SEM) studies of tamoxifen citrate-loaded implants. Determination of in vitro hydrolytic degradation of polymeric and tamoxifen citrate-loaded implants and in vitro drug release was carried out by using indigenously developed dissolution apparatus. DSC and XRD studies proved that the drug is entrapped in the implant. The highest rate of hydrolytic degradation (weight loss)
was observed in blank implants when compared to tamoxifen citrate-loaded implants.The studies proved that the developed method have potential in terms of industrial feasibility.


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References


Fung LK, Saltzman WM. Polymeric implants for cancer chemotherapy.

Adv Drug Deliv Rev 1997;7:209-30.

Macgregor JI, Jordan VC. Basic guide to the mechanisms of antiestrogen

action. Pharmacol Rev 1998;50:151-96.

Jordan VC. Designer estrogens. Sci Am 1998;279:60-7.

Szyczak J, Milewicz A, Thijssen JH, Blankenstein MA, Daroszewski

J. Concentration of sex steroids in adipose tissue after menopause.

Steroids 1998;63:319-21.

Buckley M, Goa K. Tamoxifen a reappraisal of its pharmacodynamic

and pharmacokinetic properties and therapeutic use. Drugs

;37:451-90.

Jordan VC, Collins MM, Rowsby L, Prestwich GJ. A monohydroxylated

metabolite of tamoxifen with potent antioestrogenic activity.

Endocrinol 1977;75:305-16.

Hiremath JG, Kusum DV, Kshama D, Domb AJ. Biodegradable

poly(sebacic acid-co-ricinoleic-ester anhydride) tamoxifen citrate

implants: Preparation and in vitro characterization. J App Polymer Sci

;107:2745-54.

Chawla SJ, Amiji MM. Biodegradable poly(epsilon-caprolactone)

nanoparticles for tumor targeted delivery of tamoxifen. Int J Pharm

;249:127-38.

Hiremath JG, Kusum DV. Preparation and in-vitro characterization of

paclitaxel loaded injectable microspheres. Asian J Pharm 2010;3:205-10.

Costa P, Sousa JM, Lobo S. Modeling and comparison of dissolution

profiles. Eur J Pharm Sci 2001;13:123-33.

Rothen-Weinhold A, Besseghir K, Vuaridel E, Sublet E, Oudry N, Kubel

F, et al. Injection molding versus extrusion as manufacturing technique

for the preparation of biodegradable implants. Eur J Pharm Biopharm

;48:113-21.

Costa P, Sousa JM, Lobo S. Modeling and comparison of dissolution

profiles. Eur J Pharm Sci 2001;13:123-33.

Ramchandhani M, Pankaskie M, Robinson D. The influence of

manufacturing procedure on the degradation of poly (lactide-co-

glycolide) 85:15 and 50:50 implants. J Control Release 1997;43:161-73.

Siepmann J, Siepmann F, Florence AT. Local controlled drug delivery

to the brain: Mathematical modeling of the underlying mass transport

mechanisms. Int J Pharm 2006;314:101-19.




DOI: http://dx.doi.org/10.22377/ajp.v5i1.78

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