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1.
Eur J Pharm Sci ; 47(1): 265-72, 2012 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-22525435

RESUMO

This work evaluates intercalation of tamoxifen (Tmx) in interlayer gallery of Na(+)-MMT (Montmorillonite, MMT) (Tmx-MMT), which is further compounded with poly-(ε-caprolactone) (PCL) (Tmx-MMT/PCL, MPs), for oral chemotherapy of breast cancer. The X-ray diffraction patterns, thermal and spectroscopic analyses indicated the intercalation of Tmx into the MMT interlayer that stabilized in the longitudinal monolayer mode by electrostatic interaction. No significant change in structural and functional properties of Tmx was found in the MMT layers. In vitro study of drug release profiles showed controlled release pattern. The genotoxic effect of drug was in vitro evaluated in human lymphocyte cell culture by comet assay, and results indicated moderate reduction in DNA damage when pristine Tmx was intercalated with MMT and formulated in composites. The Tmx-MMT hybrid efficacy was also confirmed on HeLa and A549 cancer cells by in vitro cell viability assay. In vivo pharmacokinetics (PK) of formulated Tmx in rats was examined and the results showed that plasma Tmx levels were within therapeutic window as compared to pristine Tmx. Therefore, Tmx-MMT hybrid and microcomposite particles (MPs) can be of considerable value in chemotherapy of malignant neoplastic disease with reduced side effects. This study clearly indicated that MMT not only plays a role as a delivery matrix for drug, but also facilitates significant increase in the delivery proficiency.


Assuntos
Antineoplásicos/administração & dosagem , Antineoplásicos/química , Bentonita/química , Portadores de Fármacos/química , Poliésteres/química , Animais , Antineoplásicos/farmacocinética , Bentonita/administração & dosagem , Neoplasias da Mama/tratamento farmacológico , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Dano ao DNA/efeitos dos fármacos , Preparações de Ação Retardada , Portadores de Fármacos/administração & dosagem , Feminino , Células HeLa , Humanos , Linfócitos/efeitos dos fármacos , Poliésteres/administração & dosagem , Ratos , Ratos Wistar , Sódio/química , Tamoxifeno/administração & dosagem , Tamoxifeno/química , Tamoxifeno/farmacocinética , Difração de Raios X/métodos
2.
J Biomater Appl ; 25(2): 161-77, 2010 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-19737810

RESUMO

Sustained intestinal delivery of thiamine hydrochloride (Vitamin B(1); VB(1)) and pyridoxine hydrochloride (Vitamin B(6); VB(6)) seems to be a feasible alternative to existing therapy. The vitamins (VB(1)/VB(6)) intercalated in montmorillonite (MMT) and intercalated VB(1)/VB(6)-MMT hybrid is further used for synthesis of VB(1)/VB(6)-MMT-alginate nanocomposite beads by gelation method and in vitro release in the intestinal environment. The structure and surface morphology of the synthesized VB(1)/VB(6)-MMT hybrid, VB(1)/VB(6)-alginate and VB(1)/VB(6)-MMT-alginate nanocomposite beads were characterized by XRD, FT-IR, TGA and SEM. In vitro release experiments revealed that the VB(1)/VB(6) releases suddenly from VB(1)/VB(6)-MMT hybrid and is pH dependent. The controlled release of VB(1)/VB(6) from VB(1)/VB(6)-MMT-alginate nanocomposite beads was observed to be controlled as compared to their release from VB(1)/VB(6)-MMT hybrid and VB(1)/VB(6)-alginate beads.


Assuntos
Alginatos , Bentonita , Nanocompostos , Tiamina/administração & dosagem , Vitamina B 6/administração & dosagem , Portadores de Fármacos , Ácido Glucurônico , Ácidos Hexurônicos , Concentração de Íons de Hidrogênio , Técnicas In Vitro , Microscopia Eletrônica de Varredura , Espectroscopia de Infravermelho com Transformada de Fourier , Termogravimetria , Difração de Raios X
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