RESUMO
Curcumin is one of the most versatile compounds obtained from Curcuma longa. The major obstacle in the therapeutic use of curcumin is its aqueous solubility. To enhance its aqueous solubility and biological activities, we prepared curcumin nanospheres (CNSs) by wet milling-solvent evaporation technique without any surfactants. In this study, we have focused on the synthesis, characterization and biological effects of CNSs. DLS and SEM analyses showed 50-80 nm spherical shaped CNSs with a zeta potential of -31.65 mV. FTIR revealed that there were no structural changes to CNSs. Antibacterial and antifungal studies proved that CNSs were much more effective than curcumin against Escherichia coil, Staphylococcus aureus and Candida albicans. Antioxidant activity of CNSs showed promising result for therapeutic applications. The in vitro anti-inflammatory studies proved that CNSs possessed enhanced anti-inflammatory effect against protein denaturation. Cytotoxicity and uptake of CNSs showed more toxicity on cancer cells (T47D, MG63, A375) sparing normal HDF and IEC cell lines. Skin permeation studies showed CNSs retained at different layers of pig skin. These results give clear evidence for their use against microbial and fungal skin infections as well as cancer treatment.
Assuntos
Curcumina/síntese química , Curcumina/farmacologia , Nanosferas/química , Animais , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Bactérias/efeitos dos fármacos , Bactérias/crescimento & desenvolvimento , Coagulação Sanguínea/efeitos dos fármacos , Morte Celular/efeitos dos fármacos , Linhagem Celular , Contagem de Colônia Microbiana , Curcumina/química , Análise Diferencial Térmica , Fungos/efeitos dos fármacos , Fungos/crescimento & desenvolvimento , Humanos , Técnicas In Vitro , Teste de Materiais , Testes de Sensibilidade Microbiana , Nanosferas/ultraestrutura , Tamanho da Partícula , Permeabilidade/efeitos dos fármacos , Pele/efeitos dos fármacos , Pele/microbiologia , Espectroscopia de Infravermelho com Transformada de Fourier , Eletricidade Estática , Sus scrofa , Termogravimetria , Difração de Raios XRESUMO
Hepatic carcinoma (HCC) is one of the most common cancer and its treatment has been considered a therapeutic challenge. Doxorubicin (Dox) is one of the most important chemotherapeutic agents used in the treatment for liver cancer. However, the efficacy of Dox therapy is restricted by the dose-dependent toxic side effects. To overcome the cardiotoxicity of Dox as well as the current problems of conventional modality treatment of HCC, we developed a locally injectable, biodegradable, and pH sensitive composite nanogels for site specific delivery. Both control and Dox loaded composite nanogel systems were analyzed by DLS, SEM, FTIR and TG/DTA. The size ranges of the control composite nanogels and their drug loaded counterparts were found to be 90±20 and 270±20 nm, respectively. The control chitin-PLA CNGs and Dox-chitin-PLA CNGs showed higher swelling and degradation in acidic pH. Drug entrapment efficiency and in vitro drug release studies were carried out and showed a higher drug release at acidic pH compared to neutral pH. Cellular internalization of the nanogel systems was confirmed by fluorescent microscopy. The cytotoxicity of the composite nanogels was analyzed toward HepG2 (human liver cancer) cell lines. Furthermore, the results of in vitro hemolytic assay and coagulation assay substantiate the blood compatibility of the system. Overall Dox-chitin-PLA CNGs system could be a promising anticancer drug delivery system for liver cancer therapy.
Assuntos
Quitina/química , Doxorrubicina/química , Ácido Láctico/química , Neoplasias Hepáticas , Polietilenoglicóis/química , Polietilenoimina/química , Polímeros/química , Sobrevivência Celular/efeitos dos fármacos , Doxorrubicina/farmacologia , Hemólise/efeitos dos fármacos , Células Hep G2 , Humanos , Nanogéis , Nanomedicina/métodos , PoliésteresRESUMO
In this work, we developed a pH responsive chitin-poly(caprolactone) composite nanogels (chitin-PCL CNGs) system for non-small cell lung cancer (NSCLC). A hydrophilic drug, doxorubicin (Dox) was loaded in Chitin-PCL CNGs (Dox-chitin-PCL CNGs). Both control and drug loaded systems were analyzed by DLS, SEM, FTIR and TG/DTA. The size ranges of the control composite nanogels and their drug loaded counterparts were found to be 70 ± 20 and 240 ± 20 nm, respectively. The control chitin-PCL CNGs and Dox-chitin-PCL CNGs showed higher swelling and degradation in acidic pH. Drug entrapment efficiency and in-vitro drug release studies were carried out and showed a higher drug release at acidic pH compared to neutral pH. Cellular internalization of the nanogel systems was confirmed by fluorescent microscopy. Dox-Chitin-PCL CNGs showed dose dependent cytotoxicity toward A549 (adenocarcinomic human alveolar basal epithelial cells) cancer cells. Furthermore, the results of in-vitro hemolytic assay and coagulation assay substantiate the blood compatibility of the system. These results indicate that chitin-PCL CNGs is a novel carrier for delivery of anticancer drugs.
