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1.
Zhongguo Zhong Yao Za Zhi ; 49(10): 2689-2698, 2024 May.
Article in Chinese | MEDLINE | ID: mdl-38812169

ABSTRACT

This study aims to prepare co-loaded indocyanine green(ICG) and elemene(ELE) nano-emulsion(NE) in situ gel(ICG-ELE-NE-gel) and evaluate its physicochemical properties and antitumor activity in vitro. ICG-ELE-NE-gel was prepared by aqueous phase titration and cold solution methods, followed by characterization of the morphology, particle size, corrosion, and photothermal conversion characteristics. The human breast cancer MCF-7 cells were taken as the model, combined with 808 nm laser irradia-tion. Cell inhibition rate test and cell uptake test were performed. ICG-ELE-NE was spherical and uniform in size. The average particle size and Zeta potential were(85.61±0.35) nm and(-21.4±0.6) mV, respectively. The encapsulation efficiency and drug loading rate were 98.51%±0.39% and 10.96%±0.24%, respectively. ICG-ELE-NE-gel had a good photothermal conversion effect and good photothermal stability. The dissolution of ICG-ELE-NE-gel had both temperature and pH-responsive characteristics. Compared with free ELE, ICG-ELE-NE-gel combined with near-infrared light irradiation significantly enhanced the inhibitory effect on MCF-7 cells and could be uptaken in large amounts by MCF-7 cells. ICG-ELE-NE-gel was successfully prepared, and its antitumor activity was enhanced after 808 nm laser irradiation.


Subject(s)
Breast Neoplasms , Cell Proliferation , Emulsions , Indocyanine Green , Humans , Indocyanine Green/chemistry , MCF-7 Cells , Emulsions/chemistry , Cell Proliferation/drug effects , Female , Particle Size , Gels/chemistry , Nanoparticles/chemistry , Drug Compounding/methods , Drugs, Chinese Herbal/chemistry , Drugs, Chinese Herbal/pharmacology , Drug Carriers/chemistry
2.
J Huazhong Univ Sci Technolog Med Sci ; 37(3): 371-378, 2017 Jun.
Article in English | MEDLINE | ID: mdl-28585133

ABSTRACT

The therapeutic potential of curcumin (Cur) is hampered by its poor aqueous solubility and low bioavailability. The aim of this study was to determine whether Cur nanoemulsions enhance the efficacy of Cur against prostate cancer cells and increase the oral absorption of Cur. Cur nanoemulsions were developed using the self-microemulsifying method and characterized by their morphology, droplet size and zeta potential. The results showed that the cytotoxicity and cell uptake were considerably increased with Cur nanoemulsions compared to free Cur. Cur nanoemulsions exhibited a significantly prolonged biological activity and demonstrated better therapeutic efficacy than free Cur, as assessed by apoptosis and cell cycle studies. In situ single-pass perfusion studies demonstrated higher effective permeability coefficient and absorption rate constant for Cur nanoemulsions than for free Cur. Our study suggested that Cur nanoemulsions can be used as an effective drug delivery system to enhance the anticancer effect and oral bioavailability of Cur.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Curcumin/pharmacology , Intestinal Absorption/drug effects , Nanostructures/administration & dosage , Prostate/drug effects , Animals , Antineoplastic Agents, Phytogenic/pharmacokinetics , Apoptosis/drug effects , Caspase 3/genetics , Caspase 3/metabolism , Caspase 7/genetics , Caspase 7/metabolism , Cell Cycle/drug effects , Cell Cycle/genetics , Cell Line, Tumor , Cell Survival/drug effects , Curcumin/pharmacokinetics , Duodenum/drug effects , Duodenum/metabolism , Emulsions , Gene Expression , Glycerol/chemistry , Humans , Ileum/drug effects , Ileum/metabolism , Jejunum/drug effects , Jejunum/metabolism , Male , Nanostructures/chemistry , Particle Size , Polyethylene Glycols/chemistry , Prostate/metabolism , Prostate/pathology , Rats , Rats, Wistar , Surface-Active Agents/chemistry
3.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-333491

ABSTRACT

The therapeutic potential of curcumin (Cur) is hampered by its poor aqueous solubility and low bioavailability.The aim of this study was to determine whether Cur nanoemulsions enhance the efficacy of Cur against prostate cancer cells and increase the oral absorption of Cur.Cur nanoemulsions were developed using the self-microemulsifying method and characterized by their morphology,droplet size and zeta potential.The results showed that the cytotoxicity and cell uptake were considerably increased with Cur nanoemulsions compared to free Cur.Cur nanoemulsions exhibited a significantly prolonged biological activity and demonstrated better therapeutic efficacy than free Cur,as assessed by apoptosis and cell cycle studies.In siru single-pass perfusion studies demonstrated higher effective permeability coefficient and absorption rate constant for Cur nanoemulsions than for free Cur.Our study suggested that Cur nanoemulsions can be used as an effective drug delivery system to enhance the anticancer effect and oral bioavailability of Cur.

4.
Molecules ; 20(6): 9671-85, 2015 May 26.
Article in English | MEDLINE | ID: mdl-26016553

ABSTRACT

In the present work, a quantitative 1H Nuclear Magnetic Resonance (qHNMR) was established for purity assessment of six aryltetralin lactone lignans. The validation of the method was carried out, including specificity, selectivity, linearity, accuracy, precision, and robustness. Several experimental parameters were optimized, including relaxation delay (D1), scan numbers (NS), and pulse angle. 1,4-Dinitrobenzene was used as internal standard (IS), and deuterated dimethyl sulfoxide (DMSO-d6) as the NMR solvent. The purities were calculated by the area ratios of H-2,6 from target analytes vs. aromatic protons from IS. Six aryltetralin lactone lignans (deoxypodophyllotoxin, podophyllotoxin, 4-demethylpodophyllotoxin, podophyllotoxin-7'-O-ß-d-glucopyranoside, 4-demethylpodophyllotoxin-7'-O-ß-d-glucopyranoside, and 6''-acetyl-podophyllotoxin-7'-O-ß -d-glucopyranoside) were analyzed. The analytic results of qHNMR were further validated by high performance liquid chromatography (HPLC). Therefore, the qHNMR method was a rapid, accurate, reliable tool for monitoring the purity of aryltetralin lactone lignans.


Subject(s)
Lactones/analysis , Lignans/analysis , Podophyllotoxin/analogs & derivatives , Podophyllotoxin/analysis , Chromatography, High Pressure Liquid , Dinitrobenzenes/analysis , Drugs, Chinese Herbal , Proton Magnetic Resonance Spectroscopy , Reference Standards
5.
Zhong Yao Cai ; 36(3): 468-71, 2013 Mar.
Article in Chinese | MEDLINE | ID: mdl-24010331

ABSTRACT

OBJECTIVE: To optimize the prescription and technique for preparing saikoside (SS) liposomes and evaluate its quality. METHODS: The preparation methods of liposomes included film dispersion, ether injection, reverse phase evaporation and pH gradients were explored. The encapsulation ratio was determined by macroreticular resin method. The main factors affecting encapsulation ratio were studied by single factor analysis and central composite design. RESULTS: The appearance of SS liposomes prepared by optimized method was satisfactory. The encapsulation ratio was more than 60% and the verage particle size of SS liposomes was 110 nm. CONCLUSION: The formulation and preparation process is practical and simple for the preparation of SS liposomes. It is valuable to be further studied.


Subject(s)
Bupleurum/chemistry , Liposomes/chemistry , Oleanolic Acid/analogs & derivatives , Phospholipids/administration & dosage , Saponins/administration & dosage , Cholesterol/administration & dosage , Cholesterol/chemistry , Citric Acid/chemistry , Drug Carriers/chemistry , Oleanolic Acid/administration & dosage , Oleanolic Acid/chemistry , Particle Size , Phospholipids/chemistry , Plant Roots/chemistry , Resins, Synthetic , Saponins/chemistry
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