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1.
Zhongguo Zhong Yao Za Zhi ; 40(15): 2982-7, 2015 Aug.
Artigo em Zh | MEDLINE | ID: mdl-26677697

RESUMO

To develop an ophthalmic preparation of Shedan, an in situ forming gel was prepared with the formulation containing 18% of poloxamer 407 and 5% of poloxamer 188 by response surface designs plus central composite designs. The rheology results showed that LVE range gamma should limited within 0.5%, Shedan high-frequency region, and the thixotropy recovery time is less than 5 seconds. The phase transition temperature was 33.25 °C according to curve of storage modulus and loss modulus determined by temperature scanning. Surface tension and osmometer of it determined by surface tension meter and dew point osmometer were 36.43 mN · m(-1), and 320.6 mOsm · kg(-1), respectively. Fluorescein sodium was selected as the marker to monitor the corneal residence time, and the results showed that Shedan gel could prolong drug residence for 180 min. In line with zero-order kinetics, releases of muscone and salvianolic acid B in vitro depends on gels erosion. The results of rabbit ocular irritation experiments suggested that Shedan in situ forming gel was biocompatible and nonirritant. In conclusion, a novel Shedan in situ forming gel was developed and characterized for potential drug treatment of retinal vein occlusion.


Assuntos
Cicloparafinas/química , Poloxâmero/química , Animais , Benzofuranos/química , Feminino , Géis/química , Masculino , Soluções Oftálmicas , Coelhos , Oclusão da Veia Retiniana/tratamento farmacológico , Viscosidade
2.
Zhongguo Zhong Yao Za Zhi ; 35(19): 2546-50, 2010 Oct.
Artigo em Zh | MEDLINE | ID: mdl-21174762

RESUMO

OBJECTIVE: To study the preparation of cantharidin entrapped non-ionic surfactant vesicle (noisome)and evaluate its quality. METHOD: The niosome loaded with cantharidin was prepared using injection method by non-ionic surfactants as the carrier. An centrifugation separation method and HPLC analysis method of the cantharidin were established to detect the entrapment efficiency. The optimum preparation technology was established by a orthogonal experiment. The morphology, and particle size were studied to evaluate the preparation. RESULT: The average size of niosomes were (209. 8 +/- 0.5) nm. The entrapment efficiency of the CTD-NS was (27.5% +/- 2.0%) and Zeta potential was (41.5 +/- 0.65) mV. CONCLUSION: The preparation of cantharidin noisome by TweenA and SpanB is practicable and successful. These experiments can be the basement of developing targeting drug delivery system.


Assuntos
Cantaridina/administração & dosagem , Sistemas de Liberação de Medicamentos , Lipossomos/química , Tensoativos/administração & dosagem , Cantaridina/química , Cantaridina/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Lipossomos/administração & dosagem , Tamanho da Partícula
3.
Int J Nanomedicine ; 15: 1771-1786, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32214810

RESUMO

PURPOSE: In this study, pH-sensitive poly(2-ethyl-2-oxazoline)-poly(lactic acid)-poly(ß-amino ester) (PEOz-PLA-PBAE) triblock copolymers were synthesized and were conjugated with an antimalaria drug artesunate (ART), for inhibition of a colon cancer xenograft model. METHODS: The as-prepared polymer prodrugs are tended to self-assemble into polymeric micelles in aqueous milieu, with PEOz segment as hydrophilic shell and PLA-PBAE segment as hydrophobic core. RESULTS: The pH sensitivity of the as-prepared copolymers was confirmed by acid-base titration with pKb values around 6.5. The drug-conjugated polymer micelles showed high stability for at least 96 h in PBS and 37°C, respectively. The as-prepared copolymer prodrugs showed high drug loading content, with 9.57%±1.24% of drug loading for PEOz-PLA-PBAE-ART4. The conjugated ART could be released in a sustained and pH-dependent manner, with 92% of released drug at pH 6.0 and 57% of drug released at pH 7.4, respectively. In addition, in vitro experiments showed higher inhibitory effect of the prodrugs on rodent CT-26 cells than that of free ART. Animal studies also demonstrated the enhanced inhibitory efficacy of PEOz-PLA-PBAE-ART2 micelles on the growth of rodent xenograft tumor. CONCLUSION: The pH-responsive artesunate polymer prodrugs are promising candidates for colon cancer adjuvant therapy.


Assuntos
Artesunato/farmacocinética , Neoplasias do Colo/tratamento farmacológico , Polímeros/química , Pró-Fármacos/química , Pró-Fármacos/farmacologia , Animais , Artesunato/química , Neoplasias do Colo/patologia , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Feminino , Humanos , Concentração de Íons de Hidrogênio , Interações Hidrofóbicas e Hidrofílicas , Camundongos Endogâmicos BALB C , Micelas , Oxazóis/química , Ensaios Antitumorais Modelo de Xenoenxerto
4.
Zhongguo Zhong Yao Za Zhi ; 32(8): 683-7, 2007 Apr.
Artigo em Zh | MEDLINE | ID: mdl-17608219

RESUMO

OBJECTIVE: To prepare tuizhang gel to cure cataract, the characteristics of Tuizhang gel on the drug-releasing in vitro were evaluated by compared with Tuizhang oculentum. METHOD: The emodin and chrysophanol in the releasing mediator were determined by HPLC, and the drug releasing characteristics of Tuizhang gel and Tuizhang oculentum were studied by bag filter method. RESULT: The emodin and chrysophanol in Tuizhang gel released (98.3, 1.1)%, (95.8, 1.8)% within 24 hours, respectively, while those in tuizhang oculentum released (10.62, 0.7)%, (10.46, 0.4)%, respectively. The emodin and chrysophanol in Tuizhang gel released more quickly and completely than in Tuizhang oculentum, so Tuizhang gel has enhanced the bioavailability. CONCLUSION: The Tuizhang gel is characterized by slow-release to some degree, and it shows a promising future on ophthalmic drug delivery.


Assuntos
Preparações de Ação Retardada/farmacocinética , Medicamentos de Ervas Chinesas/farmacologia , Plantas Medicinais/química , Tecnologia Farmacêutica/métodos , Resinas Acrílicas/química , Antraquinonas/química , Antraquinonas/farmacocinética , Preparações de Ação Retardada/química , Medicamentos de Ervas Chinesas/química , Emodina/química , Emodina/farmacocinética , Géis , Pomadas , Solubilidade
5.
J Pharm Sci ; 105(9): 2752-2759, 2016 09.
Artigo em Inglês | MEDLINE | ID: mdl-27041413

RESUMO

This study aimed to design a nanocarrier ophthalmic delivery system of muscone, a poorly water-soluble drug. The muscone thermoresponsive nanogels were self-assembled by reverse micelle → positive micelle method. Muscone was demonstrated to have uniform narrow particle size distribution in nanogel by the dynamic light scattering test. The developed nanocomposite hydrogel had a high muscone loading, and the rheology results showed that the phase transition temperature was 34.05°C. Thixotropy test indicated that the nanogel was able to resist the blinking of eyes because of the thixotropy recovery time, which is <5 s. Compared with muscone eye drops, muscone nanogels showed longer retention time on the corneal surface using fluorescent labeling technology and produced a 3.4-fold increase in apparent permeability coefficients (Papp). Draize testing showed that the developed nanogel caused no eye irritation. In vivo pharmacokinetic study indicated that the nanogel could significantly increase the bioavailability of muscone after administration compared with eye drops. These results indicate that self-assembled thermoresponsive nanogel prepared by reverse micelle → positive micelle method has potential for the ophthalmic delivery of poorly water-soluble drugs.


Assuntos
Administração Oftálmica , Cicloparafinas/administração & dosagem , Cicloparafinas/farmacocinética , Sistemas de Liberação de Medicamentos , Polietilenoglicóis/química , Polietilenoimina/química , Animais , Disponibilidade Biológica , Piscadela , Córnea/metabolismo , Irritantes , Micelas , Nanogéis , Soluções Oftálmicas , Tamanho da Partícula , Coelhos , Reologia , Temperatura , Termodinâmica
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