Binary Micellar Solutions of Poly(Ethylene Oxide)-Poly(Styrene Oxide) Copolymers with Pluronic® P123: Drug Solubilisation and Cytotoxicity Studies

被引:11
|
作者
Oliveira, Samira A. [1 ]
Moura, Carolina L. [1 ]
Cavalcante, Igor M. [1 ]
Lopes, Amanda Araujo [2 ]
Leal, Luzia K. A. M. [2 ]
Gramosa, Nilce V. [1 ]
Ribeiro, Maria E. N. P. [1 ]
Franca, Francisco C. F. [3 ]
Yeates, Stephen G. [4 ]
Ricardo, Nagila M. P. S. [1 ]
机构
[1] Univ Fed Ceara, Dept Quim Organ & Inorgan, Lab Polimeros & Inovacao Mat LABPIM, BR-60451970 Fortaleza, Ceara, Brazil
[2] Univ Fed Ceara, Dept Farm, Ctr Estudos Farmaceut & Cosmet CEFAC, BR-60430160 Fortaleza, Ceara, Brazil
[3] Univ Estadual Ceara, Fac Educ Ciencias & Letras Sertao Cent, BR-63900000 Quixada, Ceara, Brazil
[4] Univ Manchester, Sch Chem, Manchester M13 9PL, Lancs, England
关键词
solubilisation capacity; binary micelles; griseofulvin; citotoxicity; AMPHIPHILIC BLOCK-COPOLYMERS; IN-VITRO EVALUATION; AQUEOUS-SOLUTION; TRIBLOCK COPOLYMERS; ETHYLENE-OXIDE; ORAL BIOAVAILABILITY; DIBLOCK COPOLYMERS; STYRENE OXIDE; DELIVERY; GRISEOFULVIN;
D O I
10.5935/0103-5053.20150205
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The non-commercial copolymers E45S8, E45S17 and their mixtures with Pluronic (R) P123 (E21P67E21) were studied as carriers of the model drug griseofulvin. Critical micelle concentration (cmc) (dye solubilisation method), drug solubilisation capacity (S-cp and S-h) determined by ultraviolet-visible (UV-Vis) spectroscopy and H-1 nuclear magnetic resonance (H-1 NMR) and cytotoxicity (LDH activity in human neutrophils) were studied. E45S17 1.0 wt.% dispersions presented colloidal aggregates limiting its S-cp in comparison to E45S8, but in 0.1 wt.% solutions this phenomenon seemed to be absent and E45S17 presented a higher S-cp. The mixtures that showed the best S-cp results contained 50% of P123 and presented low cmc. An evaluation of literature data suggested a minimum E-m content of 62% in EmSn copolymers below which the increase of S-n length does not lead to an increase of S-h. The results suggested no toxicity of the copolymers on human neutrophils, supporting the use of P123 and poly(styrene oxide) containing copolymers as drug carriers.
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页码:2195 / 2204
页数:10
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