Usnic acid-loaded nanocapsules: an evaluation of cytotoxicity

被引:22
作者
Santos, N [1 ]
Nascimento, SC [1 ]
Silva, JF [1 ]
Pereira, ECG [1 ]
Silva, NH [1 ]
Honda, NK [1 ]
Santos-Magalhaes, NS [1 ]
机构
[1] Univ Fed Pernambuco, Lab Imunopatol Keizo Asami, BR-50670901 Recife, PE, Brazil
关键词
nanocapsules; PLGA; usnic acid; Lichen; Cladonia substellata; cytotoxicity; NCI-H; 292; cells;
D O I
10.1016/S1773-2247(05)50065-0
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The aim of the present study is the design of nanocapsules containing usnic acid (UA-NC) and the evaluation of their physicochemical properties, in vitro kinetic profile and cytotoxic effect on human lung carcinoma cells. The usnic acid was encapsulated into nanocapsules prepared with a copolymer of lactic and glycolic acid using an interfacial deposition of a preformed polymer on oil-in-water emulsion. The cytotoxicity of nanocapsules was evaluated by the MTT method. UA-NC were obtained with a mean diameter of 324 +/- 88 nm. An encapsulation ratio of 99.4 0.16% was attained at an usnic acid concentration of 1 mu g/ml. An usnic acid release of 78.3% from nanocapsules within 48 h was achieved. Concentrations required to inhibit 50% of cell growth were 10.0 and 11.5 mu g/ml for free and encapsulated usnic acid, respectively. In conclusion, usnic acid was, for the first time, efficiently encapsulated into PLGA nanocapsules, providing a suitable dosage form for introducing usnic acid in in vivo studies, the use of which has been limited by its poor solubility and toxic properties.
引用
收藏
页码:355 / 361
页数:7
相关论文
共 26 条
[11]   Paclitaxel-loaded PLGA nanoparticles: preparation, physicochemical characterization and in vitro anti-tumoral activity [J].
Fonseca, C ;
Simoes, S ;
Gaspar, R .
JOURNAL OF CONTROLLED RELEASE, 2002, 83 (02) :273-286
[12]  
Guterres S. S., 1995, PHARM RES, V12, P1
[13]  
HANS ML, 2002, CURR OPIN SOLID ST M, V1, P212
[14]   Usnic acid [J].
Ingólfsdóttir, K .
PHYTOCHEMISTRY, 2002, 61 (07) :729-736
[15]   PREPARATION OF POLY(D,L-LACTIDE GLYCOLIDE) NANOPARTICLES OF CONTROLLED PARTICLE-SIZE DISTRIBUTION - APPLICATION OF EXPERIMENTAL-DESIGNS [J].
JULIENNE, MC ;
ALONSO, MJ ;
AMOZA, JLG ;
BENOIT, JP .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1992, 18 (10) :1063-1077
[16]  
KRISTMUNDSTOTTI, 2002, J PHARM PHARMACOL, V54, P215
[17]   Lichen metabolites.: 2.: Antiproliferative and cytotoxic activity of gyrophoric, usnic, and diffractaic acid on human keratinocyte growth [J].
Kumar, S ;
Müller, K .
JOURNAL OF NATURAL PRODUCTS, 1999, 62 (06) :821-823
[18]  
LOVELAND BE, 1992, BIOCHEM INT, V27, P501
[19]   A method for the preparation of polymeric nanocapsules without stabilizer [J].
Lu, Z ;
Bei, JZ ;
Wang, SG .
JOURNAL OF CONTROLLED RELEASE, 1999, 61 (1-2) :107-112
[20]  
Magenheim B., 1991, STP PHARMA SCI, V1, P221