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Design and evaluation of self-nanoemulsifying drug delivery system of flutamide.

Jeevana JB, Sreelakshmi K - J Young Pharm (2011)

Bottom Line: Sesame oil was selected as an oil phase, Tween 20 as surfactant, and PEG400 as cosurfactant due to their higher solubilization effect.The mean particle size of the SNEDDS was 148.7 nm and percent drug content was 99.66.The dissolution rate of FLT from SNEDDS was faster and higher in three different dissolution media such as 2% sodium lauryl sulfate (97.85%), simulated gastric fluid (0.1 N HCl containing 0.5% Tween 20) (95.71%), and simulated intestinal fluid (pH 6.8 buffer) (96.21%).

View Article: PubMed Central - PubMed

Affiliation: Institute of Pharmaceutical Technology, Sri Padmavathi Mahila Viswavidyalayam (Women's University), Tirupati, Andhra Pradesh - 517 502, India.

ABSTRACT
Flutamide (FLT) is an antiandrogen drug for the treatment of prostate cancer. It has the drawback of poor water solubility and needs enhancement of its dissolution rate in simulated gastric fluids. Hence, it is prepared as self-nanoemulsifying drug delivery systems (SNEDDS) with an aim to enhance its dissolution rate. The objectives of the study are to develop SNEDDS of FLT and to characterize for particle size, self-nanoemulsification, and dissolution enhancement. Solubility of FLT was determined in various oils, surfactants, and cosurfactants. Sesame oil was selected as an oil phase, Tween 20 as surfactant, and PEG400 as cosurfactant due to their higher solubilization effect. Various formulations were prepared by simple mixing followed by vortexing. From studies, the optimized SNEDDS formulation was composed of FLT (8.04% w/w), sesame oil (24.12% w/w), Tween 20 (53.38% w/w), and PEG400 (14.46% w/w). The selected SNEDDS could be self-emulsified without precipitation upon simple mixing. The mean particle size of the SNEDDS was 148.7 nm and percent drug content was 99.66. The dissolution rate of FLT from SNEDDS was faster and higher in three different dissolution media such as 2% sodium lauryl sulfate (97.85%), simulated gastric fluid (0.1 N HCl containing 0.5% Tween 20) (95.71%), and simulated intestinal fluid (pH 6.8 buffer) (96.21%).

No MeSH data available.


Related in: MedlinePlus

Comparative results of drug release from plain FLT and the SNEDDS formulation in different dissolution media. FLT, Plain flutamide; SNEDDS, self-nanoemulsifying drug delivery system
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Figure 0002: Comparative results of drug release from plain FLT and the SNEDDS formulation in different dissolution media. FLT, Plain flutamide; SNEDDS, self-nanoemulsifying drug delivery system

Mentions: To understand the characteristics of drug release from SNEDDs, an in vitro release study was carried out for pure drug and SNEDDs of FLT in different dissolution media such as 2% sodium lauryl sulfate, simulated gastric fluid (0.1 N HCl containing 0.5% of Tween 20), and simulated intestinal fluid (pH 6.8 buffer). The dissolution profiles of pure drug and SNEDDS formulation are shown in Figure 2. As evident from the drug release profiles, the pure drug evidenced meager solubility of 27.48% in 60 min in 2% SLS, 20.7% in 0.1 N HCl containing 0.5% of Tween 20 and 20.94% in pH 6.8 buffer. The drug release from SNEDDS was markedly high such that 97.85% in 2% sodium lauryl sulfate, 95.71% in simulated gastric fluid (0.1 N HCl containing 0.5% of Tween 20) and 96.21% in simulated intestinal fluid (pH 6.8 buffer). The results indicate instantaneous and remarkably high dissolution of FLT in all three media compared to the pure drug. This higher and faster dissolution rate of FLT from SNEDDS is expected due to the nanoparticle size range of the particles offering higher interfacial area required for dissolution.


Design and evaluation of self-nanoemulsifying drug delivery system of flutamide.

Jeevana JB, Sreelakshmi K - J Young Pharm (2011)

Comparative results of drug release from plain FLT and the SNEDDS formulation in different dissolution media. FLT, Plain flutamide; SNEDDS, self-nanoemulsifying drug delivery system
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3094558&req=5

Figure 0002: Comparative results of drug release from plain FLT and the SNEDDS formulation in different dissolution media. FLT, Plain flutamide; SNEDDS, self-nanoemulsifying drug delivery system
Mentions: To understand the characteristics of drug release from SNEDDs, an in vitro release study was carried out for pure drug and SNEDDs of FLT in different dissolution media such as 2% sodium lauryl sulfate, simulated gastric fluid (0.1 N HCl containing 0.5% of Tween 20), and simulated intestinal fluid (pH 6.8 buffer). The dissolution profiles of pure drug and SNEDDS formulation are shown in Figure 2. As evident from the drug release profiles, the pure drug evidenced meager solubility of 27.48% in 60 min in 2% SLS, 20.7% in 0.1 N HCl containing 0.5% of Tween 20 and 20.94% in pH 6.8 buffer. The drug release from SNEDDS was markedly high such that 97.85% in 2% sodium lauryl sulfate, 95.71% in simulated gastric fluid (0.1 N HCl containing 0.5% of Tween 20) and 96.21% in simulated intestinal fluid (pH 6.8 buffer). The results indicate instantaneous and remarkably high dissolution of FLT in all three media compared to the pure drug. This higher and faster dissolution rate of FLT from SNEDDS is expected due to the nanoparticle size range of the particles offering higher interfacial area required for dissolution.

Bottom Line: Sesame oil was selected as an oil phase, Tween 20 as surfactant, and PEG400 as cosurfactant due to their higher solubilization effect.The mean particle size of the SNEDDS was 148.7 nm and percent drug content was 99.66.The dissolution rate of FLT from SNEDDS was faster and higher in three different dissolution media such as 2% sodium lauryl sulfate (97.85%), simulated gastric fluid (0.1 N HCl containing 0.5% Tween 20) (95.71%), and simulated intestinal fluid (pH 6.8 buffer) (96.21%).

View Article: PubMed Central - PubMed

Affiliation: Institute of Pharmaceutical Technology, Sri Padmavathi Mahila Viswavidyalayam (Women's University), Tirupati, Andhra Pradesh - 517 502, India.

ABSTRACT
Flutamide (FLT) is an antiandrogen drug for the treatment of prostate cancer. It has the drawback of poor water solubility and needs enhancement of its dissolution rate in simulated gastric fluids. Hence, it is prepared as self-nanoemulsifying drug delivery systems (SNEDDS) with an aim to enhance its dissolution rate. The objectives of the study are to develop SNEDDS of FLT and to characterize for particle size, self-nanoemulsification, and dissolution enhancement. Solubility of FLT was determined in various oils, surfactants, and cosurfactants. Sesame oil was selected as an oil phase, Tween 20 as surfactant, and PEG400 as cosurfactant due to their higher solubilization effect. Various formulations were prepared by simple mixing followed by vortexing. From studies, the optimized SNEDDS formulation was composed of FLT (8.04% w/w), sesame oil (24.12% w/w), Tween 20 (53.38% w/w), and PEG400 (14.46% w/w). The selected SNEDDS could be self-emulsified without precipitation upon simple mixing. The mean particle size of the SNEDDS was 148.7 nm and percent drug content was 99.66. The dissolution rate of FLT from SNEDDS was faster and higher in three different dissolution media such as 2% sodium lauryl sulfate (97.85%), simulated gastric fluid (0.1 N HCl containing 0.5% Tween 20) (95.71%), and simulated intestinal fluid (pH 6.8 buffer) (96.21%).

No MeSH data available.


Related in: MedlinePlus