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Study on Ascorbyl Palmitate Vesicles and Solid Lipid Nanoparticles as Transdermal Administration Carrier for Tretinoin

Author: ChenZhengMing
Tutor: LongXiaoYing
School: Guangdong College of Pharmacy
Course: Pharmacy
Keywords: Victoria A acid Vesicles Solid Lipid Nanoparticles
CLC: R94
Type: Master's thesis
Year: 2008
Downloads: 279
Quote: 1
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Abstract

Objective: dimension A acid vitamin C palmitate bubble capsule and solid lipid nanoparticles as transdermal drug delivery carrier, its prescription, preparation technology, encapsulation efficiency, stability, release and in vitro skin permeability and skin storing research. Expectations by these two new particulate drug delivery systems for the topical administration of the skin, improve the stability of the dimension A acid, while allowing more of the drug reserving within the skin in order to increase local drug concentration to reduce the system to absorb. Method: (1) preparation of dimension A acid vitamin C palmitate bubble capsule and solid lipid nanoparticles. By solvent injection Prepared dimension A acid vitamin C palmitate vesicles and formulation optimization using dialysis method for the determination of encapsulation efficiency. The prepared nanoemulsion-dimensional A acid solid lipid nanoparticles composed of glucan G50 micro gel entrapment efficiency was determined by the phase diagram to determine the prescription. (2) the stability of the dimension A acid vitamin C palmitate bubble capsule and solid lipid nanoparticles. Stability studies examine the dimension A acid vitamin C palmitate bubble capsule and solid lipid nanoparticle drug degradation under illumination (4500 ± 500 lx); indicators of drug content and encapsulation efficiency was examined vesicles 4 ℃ and 25 ° C, 75% relative humidity, storage stability of 6 months; drug content, particle size, indicators of potential and encapsulation efficiency was examined solid lipid nanoparticles at 4 ℃, 25 ℃ and 40 ℃ relative humidity of 75%, the stability of storage of 3 months. (3) dimension A acid vitamin C palmitate bubble capsule and solid lipid nanoparticles in vitro release and skin penetration and skin retention. Victoria A acid release from the carrier speed is measured with a Franz diffusion cell. Diffusion cell between the supply pool cellulose membrane (molecular weight of 8000 to 14000), the diffusion cell an area of ??2.92cm2. The timing sampling 0.5 ml of 2,4,6,8,12,24 h, and added the same amount of fresh medium sample treatment was determined by HPLC. Alternative semipermeable membrane in vitro percutaneous penetration test with the release, with the back skin of mice, rats, or rabbits. Reserving skin after the end of the in vitro skin permeation test, remove the skin, minced homogenizer, with 50% isopropanol - saline extract, after treatment of the extract was determined by HPLC drug concentration. Results: (1)-dimensional A acid vitamin C palmitate vesicles to optimize the prescription and craft. Take 0.1g L-cysteine ??hydrochloride salt and 0.05g EDTANa2, dissolved in 100ml PBS (pH 5.5), and then take as phase Ⅰ; 0.1g dimension A acid, 2.1g vitamin C palmitate, 1.9g cholesterol and Ⅰ phase 0.02g 2,6 - di-tert-butyl-methyl phenol plus 25ml ethanol - ether (3:2) is completely dissolved, as the phase Ⅱ; 1000r · min-1 stirring phase Ⅱ slowly drops to 60 ° C. in; after completion of the dropwise addition, continue incubation at 60 ℃ stirred for 30min, removal of organic solvent, and then heating was stopped and stirring continued for 30min. Control the final volume of 100 ml is, too. Dialysis method for the determination of its encapsulation efficiency gt; 90%. 4 ℃ storage content of 6 months no significant changes, the encapsulation efficiency decreased slightly; 25 ° C storage of six months content and the encapsulation efficiency decreased to some extent. (2) The dimension A acid solid lipid nanoparticles to optimize the prescription and workmanship. Taken 0.5g Glycerol monostearate 0.2g Span 60,4 g of Tween 80,5 g vitamin C palmitate, polyethylene glycol 400,0.04 g, 1g poloxamer F-127, 0.04g 2,6 - di-tert-butyl-methyl phenol, set 70 ℃ water bath heated to melt. 0.025g dimension A acid in 70 ℃, 200r · min-1 under stirring, continue stirring 10min Victoria A acid completely dissolved, was clear and transparent yellow solution. Then 15 ml of 70 ° C water at 200r · min-1 stirring 20min, the formation of a stable homogeneous emulsion. The speed adjusted emulsion into 1000r · min-1 stirring 78ml, 2 ℃ 0.01g EDTA-containing water, stirring 5min 200r · min-1, stirring 2h, ie. Glucan G50 micro gel entrapment efficiency was determined gt; 92%. 4 ℃, 25 ℃ and 40 ℃ stored for 3 months, content and encapsulation efficiency was no significant change. (3) release rate in vitro skin permeation and skin retention. The release table Ming Wei A acid vitamin C palmitate bubble capsule release rate is greater than the commercially available creams and Victoria A acid solid lipid nanoparticles. Mice in vitro percutaneous penetration tests showed that the accumulation of vesicles dimensional A acid higher than the commercially available creams and solid lipid nanoparticles through the skin, but the the skin storage capacity of solid lipid nanoparticles than commercially available cream and bubble capsule. Comparison vesicles and solid lipid nanoparticles in vitro skin permeability of the skin of mice, rats and rabbits, mice gt; rats gt; rabbits. Comparison vesicles and solid lipid nanoparticles in the storage capacity of the skin of mice, rats and rabbits, results in rabbits gt; rats gt; mice. Conclusion: The injection method dimensional A acid vitamin C palmitate vesicles and the prepared nanoemulsion-dimensional A acid solid lipid nanoparticles, the method is simple, optimize the prescription products encapsulation efficiency greater than 90%. Stability of lipid nanoparticles than vesicles. Vesicles in vitro release fast accumulated in vitro percutaneous through more than the commercially available creams and solid lipid nanoparticles, increasing drug percutaneous permeation of vesicles. Slow solid lipid nanoparticles in vitro release and skin retention greater than commercially available creams and solid lipid nanoparticles, its help to increase the local drug concentration. Vesicles and solid lipid nanoparticles accumulation of the dorsal skin of mice than rats and rabbits, the percutaneous penetration and skin retention is lower than in rats and rabbits.

Study on Ascorbyl Palmitate Vesicles and Solid Lipid Nanoparticles as Transdermal Administration Carrier for Tretinoin

Abstract

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