Dissertation > Excellent graduate degree dissertation topics show

Construction, Exosyndrome and Skin Targeting Study of Liranaftate Solid Lipid Nanoparticles-based Gel

Author: LiuHaiLe
Tutor: DingJinSong
School: Central South University
Course: Pharmacy
Keywords: Liranaftate Superficial mycoses Solid Lipid Nanoparticles Skin targeting
CLC: R943
Type: Master's thesis
Year: 2011
Downloads: 122
Quote: 0
Read: Download Dissertation

Abstract

First, the purpose Liranaftate (Liranaftate, LN) is a topical treatment of superficial fungal infections of the skin, its efficacy and drug related holdup in the skin, and is currently commercially available cream skin holdup is only administered 0.01% of the dose (skin retention ratio). In this paper, the the solvent emulsification diffusion method to build LN solid lipid nanoparticles (Solid lipid nanoparticles, SLN) and its gel and Characterization and preliminary stability study, designed to improve the LN skin targeting, improving skin retention ratio for the LN topical antifungal skin research methods and experimental basis for targeted drug delivery systems. Methods and Results LN-SLN build establish an HPLC method for determination of the content of the LN-SLN LN concentration in the range of 1 ~ 40μg/mL good linear relationship with the peak area day precision were less than 3%, and the average recovery was (100.04 ± 3.11)%. Take advantage of the the minicolumn centrifugation free of drugs and drug-loaded nanoparticles, method reproducibility, high recovery rate, for the LN-SLN encapsulation efficiency determination. The encapsulation efficiency, particle size, stability evaluation index, respectively microemulsion method, hot melt solidification method, film - ultrasonic dispersion method, solvent emulsification diffusion method LN-SLN, results in better solvent emulsification diffusion method. Single factor and orthogonal experimental design to optimize the formulation and process, to determine preparation process is as follows: take phospholipids (Epikuron 200) 300 mg dissolved in 5mL ethanol, glycerin monostearate (GMS) 90 mg cholesterol (CHO) 10 mg, LN 5 mg dissolved in 5 ml of acetone, after mixing, was heated to 60 ° C as the oil phase; taken poloxamer 188 (F-68) 100mg was dissolved in 30 ml of water, heated to 60 ° C, as the water phase; with 5mL syringes oil phase injected into the aqueous phase, 60 ° C, 1000r · min-1 magnetic stirring 30min, removal of the organic solvent, i.e. the suspension was LN-SLN. Good reproducibility of the process. 2 LN-SLN gel characterization and preliminary stability study the carbomer LN-SLN suspension after swelling constructed LN-SLN gel (carbopol content of 0.20%, 0.023% of the LN content) and LN-SLN gel characterization and preliminary stability study. Using TEM observations nanoparticles as spherical or spherical. Laser diffraction particle size potential analyzer determination LN-SLN, LN-SLN gel particle size (145.3 ± 6.09) nm (190.3 ± 1.63) nm; polydispersity index (PDI), respectively 0.203 ± 0.01,0.267 ± 0.04; Zeta potential (-3.44 ± 0.47) mV (-21.2 ± 1.02) mV. The minicolumn centrifugation Determination LN-SLN encapsulation efficiency was (75.8 ± 0.70)%, drug loading (5.17 ± 0.03)%. By HPLC the LN-SLN the LN-SLN gel content, respectively (0.47 ± 0.01) mg / mL (0.023 ± 0.001)%. The differential scanning calorimetry analysis suggests LN may be present on the carrier in an amorphous state. LN-SLN sensitive to bright light (4500 ± 500Lx) and temperature (25,40 ℃), 4 ° C shading conditions can be stored for 10 days; LN-SLN gel 4,25,40 ℃ to 30 days of storage stability. LN-SLN gel skin targeting using modified Franz vertical diffusion cell in vitro piglet skin permeability barrier in vitro transdermal diffusion test were 2,6,12 h after administration Remove skin and transdermal receiving fluid. The cumulative permeation investigated drug loading of 0.023% gel (suspension) LN LN cream (solution type), LN-SLN gel and 2% LN cream (zefnart) per unit area of ??epidermal holdup Qe unit area leather hold-up volume to Qd, discusses LN-SLN gel skin targeting. Results LN formulations drug substantially no penetration into the receptor fluid. The LN-SLN gel with the same concentration of LN gel, cream ratio, can significantly improve the LN in the holdup of the epidermis and dermis, its Qe12h of about 2.3 times the LN gel, for LN cream the 11.6 times; Qdl2h LN The gel is 2.5-fold, 8.5-fold LN cream. LN-SLN the gel with zefnart than, Qe, Qd There was no significant difference 12h skin retention ratio (0.94%) approximately zefnart to (0.01%) 100 times. LN-SLN gel drug can significantly improve the ability to stay on the skin. Conclusion LN suitable lipid contained package made SLN drug delivery system, using the the solvent emulsification diffusion method to build LN-SLN particle size is smaller, uniform distribution, encapsulation efficiency, high stability. LN-SLN gel has good skin targeting, the skin topically administered drug skin retention of up treatment requirements, while improving skin retention than help to improve LN clinical efficacy stability.

Construction, Exosyndrome and Skin Targeting Study of Liranaftate Solid Lipid Nanoparticles-based Gel

Abstract

Related Dissertations