Preparation and in vitro characterization of a eutectic based semisolid self-nanoemulsified drug delivery system (SNEDDS) of ubiquinone: mechanism and progress of emulsion formation

被引:219
作者
Nazzal, S
Smalyukh, II
Lavrentovich, OD
Khan, MA
机构
[1] Texas Tech Univ, Hlth Sci Ctr, Sch Pharm, Dept Pharmaceut Sci, Amarillo, TX 79106 USA
[2] Kent State Univ, Chem Phys Interdisciplinary Program, Kent, OH 44242 USA
[3] Kent State Univ, Inst Liquid Crystal, Kent, OH 44242 USA
关键词
coenzyme Q(10); eutectic mixture; self-nanoemulsified drug delivery system; SNEDDS; turbidimetry; liquid crystals;
D O I
10.1016/S0378-5173(02)00003-0
中图分类号
R9 [药学];
学科分类号
1007 [药学];
摘要
The objectives of the present work were, first, to develop a self-nanoemulsified drug delivery system (SNEDDS) based on the eutectic properties of ubiquinone (CoQ(10)); and second, to Study the progress of emulsion formation and drug release mechanisms by turbidimetry and droplet size analysis. Binary phase diagrams of CoQ(10) with menthol and essential oils were constructed and used to develop the self- nanoemulsified formulation. Pseudo ternary phase diagram was constructed to identify the efficient self-emulsification region. Release mechanisms of the resultant formulas were quantified using turbidimetry in combination with dissolution studies. Turbidity time profiles revealed three distinctive regions: lag phase. plateau, and the pseudolinear phase. Lag phase was attributed to the liquid crystalline properties of the formula. Plateau turbidity was correlated with droplet size. Laser diffraction analysis revealed an average droplet diameter of 100 nm. Emulsification rate was obtained from the corrected slope of the pseudolinear phase of the profile. Stability of the formula was further evaluated using Fourier transform-infrared (FT-IR) attached to an attenuated total reflectance (ATR) accessory. The present study revealed a eutectic based semisolid self-emulsified delivery system that can overcome the drawbacks of the traditional emulsified systems such as low solubility and irreversible precipitation of the active drug in the vehicle with time. (C) 2002 Elsevier Science B.V. All rights reserved.
引用
收藏
页码:247 / 265
页数:19
相关论文
共 34 条
[1]
Factors affecting the efficiency of a self-emulsifying oral delivery system [J].
Bachynsky, MO ;
Shah, NH ;
Patel, CI ;
Malick, AW .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1997, 23 (08) :809-816
[2]
Benet LZ., 1998, U. S. Patent, Patent No. [5,716,928, 5716928]
[3]
BOLTENHAGEN P, 1991, J PHYS II, V1, P1233, DOI 10.1051/jp2:1991130
[4]
SELF-EMULSIFYING DRUG DELIVERY SYSTEMS - FORMULATION AND BIOPHARMACEUTIC EVALUATION OF AN INVESTIGATIONAL LIPOPHILIC COMPOUND [J].
CHARMAN, SA ;
CHARMAN, WN ;
ROGGE, MC ;
WILSON, TD ;
DUTKO, FJ ;
POUTON, CW .
PHARMACEUTICAL RESEARCH, 1992, 9 (01) :87-93
[5]
Chiwele I, 2000, CHEM PHARM BULL, V48, P951
[6]
Chopra RK, 1998, INT J VITAM NUTR RES, V68, P109
[7]
Formulation and physical characterization of water-in-oil microemulsions containing long- versus medium-chain glycerides [J].
Constantinides, PP ;
Scalart, JP .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1997, 158 (01) :57-68
[8]
AN INVESTIGATION INTO THE MECHANISMS OF SELF-EMULSIFICATION USING PARTICLE-SIZE ANALYSIS AND LOW-FREQUENCY DIELECTRIC-SPECTROSCOPY [J].
CRAIG, DQM ;
BARKER, SA ;
BANNING, D ;
BOOTH, SW .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1995, 114 (01) :103-110
[9]
AN INVESTIGATION INTO THE PHYSICOCHEMICAL PROPERTIES OF SELF-EMULSIFYING SYSTEMS USING LOW-FREQUENCY DIELECTRIC-SPECTROSCOPY, SURFACE-TENSION MEASUREMENTS AND PARTICLE-SIZE ANALYSIS [J].
CRAIG, DQM ;
LIEVENS, HSR ;
PITT, KG ;
STOREY, DE .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1993, 96 (1-3) :147-155
[10]
Physicochemical characterization and evaluation of a microemulsion system for oral delivery of cyclosporin A [J].
Gao, ZG ;
Choi, HG ;
Shin, HJ ;
Park, KM ;
Lim, SJ ;
Hwang, KJ ;
Kim, CK .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1998, 161 (01) :75-86