Lipid - An emerging platform for oral delivery of drugs with poor bioavailability

被引:298
作者
Chakraborty, Subhashis [1 ]
Shukla, Dali [1 ]
Mishra, Brahmeshwar [1 ]
Singh, Sanjay [1 ]
机构
[1] Banaras Hindu Univ, Inst Technol, Dept Pharmaceut, Varanasi 221005, Uttar Pradesh, India
关键词
Lipid-based oral drug delivery; Lipase activity; Lymphatic uptake; Bioavailability enhancement; Solid dosage form; Adsorption; Lipid digestion products; In vitro lipolytic model; In vitro-in vivo correlation; Solid lipid nanoparticles; WATER-SOLUBLE DRUGS; IN-VITRO LIPOLYSIS; INTESTINAL LYMPHATIC TRANSPORT; COMMON FORMULATION LIPIDS; ACID-BINDING PROTEIN; DRY EMULSION TABLET; P-GLYCOPROTEIN; FATTY-ACID; NANOPARTICLES SLN; MEDIUM-CHAIN;
D O I
10.1016/j.ejpb.2009.06.001
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The sole objective of pharmaceutical science is to design successful dosage forms which fulfill the therapeutic needs of the patients effectively. Development of new drug entities is posing real challenge to formulators, particularly due to their poor aqueous solubility which in turn is also a major factor responsible for their poor oral bioavailability. Lipids as carriers, in their various forms, have the potential of providing endless opportunities in the area of drug delivery due to their ability to enhance gastrointestinal solubilization and absorption via selective lymphatic uptake of poorly bioavailable drugs. These properties can be harvested to improve the therapeutic efficacy of the drugs with low bioavailability, as well as to reduce their effective dose requirement. The present communication embodies an in-depth discussion on the role of lipids (both endogenous and exogenous) in bioavailability enhancement of poorly soluble drugs, mechanisms involved therein, approaches in the design of lipid-based oral drug delivery systems with particular emphasis on solid dosage forms, understanding of morphological characteristics of lipids upon digestion, in vitro lipid digestion models, in vivo studies and in vitro-in vivo correlation. (c) 2009 Elsevier B.V. All rights reserved.
引用
收藏
页码:1 / 15
页数:15
相关论文
共 208 条
  • [1] Relative bioavailability of griseofulvin lyophilized dry emulsion tablet vs. immediate release tablet: A single-dose, randomized, open-label, six-period, crossover study in healthy adult volunteers in the fasted and fed states
    Ahmed, Iman Saad
    Aboul-Einien, Mona Hassan
    Mohamed, Osama Hussein
    Farid, Samar Farghali
    [J]. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2008, 35 (03) : 219 - 225
  • [2] In vitro and in vivo evaluation of a fast-disintegrating lyophilized dry emulsion tablet containing griseofulvin
    Ahmed, Iman Saad
    Hassan, Mona Aboul-Einien
    [J]. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2007, 32 (01) : 58 - 68
  • [3] THE ROLE OF CALCIUM-IONS AND BILE-SALTS ON THE PANCREATIC LIPASE-CATALYZED HYDROLYSIS OF TRIGLYCERIDE EMULSIONS STABILIZED WITH LECITHIN
    ALVAREZ, FJ
    STELLA, VJ
    [J]. PHARMACEUTICAL RESEARCH, 1989, 6 (06) : 449 - 457
  • [4] A THEORETICAL BASIS FOR A BIOPHARMACEUTIC DRUG CLASSIFICATION - THE CORRELATION OF IN-VITRO DRUG PRODUCT DISSOLUTION AND IN-VIVO BIOAVAILABILITY
    AMIDON, GL
    LENNERNAS, H
    SHAH, VP
    CRISON, JR
    [J]. PHARMACEUTICAL RESEARCH, 1995, 12 (03) : 413 - 420
  • [5] PHASE-TRANSITIONS BETWEEN VESICLES AND MICELLES DRIVEN BY COMPETING CURVATURES
    ANDELMAN, D
    KOZLOV, MM
    HELFRICH, W
    [J]. EUROPHYSICS LETTERS, 1994, 25 (03): : 231 - 236
  • [6] AOYAGI N, 1982, J PHARMACOBIO-DYNAM, V5, P120
  • [7] CALCITONIN-LOADED LIPOSOMES - STABILITY UNDER ACIDIC CONDITIONS AND BILE SALTS-INDUCED DISRUPTION RESULTING IN CALCITONIN-PHOSPHOLIPID COMPLEX-FORMATION
    ARIEN, A
    HENRYTOULME, N
    DUPUY, B
    [J]. BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES, 1994, 1193 (01): : 93 - 100
  • [8] STUDY OF IN-VITRO AND IN-VIVO STABILITY OF LIPOSOMES LOADED WITH CALCITONIN OR INDIUM IN THE GASTROINTESTINAL-TRACT
    ARIEN, A
    GOIGOUX, C
    BAQUEY, C
    DUPUY, B
    [J]. LIFE SCIENCES, 1993, 53 (16) : 1279 - 1290
  • [9] CORRELATION BETWEEN ORAL-DRUG ABSORPTION IN HUMANS AND APPARENT DRUG PERMEABILITY COEFFICIENTS IN HUMAN INTESTINAL EPITHELIAL (CACO-2) CELLS
    ARTURSSON, P
    KARLSSON, J
    [J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1991, 175 (03) : 880 - 885
  • [10] The metastatic cascade in prostate cancer
    Arya, Manit
    Bott, Simon R.
    Shergill, Iqbal S.
    Ahmed, Flashim U.
    Williamson, Magali
    Patel, Fliten R.
    [J]. SURGICAL ONCOLOGY-OXFORD, 2006, 15 (03): : 117 - 128