Amelioration of lipophilic compounds in regards to bioavailability as self-emulsifying drug delivery system (SEDDS)

被引:27
作者
Baghel, Pragya [1 ]
Roy, Amit [1 ]
Verma, Shekhar [2 ]
Satapathy, Trilochan [3 ]
Bahadur, Sanjib [1 ]
机构
[1] Columbia Inst Pharm, Raipur, Chhattisgarh, India
[2] Pt Deendayal Upadhyay Smriti Hlth Sci & Aayush Un, Raipur, Chhattisgarh, India
[3] Raipur Inst Technol, Raipur, Chhattisgarh, India
关键词
Dispersion system; Lipophilicity; Self-emulsification; Nano-carrier; Bioavailability; ENHANCED ORAL BIOAVAILABILITY; IN-VITRO; DISSOLUTION RATE; DESIGN; CARRIERS; FORMULATION; STABILITY; SMEDDS; NANOEMULSIONS; MICROEMULSION;
D O I
10.1186/s43094-020-00042-0
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Background: High lipophilicity and poor aqueous solubility are the endemic problems of new drug molecules. Sixty to seventy percent of these drugs are unable to solubilize completely in aqueous media, or have very low permeability. This hampers their oral absorption and further leads to their poor bioavailability. Various researches are in progress to overcome these limitations. Novel technologies like nano-carrier systems have become popular for improving the solubility of drugs. Main body: Lipid-based formulations, among nano systems, are taking pace for the enhancement of solubility, oral absorption, and hence the bioavailability of drugs. Among the lipid formulations, self-emulsification systems are gaining popularity by offering various advantages to delivery systems. Self-emulsifying drug delivery systems (SEDDS) are isotropic blends of oil and surfactant/co-surfactants. These ingredients upon gentle agitation in aqueous media results in the formation of o/w emulsion. In spite of many works published in SEDDS, the major concerns of this article are to discuss the various approaches to formulate a good lipid-based carrier system for poorly aqueous soluble drugs, role of various polymers, and their categories used in the formulation along-with the modern technologies used for enhancing the stability of liquid SEDDS. This review majorly focuses upon the problems related to the poor aqueous solubility of the newer lipid molecules and the solutions to overcome their solubility and in addition bioavailability. Conclusion: As per the researches done in formulation and optimization of SEDDS for the enhancement of bioavailability of lipophilic molecules, it can be stated that the aqueous solubility as well as bioavailability can be increased by many folds compared to their marketed or other oral formulations.
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页数:11
相关论文
共 86 条
[1]  
Anette M, 2016, EUR J PHARM SCI, V108, P62
[2]  
[Anonymous], ASIAN J PHARM SCI
[3]   Design of a gelatin microparticle-containing self-microemulsifying formulation for enhanced oral bioavailability of dutasteride [J].
Baek, In-Hwan ;
Ha, Eun-Sol ;
Yoo, Jin-Wook ;
Jung, Yunjin ;
Kim, Min-Soo .
DRUG DESIGN DEVELOPMENT AND THERAPY, 2015, 9 :3231-3238
[4]  
Bhandari S, 2017, THER DELIV, V8, P201, DOI 10.4155/tde-2016-0092
[5]   Tablets and minitablets prepared from spray-dried SMEDDS containing naproxen [J].
Cerpnjak, Katja ;
Pobirk, Alenka Zvonar ;
Vrecer, Franc ;
Gasperlin, Mirjana .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2015, 495 (01) :336-346
[6]   Development of a solid self-microemulsifying drug delivery system (SMEDDS) for solubility enhancement of naproxen [J].
Cerpnjak, Katja ;
Zvonar, Alenka ;
Vrecer, Franc ;
Gasperlin, Mirjana .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2015, 41 (09) :1548-1557
[7]   Characterization of naproxen-loaded solid SMEDDSs prepared by spray drying: The effect of the polysaccharide carrier and naproxen concentration [J].
Cerpnjak, Katja ;
Zvonar, Alenka ;
Vrecer, Franc ;
Gasperlin, Mirjana .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2015, 485 (1-2) :215-228
[8]   Controversies with self-emulsifying drug delivery system from pharmacokinetic point of view [J].
Chatterjee, Bappaditya ;
Almurisi, Samah Hamed ;
Dukhan, Ather Ahmed Mahdi ;
Mandal, Uttam Kumar ;
Sengupta, Pinaki .
DRUG DELIVERY, 2016, 23 (09) :3639-3652
[9]   Preparation and In Vitro/In Vivo Evaluation of Puerarin Solid Self-Microemulsifying Drug Delivery System by Spherical Crystallization Technique [J].
Cheng, Gang ;
Hu, Rongfeng ;
Ye, Lei ;
Wang, Bin ;
Gui, Yun ;
Gao, Song ;
Li, Xiaoxiang ;
Tang, Jihui .
AAPS PHARMSCITECH, 2016, 17 (06) :1336-1346
[10]   Comparison of paclitaxel solid dispersion and polymeric micelles for improved oral bioavailability and in vitro anti-cancer effects [J].
Choi, Jin-Seok ;
Cho, Nam Hyuk ;
Kim, Dong-Hyun ;
Park, Jeong-Sook .
MATERIALS SCIENCE AND ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS, 2019, 100 :247-259