Research advancement on sokid kipid nanopartickes (1)
[Abstract] In recent years, the SLNs have been reported as potential drug carrier systems. They offer the possibility of controlled drug release and drug targeting and produce protection of incorporated active compounds against degradation, which combine the advantages of other traditional collodial systems(i.e. microemulsions, liposomes and polymeric nanoparticles). SLNs formulations for various application routes(oral, parenteral, dermal, pulmonary, ocular) have been developed and thoroughly characterized in vitro and in vivo. This paper is focused on general ingredients, the preparation, application routes and development prospect.
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[Key words] Solid lipid nanoparticles; Carrier; Oral administration; Transdermal administration
[CLC number] R966 [Document code]A [Article ID]1673-7210(2009)08(c)-010-03
固体脂质纳米粒给药系统新载体的研究进展
陈桐楷,李 园,林华庆
(广东药学院,广东省药物新剂型重点实验室,广州 510006)
[摘要] 固体脂质纳米粒是近年来很受重视的一种新型药物传递载体,它综合了传统胶体给药系统如乳剂、脂质体及聚合物纳米粒等的优点,具有靶向、控释、提高药物稳定性、毒性小、可大批量生产等特性,可供多途径给药。本文就近年来固体脂质纳米粒的组成、制备方法、在给药途径中的应用以及发展前景作一综述。
, http://www.100md.com
[关键词] 固体脂质纳米粒;载体;口服给药;经皮给药
Recently, solid lipid nanoparticles (SLNs) have gained increasing attention as a promising colloidal carrier system, particularly for lipophilic drugs. SLNs are high melting point lipid as a solid core coated by surfactants such as lecithin, Tween-80. Thus, lipophilic drugs can be highly efficiently incorporated in the lipid core of SLNs. The solid core of SLNs, instead of fluid core of liposomes and emulsions, allows the prolonged and controlled release of drugs and may protect the incorporated drugs against chemical degradation[1].
, http://www.100md.com
It has been claimed that SLNs combine the advantages and avoid the disadvantages of other colloidal carriers, such as controlling drug release and drug targeting to decrease the drug toxicity, high temporal and physical stability, high loading capacities, incorporation of lipophilic and hydrophilic drugs, no biotoxicity of the carrier, avoidance of organic solvents, no problems with respect to large scale production and sterilization[2].
1 Production of SLNs
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1.1 High pressure homogenization
1.1.1 Hot homogenization Hot homogenization is carried out at temperatures above the melting point of the lipid and can therefore be regarded as the homogenization of an emulsion[3]. A pre-emulsion of the drug loaded lipid melt and the aqueous emulsifier phase is obtained by high-shear mixing device. The hot pre-emulsion is then processed in a temperature controlled high pressure homogeniser, generally a maximum of three cycles at 500 bar are sufficient[4].
, 百拇医药
1.1.2 Cold homogenization The Cold homogenization is a suitable technique for processing temperature labile drugs or hydrophilic drugs. Here, lipid and drugs are melted together and then rapidly ground under liquid nitrogen forming solid lipid microparticles. A pre-suspension is then homogenized at or below room temperature forming SLNs, the homogenizing conditions are always five cycles at 500 bar[5]., 百拇医药(ＣＨＥＮ Ｔｏｎｇｋａｉ ＬＩ Ｙｕａｎ ＬＩＮ Ｈｕａｑｉ)
, http://www.100md.com
[Key words] Solid lipid nanoparticles; Carrier; Oral administration; Transdermal administration
[CLC number] R966 [Document code]A [Article ID]1673-7210(2009)08(c)-010-03
固体脂质纳米粒给药系统新载体的研究进展
陈桐楷,李 园,林华庆
(广东药学院,广东省药物新剂型重点实验室,广州 510006)
[摘要] 固体脂质纳米粒是近年来很受重视的一种新型药物传递载体,它综合了传统胶体给药系统如乳剂、脂质体及聚合物纳米粒等的优点,具有靶向、控释、提高药物稳定性、毒性小、可大批量生产等特性,可供多途径给药。本文就近年来固体脂质纳米粒的组成、制备方法、在给药途径中的应用以及发展前景作一综述。
, http://www.100md.com
[关键词] 固体脂质纳米粒;载体;口服给药;经皮给药
Recently, solid lipid nanoparticles (SLNs) have gained increasing attention as a promising colloidal carrier system, particularly for lipophilic drugs. SLNs are high melting point lipid as a solid core coated by surfactants such as lecithin, Tween-80. Thus, lipophilic drugs can be highly efficiently incorporated in the lipid core of SLNs. The solid core of SLNs, instead of fluid core of liposomes and emulsions, allows the prolonged and controlled release of drugs and may protect the incorporated drugs against chemical degradation[1].
, http://www.100md.com
It has been claimed that SLNs combine the advantages and avoid the disadvantages of other colloidal carriers, such as controlling drug release and drug targeting to decrease the drug toxicity, high temporal and physical stability, high loading capacities, incorporation of lipophilic and hydrophilic drugs, no biotoxicity of the carrier, avoidance of organic solvents, no problems with respect to large scale production and sterilization[2].
1 Production of SLNs
, http://www.100md.com
1.1 High pressure homogenization
1.1.1 Hot homogenization Hot homogenization is carried out at temperatures above the melting point of the lipid and can therefore be regarded as the homogenization of an emulsion[3]. A pre-emulsion of the drug loaded lipid melt and the aqueous emulsifier phase is obtained by high-shear mixing device. The hot pre-emulsion is then processed in a temperature controlled high pressure homogeniser, generally a maximum of three cycles at 500 bar are sufficient[4].
, 百拇医药
1.1.2 Cold homogenization The Cold homogenization is a suitable technique for processing temperature labile drugs or hydrophilic drugs. Here, lipid and drugs are melted together and then rapidly ground under liquid nitrogen forming solid lipid microparticles. A pre-suspension is then homogenized at or below room temperature forming SLNs, the homogenizing conditions are always five cycles at 500 bar[5]., 百拇医药(ＣＨＥＮ Ｔｏｎｇｋａｉ ＬＩ Ｙｕａｎ ＬＩＮ Ｈｕａｑｉ)