Phospholipids become increasingly important as formulation excipients and as active ingredients per se. The present article summarizes particular features of commonly used phospholipids and their application spectrum within oral drug formulation and elucidates current strategies to improve bioavailability and disposition of orally administered drugs. Advantages of phospholipids formulations not only comprise enhanced bioavailability of drugs with low aqueous solubility or low membrane penetration potential, but also improvement or alteration of uptake and release of drugs, protection of sensitive active agents from degradation in the gastrointestinal tract, reduction of gastrointestinal side effects of non-steroidal anti-inflammatory drugs and even masking of bitter taste of orally applied drugs. Technological strategies to achieve these effects are highly diverse and offer various possibilities of liquid, semi-liquid and solid lipid-based formulations for drug delivery optimization.

Phospholipids and lipid-based formulations in oral drug delivery.

Silymarin, a flavonolignan derived from Silybum marianum, possesses diverse pharmacological activities, including hepatoprotective, antioxidant, anti-inflammatory, anticancer, and cardioprotective. Although clinical trials have shown silymarin is safe at high doses (>1500 mg/day) in humans, the pharmacokinetic studies over the past three decades related to absorption, distribution, metabolism, and excretion of silymarin have revealed poor absorption, rapid metabolism, and ultimately poor oral bioavailability. For optimum silymarin bioavailability, issues of solubility, permeability, metabolism, and excretion must be addressed. An array of methods have been described in recent years that can improve its bioavailability, including complexation with β-cyclodextrins, solid dispersion method, formation of microparticles and nanoparticles, self-microemulsifying drug delivery systems, micelles, liposomes, and phytosomes. This article critically reviews the recent published literature on various techniques for increasing the bioavailability of silymarin.

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Reassessing bioavailability of silymarin.

Oil based nanocarrier for improved oral delivery of silymarin: In vitro and in vivo studies

Topical ophthalmic lipid nanoparticle formulations (SLN, NLC) of indomethacin for delivery to the posterior segment ocular tissues.

Preparation and characterization of intravenously injectable nimodipine nanosuspension

Preparation, Pharmacokinetics and Body Distribution of Silymarin-Loaded Solid Lipid Nanoparticles After Oral Administration

OBJECTIVE: To investigate lyophilization of SM-SLN. METHOD: The parameters of lyophilization process was optimized. In addition, the protective effect of various types and concentrations of cryoprotectants were tested by shape, colour and disparity. RESULT: The mixture of 2% lactose and 2% glucose could better prevent nanoparticles from aggregating, the optimal lyophilization process was followed: precooled at -45 degrees C for 10 hr; primary drying at -25 degrees C for 5 hr; secondary drying at 10 degrees C for 3 hr; finally drying at 30 degrees C for 6 hr. CONCLUSION: Changes in particle size distribution during lyophilization could be minimized by optimizing the parameters of the lyophilization process and adding supporting agent.

[Freeze-drying of silymarin-loaded solid lipid nanoparticles (SM-SLN)].

The present invention is one kind of nano silybin preparation and its preparation process. The preparation has silybin extracted from Chinese medicine material silybum mariamum as effective component, stearic acid as carrier and lecithin as emulsifying agent, and is prepared via combined process of stirring emulsification and high pressure emulsification to coat silybin inside nano solid liposome particle. The nano particle has size of about 200 nm.

Silymarin nano granular preparation and process for preparing the same

An oralloy applied solution of silymarinum-glyceride behenate nanoparticles is prepared from silymarinum, glyceride behenate and soybean phosphatide as carrier, and poloxamer 188 and glycerine as suspending aid by solvent-fusing dispersion method and high-pressure emulsifying and homogenizing method. Its advantages are high biologic utilization rate and higher curative effect.

Silymarin behenic acid glyceride lipid nano particle oral solution dosage and its preparation method

A lipid nanoparticle (size 100-200nm) of glyceride behenate is prepared by the combination of solvent-fusion method and high-pressure emulsifying, where the mixture of ATO and soybean phosphatide is used as carrier and the poloxamer 188 is used as suspending aid to make the medicine is wrapped by lipid nanoparticle to form uniform dispersed system in water Its advantages are high biological utilization rate and stable absorptivity

Lu Weigen

Papers

Preparation, Pharmacokinetics and Body Distribution of Silymarin-Loaded Solid Lipid Nanoparticles After Oral Administration

[Freeze-drying of silymarin-loaded solid lipid nanoparticles (SM-SLN)].

Silymarin nano granular preparation and process for preparing the same

Silymarin behenic acid glyceride lipid nano particle oral solution dosage and its preparation method

Lipid nano-particle of glyceride behenate and its preparation method