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Abstract
Lipid-based drug delivery systems, or lipidic carriers, are being extensively employed to enhance the bioavailability of poorly-soluble drugs. They have the ability to incorporate both lipophilic and hydrophilic molecules and protecting them against degradation in vitro and in vivo. There is a number of physical attributes of lipid-based nanocarriers that determine their safety, stability, efficacy, as well as their in vitro and in vivo behaviour. These include average particle size/diameter and the polydispersity index (PDI), which is an indication of their quality with respect to the size distribution. The suitability of nanocarrier formulations for a particular route of drug administration depends on their average diameter, PDI and size stability, among other parameters. Controlling and validating these parameters are of key importance for the effective clinical applications of nanocarrier formulations. This review highlights the significance of size and PDI in the successful design, formulation and development of nanosystems for pharmaceutical, nutraceutical and other applications. Liposomes, nanoliposomes, vesicular phospholipid gels, solid lipid nanoparticles, transfersomes and tocosomes are presented as frequently-used lipidic drug carriers. The advantages and limitations of a range of available analytical techniques used to characterize lipidic nanocarrier formulations are also covered.
Highlights
The number of products on the market manufactured using lipidic nanocarriers is increasing in parallel with increasing public awareness of the health benefits of such products
Lipid vesicles are initially prepared as a liquid suspension, they can be subsequently incorporated in a cream, lotion, aerosol, soft-gel, powder or other formulations and dosage forms
polydispersity index (PDI) values bigger than 0.7 indicate that the sample has a very broad particle size distribution and is probably not suitable to be analysed by the dynamic light scattering (DLS) technique
Summary
The number of products on the market manufactured using lipidic nanocarriers is increasing in parallel with increasing public awareness of the health benefits of such products. The main chemical components of liposomes are amphiphilic lipid/phospholipid molecules [1] They improve the efficacy of pharmaceutical, nutraceutical and other bioactive compounds by entrapment and release of water-soluble, lipid-soluble and amphiphilic materials, as well as targeting the encapsulated compounds to particular cells or tissues [2]. There are a number of review articles describing the preparation methods of lipid-based vesicles, which readers are referred to for a broader coverage [1,2,5,8] In addition to their application in the fields of encapsulation of bioactive compounds and drug delivery and targeting, lipid vesicles are being used as simplified models of cells and biological membranes. Lipidic nanocarriers could be retained because of the capillary pore size or dimensions of the interstitial space of the tissue [26,27]
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