Lipid Formulation as a Drug Carrier for Drug Delivery

Abstract

In recent years, a Drug Delivery System (DDS), a preparative approach attracts the attention in the development of new drugs. DDS focuses on the regulation of the in vivo dynamics, such as absorption, distribution, metabolism, and elimination, thereby improving the effectiveness and the safety of the drugs by an applicable use of drug preparation technologies. A conventional intravenous dosage form of Amphotericin B (AmB), Fungizone, is the most effective clinically available for treating fungal infections. However, the clinical efficacy of AmB is limited by its adverse effects. Several lipid formulations, such as Liposomal AmB (L-AmB), AmB lipid complex (ABLC), and AmB colloidal dispersion (ABCD), with reduced side effects have been developed. These formulations are reported to have excellent safety and efficacy. However, comparable efficacy can be achieved only when they are administered at high doses than AmB. One of the problems of using these formulations is that they are easily taken up by the reticuloendothelial system (RES). An artificial lipoprotein-like particles, a novel drug carrier Lipid Nano-Sphere (LNS), which is 25 - 50 nm in size and is composed of phospholipids and simple lipid. LNS show a higher plasma concentration of drugs and lower uptake by RES-tissue different forms other lipid base drug carriers. In vitro and in vivo, LNS incorporating AmB, NS-718, shows reduced toxicity, while maintaining activity against fungi. LNS have a unique characteristic as an effective carrier of AmB for treatment of fungal infection.

Optimizing efficacy of amphotericin B through nanomodification

“…This characteristic of NS-718 to avoid uptaking by reticuloendothelial system (RES) is related to high plasma concentration of AmB. These results suggest that NS-718 have several unique characteristics different from other lipid formulations for the treatment of fungal infections (Seki et al 1994; Tomii 2002). In another study NS-718 was found to be more effective than D-AmB or L-AmB against clinical isolates of C. albicans and Aspergillus fumigatus .…”

“…In DDS, pharmacological techniques are used to control pharmacokinetic properties (absorption, distribution, metabolism, and excretion) and to improve the efficacy and safety of a drug. Lipid formulations, such as liposomes and emulsion based carriers, are very highly predictable and are now explored in numerous directions, and several products have already been made commercially available (Tomii 2002). …”

Nanostructure-mediated drug delivery

“…Biologic nanostructures that have been developed for drug delivery purposes include lipid nanotubes [33], lipid nanospheres [34][35][36], lipid nanoparticles [37][38][39], lipid emulsions [40][41][42] circular peptides [43,44], chitosan [45][46][47][48], viral nanoparticles [49], and nucleic acid nanostructures [50]. One of the most investigated lipid forms is the liposome, which is a hollow vesicle that can be used to entrap and release drug molecules [51][52][53][54][55].…”

Nanotechnology and site-targeted drug delivery

“…One of the problems of lipid formulations is their easy uptake by the reticuloendothelial system (RES). Another artificial lipoprotein-like particle, a novel drug carrier LNS developed by Tomii et al [35], is 25-50 nm in size and is composed of phospholipids and simple lipids. LNS were reported to show a higher plasma concentration of drugs and lower uptake by RES-tissue as compared to other forms of lipid-based drug carriers.…”