Drug carrier

About: Drug carrier is a research topic. Over the lifetime, 18276 publications have been published within this topic receiving 997718 citations. The topic is also known as: drug carriers & drug vehicle.

Polymer-coated long-circulating microparticulate pharmaceuticals

Abstract: The field of long-circulating microparticulate drug carriers is reviewed. The protective effect of certain polymers including poly(ethylene glycol) on nanoparticulate carriers (liposomes, nanoparticles, micelles) is considered in terms of statistical behaviour of macromolecules in solution. Using liposomes as an example, the mechanism is discussed assuming that surface-grafted chains of flexible and hydrophilic polymers form dense 'conformational clouds' preventing other macromolecules from interaction with the surface even at low concentrations of the protecting polymer. The scale of the protective effect is interpreted as the balance between the energy of the hydrophobic anchor interaction with the liposome membrane core or with the particle surface and the energy of the polymer chain free motion in solution. The possibility of using protecting polymers other than poly(ethylene glycol) is analysed, and examples of such polymers are given, based on polymer-coated liposome biodistribution data. General requirements for protecting polymers are formulated. Sterically protected nanoparticles and micelles are considered, and differences in steric protection of liposomes and particles are discussed. The problem of the preparation of drug carriers combining longevity and targetability is analysed. The biological consequences of steric protection of drug carriers with surface-grafted polymers are discussed, and possible clinical applications for long-circulating pharmaceutical carriers are considered.

Site-specific drug delivery to pilosebaceous structures using polymeric microspheres

Abstract: In order to improve the therapeutic index of adapalene, a new drug under development for the treatment of acne, site-specific delivery to the hair follicles using 50:50 poly(DL-lactic-co-glycolic acid) microspheres as particulate carriers was investigated in vitro and in vivo. The percutaneous penetration pathway of the microspheres was shown to be dependent on their mean diameter. Thus, after topical application onto hairless rat or human skin, adapalene-loaded microspheres (5-µm diameter) were specifically targeted to the follicular ducts and did not penetrate via the stratum corneum. The in vitro release of adapalene from the microspheres into artificial sebum at 37°C was controlled and faster than the in vivo sebum excretion in humans. Aiming to reduce either the applied dose of drug or the frequency of administration, different formulations of adapalene-loaded microspheres were evaluated in vivo in the rhino mouse model. A dose-related comedolytic activity of topical formulations of adapalene-loaded microspheres was observed in this model. Furthermore, by applying a site-specific drug delivery system (0.1% adapalene) every other day or by administering a 10-fold less concentrated targeted formulation (0.01%) every day, a pharmacological activity equivalent to a daily application of an aqueous gel containing drug crystals (0.1% adapalene) was observed. Since an aqueous gel containing 10% adapalene-loaded microspheres was not irritating in a rabbit skin irritancy test, this formulation was applied onto forearms of human volunteers. Site-specific drug delivery was further evidenced by follicular biopsy. These results support the view that follicular drug targeting using 5-µm polymeric microspheres may represent a promising therapeutic approach for the treatment of pathologies associated with pilosebaceous units.