Phospholipids and Lipid-Based Formulations in Oral Drug Delivery

Abstract

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.

Recent Advances in Drug Delivery Systems

“…Those systems can incorporate a variety of molecules and can be designed to improve the uptake by dendritic cells through different receptor-mediated routes [31]. Furthermore, cochleates are stable particles (more than other lipidic structures) derived from liposomes composed mainly of charged phosphatidylserine in the presence of divalent counter ion such as Ca 2+ which forms a continuous large lipid bilayer sheet with no internal aqueous space [35,42,43]. Cochleate delivery has shown potential use for amphotericin B, factor VIII delivery, proteins, peptides and DNA [43,44].…”

“…Liposomes which are most commonly produced with phosphatidylcholine show great compatibility, ease of preparation, wide range of drug compatibilities, increased solubility of drugs (e.g. cycloporin A [35]), tuned pharmacokinetic profile and improved oral absorption. Commonly, they present difficulties when orally delivered due to the poor stability of the vesicles under the physiological conditions typically found in the GI tract [4,35,36].…”

“…cycloporin A [35]), tuned pharmacokinetic profile and improved oral absorption. Commonly, they present difficulties when orally delivered due to the poor stability of the vesicles under the physiological conditions typically found in the GI tract [4,35,36]. Liposomes can also act as a drug depot injected subcutaneously and intact vesicles were found after 96h.…”

The comparison of different daidzein-PLGA nanoparticles in increasing its oral bioavailability

“…45 In addition, phospholipids have been proven to have a high affinity for flavonoids and accelerates daidzein transport across the cell membrane. [46][47][48] Cyclodextrin has been proven as a drug absorption enhancer as well. 49,50 Since daidzein is a typical poor hydrophilic and poor lipophilic drug with very low oral bioavailability, …”

Sistemas carreadores lipídicos nanoestruturados para ivermectina e metopreno visando controle de parasitas

“…Dentre essas estruturas, destacam-se os nanocarreadores, que permitem melhorar a biodisponibilidade de muitos compostos bioativos, como, por exemplo, o aumento da solubilidade aquosa, melhorando assim processos de absorção e distribuição tecidual (farmacocinética) e também a diminuição de possíveis efeitos tóxicos (redução da toxidade local e sistêmica). 1 O desenvolvimento da nanotecnologia permitirá seu uso na produção animal em forma de monitoramento ou mesmo de aplicação direta de produtos nanotecnológicos na saúde, na alimentação, controle de parasitas, conforto térmico e ambiental desses animais. 2 A nanotecnologia apresenta grande potencial para as pesquisas, possibilitando o desenvolvimento de novos produtos destinados à melhoria da sanidade e saúde animal, o que propicia produtos derivados de animais com maior qualidade e segurança, além de possibilitar potenciais aplicações na área da medicina veterinária, que incluem sistemas de diagnóstico e tratamento de doenças, novas ferramentas para o melhoramento molecular e celular, modificação de resíduos animais, detecção de patógenos, isolamento de toxinas, vetores para o transporte de fármacos, 3 entre outros.…”