Abstract
Drug toxicity is an important factor that contributes significantly to adverse drug events in current healthcare practice. Application of lipid-based nanocarriers in drug formulation is one approach to improve drug safety. Lipid-based delivery systems include micelles, liposomes, solid lipid nanoparticles, nanoemulsions and nanosuspensions. These carriers are generally composed of physiological lipids well tolerated by human body. Delivery of water-insoluble drugs in these formulations increases their solubility and stability in aqueous media and eliminates the need for toxic co-solvents or pH adjustment to solubilize hydrophobic drugs. Association or encapsulation of peptides/proteins within lipid-based carriers protects the labile biologics against enzymatic degradation, hence reducing the therapeutic dose required and risk of dose-dependent toxicity. Most importantly, lipid-based nanocarriers alter the pharmacokinetics and biodistribution of drugs through passive and active targeting, leading to increased drug accumulation at target sites while significantly decreasing non-specific distribution to other tissues. Furthermore, surface modification of these nanocarriers reduces immunogenicity of drug–carrier complexes, imparts stealth by preventing opsonization and removal by phagocytes and minimizes interaction with circulating blood components. In view of heightening attention on drug safety in patient treatment, lipid-based nanocarrier is therefore an important and promising option for formulation of pharmaceutical products to improve treatment safety and efficacy.
Highlights
In drug discovery pipeline, it was estimated that approximately 10,000 chemical entities need to be tested before one would eventually reach the consumer market
It should be noted that nanomedicines that are between 10-100nm have superior advantage over bigger sized particles for passive targeting and tissue penetration
We have developed 99Tc-HMPAO encapsulated sterically stabilized liposomes that were actively targeted with vasoactive intestinal peptide (VIP) for theragonostic purpsose [105]
Summary
It was estimated that approximately 10,000 chemical entities need to be tested before one would eventually reach the consumer market. When used to formulate docetaxel, a water-insoluble cytotoxic taxane drug analogous to paclitaxel, polysorbate 80 resulted in occurrence of acute hypersensitivity reactions similar to Cremophor EL® in Taxol® [14] This surface active agent was postulated to be accountable, in part, for the fluid retention side effect observed with the use of this docetaxel formulation [15]. Another common strategy applied to increase aqueous solubility of drugs, acidic or basic drugs, is pH adjustment While this approach helps to maximize drug solubilization in their salt forms, there is amplified risk of drug precipitation upon intravenous injection when formulation pH becomes increasingly different from physiological pH, leading to injection phlebitis and decreased drug effect [18, 19]. It should be noted that nanomedicines that are between 10-100nm have superior advantage over bigger sized particles for passive targeting and tissue penetration
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