Design of temozolomide-loaded proliposomes and lipid crystal nanoparticles with industrial feasible approaches: comparative assessment of drug loading, entrapment efficiency, and stability at plasma pH.

Temozolomide is a drug approved for treating glioblastomas, which has 100% oral bioavailability but gets degraded at physiological pH thus having very short half-life and only 20-30% brain bioavailability. Due to its amphiphilic nature, reported nanoformulations exhibits poor drug loading. The objective of this work was to formulate lipid-based drug delivery systems to enhance the brain bioavailability by prolonging the drug release and circulation time of the drug to overcome the limitations of the existing therapies and possible reduction of side effects.

Lipid Nanocarriers for Enhanced Delivery of Temozolomide to the Brain.

Brain disorders, a diverse range of conditions comprising of neurological and psychiatric conditions, are the leading cause of disability, severely affect the quality of life, and in many cases lead to mortality. The prime challenge in treatment of brain disorders is to deliver therapeutics by overcoming the blood-brain barrier (BBB), a unique anatomical and physiological barrier which restricts the passage of a number of molecules, proteins, and cells from the bloodstream. Lipid nanoparticles have emerged as promising drug delivery systems primarily because of biodegradability, low toxicity potential, and the ability to cross physiological barriers especially the BBB even without surface modifications.

Nanostructured lipid carriers for site-specific drug delivery.

Nanostructured lipid carriers (NLC), comprises of a blend of solid and liquid lipids which results in a partially crystallized lipid system and imparts many advantages over solid lipid nanoparticles such as enhanced drug loading capacity, drug release modulation flexibility and improved stability. NLC have found numerous applications in both pharmaceutical and cosmetic industry due to ease of preparation, the feasibility of scale-up, biocompatibility, non-toxicity, enhanced targeting efficiency and the possibility of site-specific delivery via various routes of administration. This review highlights the NLC with focus on the structure, the various fabrication techniques used and the characterization techniques which are critical in the development of a suitable and stable formulation.