Anjali More, Ameeduzzafar Zafar, Omar Awad Alsaidan, Misbahuddin Rafeeq, Ali Hazazi, Abdulkarim S Binshaya, Jawaher Amer Alsaiari, Shoaeb Mohammad Syed
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引用次数: 0
Abstract
This study aimed to create nanostructured lipid carriers (NLCs) loaded with pravastatin to improve its long-term anti-hyperlipidemic effects. Preformulation research was conducted. High-shear homogenisation and ultrasonication were used to prepare NLCs containing stearic acid (solid lipid), oleic acid (liquid lipid), and varying amounts of Tween 80 and Poloxamer 188 as surfactants. Nine formulations were prepared using a 32 factorial design and evaluated for size, zeta, scanning electron microscopy, entrapment efficiency, release, and kinetics. The optimum formulation was further evaluated for in vivo antihyperlipidemic activity in rats, and the in vitro release profile and stability of the commercial preparation were assessed. The optimised formulation (F4) exhibited an entrapment efficiency of 98.35%, a zeta potential of -65.9 mV, and a particle size of 203.0 nm. Scanning electron microscopy revealed that the particles were spherical and exhibited sustained in vitro drug release (96.4% over 12 h). In vivo evaluation in hyperlipidemic Wistar rats showed significantly improved lipid profiles and reduced oxidative stress compared to marketed pravastatin tablets. Stability studies confirmed that the formulation was stable under various conditions, and release studies showed sustained release compared with the marketed formulation. These findings suggest that pravastatin-loaded NLCs are promising sustained-release systems for improved management of hyperlipidaemia.
期刊介绍：
Journal of Drug Targeting publishes papers and reviews on all aspects of drug delivery and targeting for molecular and macromolecular drugs including the design and characterization of carrier systems (whether colloidal, protein or polymeric) for both vitro and/or in vivo applications of these drugs.
Papers are not restricted to drugs delivered by way of a carrier, but also include studies on molecular and macromolecular drugs that are designed to target specific cellular or extra-cellular molecules. As such the journal publishes results on the activity, delivery and targeting of therapeutic peptides/proteins and nucleic acids including genes/plasmid DNA, gene silencing nucleic acids (e.g. small interfering (si)RNA, antisense oligonucleotides, ribozymes, DNAzymes), as well as aptamers, mononucleotides and monoclonal antibodies and their conjugates. The diagnostic application of targeting technologies as well as targeted delivery of diagnostic and imaging agents also fall within the scope of the journal. In addition, papers are sought on self-regulating systems, systems responsive to their environment and to external stimuli and those that can produce programmed, pulsed and otherwise complex delivery patterns.
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