Search

The present study aimed to develop a surface-modified biocompatible nanostructured lipid carrier (NLCs) system using polyoxyethylene (40) stearate (POE-40-S) to improve the oral bioavailability of poorly water-soluble Biopharmaceutics Classification System class-II drug like tamoxifen (TMX). Also aimed to screen the most influential factors affecting the particle size (PS) using Taguchi (L12 (211)) orthogonal array design (TgL12OA). Then, to optimize the TMX loaded POE-40-S (P) surface-modified NLCs (TMX-loaded-PEG-40-S coated NLC (PNLCs) or PNLCs) by central composite design (CCD) using a four-factor, five-level model. The most influential factors affecting the PS was screened and optimized. The in-vitro study showed that increased drug-loading (DL) and encapsulation efficiency (EE), decreased PS and charge, sustained drug release for the prolonged period of the time with good stability and suppressed protein adsorption. The Ex-vivo study showed that decreased mucous binding with five-fold enhanced permeability of PNLC formulation after surface modification with POE-40-S. The in-vitro cytotoxicity study showed that the blank carrier is biocompatible and cytotoxicity of the formulation was dependent on the concentration of the drug. Finally, it can be concluded that the surface-modified PNLCs formulation was an effective, biocompatible, stable formulation in the enhancement of dissolution rate, solubility, stability with reduced mucus adhesion and increased permeability thereby which indicates its enhanced oral bioavailability.

Background:The high molecular weight and increasing lipophilicity drug face many problems starting from the drug development to formulation and conduction of pharmacological, toxicological and pharmacokinetic studies to its biological application. To overcome this problem, a different formulation of nano-sized drugs was developed recently. The use of Solid lipid nanoparticles (SLNs) and Nanostructured lipid carriers (NLCs) offers new insight into the formulation of the poorly soluble drug.Objective:The study aimed to investigate the literature with regard to the development of SLNs and NLCs for lipid-based nano drug delivery of poorly soluble drugs, with a view to identifying the factors influencing the optimization of the formulation of SLNs and NLCs and strategies to decrease the use of organic solvent during the preparation.Results:This review highlights the simple and easily scaled-up novel lipid nanoparticles (SLNs and NLCs) and their factors to be considered in the formulation for the proper selection of excipients. Also, this review summarizes the research findings reported by the different researchers regarding the principle formulation components, different preparation techniques, characterization, and toxicology of lipid nanoparticles.Conclusion:The SLNs/NLCs make this drug delivery system as one of the promising delivery systems, and safe colloidal lipid carriers for the delivery of poorly soluble drug and will be a solution to the formulation scientist for the solubility and permeability problem associated with the drugs to assure its good bioavailability.

In today's drug development world, combinatorial chemistry, high-throughput screening, and genomics have provided a technologic platform that produces a large number of new chemical entities with therapeutic potential each year. Its outcome the new chemical entities shifted towards higher molecular weight and increasing lipophilicity that results in poor water solubility which primarily affects the bioavailability of orally administered drugs. Hence, the poor aqueous solubility not only limits the drug's biological application but also challenges its pharmaceutical development. This review highlights the significant solubility problem and BCS/BDDCS formulation choices, and importance of lipid nanoparticles (LNPs). Also, this review summarizes the fate of lipid and lipid formulations in the human body, Lymphatic transport of drugs in the human body, Challenges of lipid-based delivery, the role of lipids in the enhancement of bioavailability, Mechanism of Lipid nanoparticles and BCS class II drugs as an ideal candidate for the LNPs formulation with their significant finding in research outcomes reported by the different researchers. Based on the available data, the lipid nanoparticles makes this drug delivery systems as one of the promising delivery systems and will be a solution to the formulation scientist. Also, it complies the key objectives of Green chemistry and sustainable chemistry. Keywords: Solubility, BCS/BDDCS, Lipid nanoparticles, BCS class II drugs