Numerous drugs have emerged to treat various diseases, such as COVID-19, cancer, and protect human health. Approximately 40% of them are lipophilic and are used for treating diseases through various delivery routes, including skin absorption, oral administration, and injection. However, as lipophilic drugs have a low solubility in the human body, drug delivery systems (DDSs) are being actively developed to increase drug bioavailability. Liposomes, micro-sponges, and polymer-based nanoparticles have been proposed as DDS carriers for lipophilic drugs. However, their instability, cytotoxicity, and lack of targeting ability limit their commercialization. Lipid nanoparticles (LNPs) have fewer side effects, excellent biocompatibility, and high physical stability. LNPs are considered efficient vehicles of lipophilic drugs owing to their lipid-based internal structure. In addition, recent LNP studies suggest that the bioavailability of LNP can be increased through surface modifications, such as PEGylation, chitosan, and surfactant protein coating. Thus, their combinations have an abundant utilization potential in the fields of DDSs for carrying lipophilic drugs. In this review, the functions and efficiencies of various types of LNPs and surface modifications developed to optimize lipophilic drug delivery are discussed.

/pdf/recent-progress-of-lipid-nanoparticles-based-lipophilic-drug-23umxd8r.pdf

Recent Progress of Lipid Nanoparticles-Based Lipophilic Drug Delivery: Focus on Surface Modifications

Polyethylene glycol (PEG) is an industrial commodity produced for applications foremost in the medial and personal care business. This review focuses on the much less explored application of using PEG as a chemical solvent. This review highlights some of the successful chemical synthesis strategies to illustrate the advantages of using PEG as an environmentally friendly reaction medium. These advantages include its ability to (a) dissolve a wide range of chemicals including mineral salts, (b) serve as a catalyst because of its acid/base functionalities, (c) complex metal cations, and (d) engage in redox chemistry. New developments of combining PEG with other green solvents and/or functionalizing PEGs are covered as well. The present state of physicochemical studies of PEG as a solvent is also provided and clearly shows the need for future research in this area to further promote the effective use of PEG as a medium for chemistry. 

http://manuscript.elsevier.com/S1359029421001217/pdf/S1359029421001217.pdf

Polyethylene glycol as a green chemical solvent

Abstract Target-site drug delivery systems are gaining interest in the pharmaceutical field due to their great advantages, such as higher drug dosing capacity and better bioavailability. However, some existing problems need to be overcome. An example, is the interaction between blood proteins and drug delivery systems. A potent candidate to approach the mentioned problem is based on polyethylene glycol (PEG) surface modifications. This polymer acts as a protector against the external possible interactions with other compounds, making targeted delivery possible. Diseases such as cancer, diabetes, hemophilia and pain treatment can benefit from these new systems. This review aims to give an overview of drug delivery systems based on PEGylation as surface modification as the pharmaceutical approach. Moreover, a deeper insight into the properties of PEG and its advantages is given, as well as a brief overview of present therapies based on this technology.

https://www.tandfonline.com/doi/pdf/10.1080/03639045.2022.2101062?needAccess=true

PEGylated drug delivery systems in the pharmaceutical field: past, present and future perspective

Objective The emergence of multi-drug resistance (MDR) in esophageal carcinoma has severely affected the effect of chemotherapy and shortened the survival of patients. To this end, we intend to develop a biomimetic nano-targeting drug modified by cancer cell membrane, and investigate its therapeutic effect. Methods The degradable poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) co-loaded with doxorubicin (DOX) and curcumin (Cur) were prepared by solvent evaporation method. TE10 cell membrane and Distearoyl phosphatidylethanolamine-polyethylene glycol (DSPE-PEG) were then coated on the PLGA NPs by membrane extrusion to prepare the PEG-TE10@PLGA@DOX-Cur NPs (PMPNs). Size and zeta potential of the PMPNs were analyzed by lazer particle analyzer, and the morphology of PMPNs was observed by transmission electron microscope. The TE10 cell membrane protein on PMPNs was analyzed by gel electrophoresis. The DOX-resistant esophageal cancer cell model TE10/DOX was established through high-dose induction. The In vitro homologous targeting ability of PMPNs was evaluated by cell uptake assay, and the in vitro anti-tumor effect of PMPNs was assessed through CCK-8, clone formation and flow cytometry. A Balb/c mouse model of TE10/DOX xenograft was constructed to evaluate the anti-tumor effect in vivo and the bio-safety of PMPNs. Results The prepared cell membrane coated PMPNs had a regular spherical structure with an average diameter of 177 nm. PMPNs could directly target TE10 and TE10/DOX cells or TE10/DOX xenografted tumor and effectively inhibit the growth of DOX-resistant esophageal carcinoma. Besides, the PMPNs was confirmed to have high biosafety. Conclusion In this study, a targeted biomimetic nano-drug delivery system PMPNs was successfully prepared, which overcome the MDR of esophageal carcinoma by co-delivering DOX and sensitizer curcumin.

/pdf/surface-pegylated-cancer-cell-membrane-coated-nanoparticles-3jexr0nphp.pdf

Surface PEGylated Cancer Cell Membrane-Coated Nanoparticles for Codelivery of Curcumin and Doxorubicin for the Treatment of Multidrug Resistant Esophageal Carcinoma.

Abstract Background and aim The study was to extend systemic circulation and biological half-life (t1/2) of trans-resveratrol (RSV) using solid lipid nanoparticles (RSV-SLN) to improve its anti-cancer potential. Methods RSV-SLN was prepared by solvent emulsification evaporation technique and proceeded for evaluation like particle size, PDI, zeta potential, in vitro release, in vitro cytotoxicity, cellular internalisation, haemolysis and erythrocyte membrane integrity, platelet aggregation and pharmacokinetic studies in rats. Moreover, cancer cells accumulation of RSV-SLN also needs to be evaluated for proving their targeting ability. Result Prepared SLN showed 126.85 ± 12.09 nm particle size, −24.23 ± 3.27 mV Zeta potential and 74.67 ± 4.76%. release at 48 h and haemocompatible. The cellular internalisation image showed the SLN reach in a cytoplasm and nucleus of PC3 prostate cells. RSV-SLN exhibited high t1/2 (8.22 ± 1.36 h) and 7.19 ± 0.69 h MRT (Mean residence time) and lower clearance i.e. 286.42 ± 13.64 mL/min/kg. The bio-distribution of RSV-SLN was found to be extremely high in prostate cells and accumulate 7.56 times greater than that of RSV solution. Conclusion The developed RSV-SLN can be applied as potential carrier for delivery of drug of chemotherapeutics at an extend systemic circulation and targeting efficiency at tumour site.

Development, evaluation, pharmacokinetic and biodistribution estimation of resveratrol-loaded solid lipid nanoparticles for prostate cancer targeting

PEGylation is the covalent addition of PEG to one more molecule. PEGylation can improve the maintenance time of the therapeutics similar to proteins, liposomes, and nanoparticle through shielding them beside different debasing mechanisms dynamic in a body that improve beneficial properties. This skill is used to get better half-life and other pharmaceutical properties of a protein, peptide, or non-peptide molecule. Polyethylene glycol is harmless, non-immunogenic, non-antigenic, and extremely soluble in water and FDA accepted polymer. It shows a significant role in drug delivery. A variety of PEG-based formulations are available in the market. This paper represents the benefits of PEGylation over non-PEGylated products. Now a day, PEGylation plays an important role in the drug delivery system. PEGylation increases the therapeutic potential of drugs.

PEGYLATION: an important approach for novel drug delivery system.

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PEGYLATION: an important approach for novel drug delivery system.