scholarly journals Thiol-ene Reaction: An Efficient Tool to Design Lipophilic Polyphosphoesters for Drug Delivery Systems

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1750
Author(s):  
Stéphanie Vanslambrouck ◽  
Raphaël Riva ◽  
Bernard Ucakar ◽  
Véronique Préat ◽  
Mick Gagliardi ◽  
...  
Keyword(s):  
Click Reaction ◽  
Drug Loading ◽  
Water Soluble ◽  
Amphiphilic Copolymers ◽  
Poorly Water Soluble Drugs ◽  
Ene Reaction ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Poly Ethylene

Poly(ethylene glycol)-b-polyphosphoester (PEG-b-PPE) block copolymer nanoparticles are promising carriers for poorly water soluble drugs. To enhance the drug loading capacity and efficiency of such micelles, a strategy was investigated for increasing the lipophilicity of the PPE block of these PEG-b-PPE amphiphilic copolymers. A PEG-b-PPE copolymer bearing pendant vinyl groups along the PPE block was synthesized and then modified by thiol-ene click reaction with thiols bearing either a long linear alkyl chain (dodecyl) or a tocopherol moiety. Ketoconazole was used as model for hydrophobic drugs. Comparison of the drug loading with PEG-b-PPE bearing shorter pendant groups is reported evidencing the key role of the structure of the pendant group on the PPE backbone. Finally, a first evidence of the biocompatibility of these novel PEG-b-PPE copolymers was achieved by performing cytotoxicity tests. The PEG-b-PPE derived by tocopherol was evidenced as particularly promising as delivery system of poorly water-soluble drugs.

scholarly journals Insoluble Polymers in Solid Dispersions for Improving Bioavailability of Poorly Water-Soluble Drugs

Polymers ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 1679
Author(s):  
Thao T.D. Tran ◽  
Phuong H.L. Tran
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Insoluble Polymers

In recent decades, solid dispersions have been demonstrated as an effective approach for improving the bioavailability of poorly water-soluble drugs, as have solid dispersion techniques that include the application of nanotechnology. Many studies have reported on the ability to change drug crystallinity and molecular interactions to enhance the dissolution rate of solid dispersions using hydrophilic carriers. However, numerous studies have indicated that insoluble carriers are also promising excipients in solid dispersions. In this report, an overview of solid dispersion strategies involving insoluble carriers has been provided. In addition to the role of solubility and dissolution enhancement, the perspectives of the use of these polymers in controlled release solid dispersions have been classified and discussed. Moreover, the compatibility between methods and carriers and between drug and carrier is mentioned. In general, this report on solid dispersions using insoluble carriers could provide a specific approach and/or a selection of these polymers for further formulation development and clinical applications.

scholarly journals Cyclodextrin Based Nanoparticles for Drug Delivery and Theranostics

2020 ◽  
Vol 10 (2) ◽  
pp. 166-183 ◽  
Author(s):  
Dipak Dilip Gadade ◽  
Sanjay Sudhakar Pekamwar
Keyword(s):  
Drug Delivery ◽  
Targeted Drug Delivery ◽  
Drug Loading ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Solubility Profile ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Treatment Procedures ◽  
Consequent Improvement

Colloidal nanoparticulate technology has been described in the literature as a versatile drug delivery system. But it possesses some inherent lacunae in their formulation. Cyclodextrins (CDs) have been extensively reported for the solubility enhancement of poorly water-soluble drugs. The CDs can cause intervention in aspects related to nanoparticles (NPs) that include improving drug loading in nano-system, improving stability, site-specific/targeted drug delivery, improving solubility profile and absorption of the drug in nanosystem with consequent improvement in bioavailability, with the possibility of controlled release, safety and efficacy. They find application in for simultaneous diagnosis and therapeutics for better treatment procedures. The current communication is focused on the application of CDs to overcome troubles in nanoparticulate formulation and enhancement of their performance. It also envisages the theranostic aspects of CDs.

scholarly journals Molecular Interactions in Solid Dispersions of Poorly Water-Soluble Drugs

Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 745
Author(s):  
Thao T. D. Tran ◽  
Phuong H. L. Tran
Keyword(s):  
Molecular Interactions ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Potent Drug

Physicochemical characterization is a crucial step for the successful development of solid dispersions, including the determination of drug crystallinity and molecular interactions. Typically, the detection of molecular interactions will assist in the explanation of different drug performances (e.g., dissolution, solubility, stability) in solid dispersions. Various prominent reviews on solid dispersions have been reported recently. However, there is still no overview of recent techniques for evaluating the molecular interactions that occur within solid dispersions of poorly water-soluble drugs. In this review, we aim to overview common methods that have been used for solid dispersions to identify different bond formations and forces via the determination of interaction energy. In addition, a brief background on the important role of molecular interactions will also be described. The summary and discussion of methods used in the determination of molecular interactions will contribute to further developments in solid dispersions, especially for quick and potent drug delivery applications.

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