21568-87-6Relevant articles and documents
Designed proteinoid polymers and nanoparticles encapsulating risperidone for enhanced antipsychotic activity
Einat, H.,Grinberg, I.,Lugasi, L.,Margel, S.,Okun, E.,Rudnick-Glick, S.
, (2020)
Background: Nanoparticles (NPs) incorporating drug formulations can be used to facilitate passage through biological barriers including the blood–brain barrier (BBB) and increase drug delivery and bioavailability. Hence, NP-based administration may enhance the efficiency of current antipsychotics. Encapsulation within NPs can resolve aqueous solubility problems that not only reduce permeability through the BBB but also affect targeting. The present study describes a new drug delivery system based on proteinoid NPs to explore the possibility of improving drug efficacy. Risperidone (RSP) is a commonly used atypical antipsychotic medication, and was therefore selected for encapsulation by proteinoid NPs. Results: Proteinoid polymers with high molecular weight and low polydispersity were synthesized from l-amino acids and poly-l-lactic acid (PLLA) by thermal step-growth polymerization mechanism. RSP-loaded proteinoid NPs were then prepared using a self-assembly process in the presence of RSP, followed by PEGylation. The optimal PEGylated RSP-loaded NPs were characterized in terms of diameter and size distribution, drug loading, ζ-potential, cytotoxicity, biodistribution, and psychopharmacological effects. The findings indicate significantly higher antipsychotic activity of drug-loaded proteinoid NPs compared to free RSP. Conclusions: Proteinoid NPs enhance RSP delivery and may potentially increase drug efficiency by reducing dosage and side effects.[Figure not available: see fulltext.].
Chiral discrimination controlled by the solvent dielectric constant
Sakai, Kenichi,Sakurai, Rumiko,Hirayama, Noriaki
, p. 1073 - 1076 (2004)
Chiroselective molecular recognition accompanied by a change in configuration of a target substrate has been studied. (RS)-α-Amino-ε- caprolactam 1 was used as the target substrate to be resolved while N-tosyl-(S)-phenylalanine 2 was used as the chiral selector. The dielectric constant (ε) of the solvent was found to have a profound effect on the chiroselective molecular recognition. The specific chiral selector (S)-2 not only recognized both enantiomers (R)- and (S)-1 individually to be deposited as the less-soluble salt from the different solvent but also controlled the configuration and diastereomeric excess of the less-soluble diastereomeric salt by simple adjustment of the solvents dielectric constant. The chiroselective recognition mechanism was examined based on the crystal structures of the salts, (S)-1·(S)-2·H2O and (R)-1·(S)-2, obtained from the resolution process.
Design, synthesis and properties investigation of Nα-acylation lysine based derivatives
Shi, Ting-Ting,Fang, Zheng,Zeng, Wen-Bo,Yang, Zhao,He, Wei,Guo, Kai
, p. 7587 - 7593 (2019)
Amino acid-based compounds have attracted attention as environmentally friendly bio-based materials. Our group has recently developed a novel family of Nα-acylation lysine based derivatives. We introduced long chain acyl groups at the Nα position selectively by a new synthetic route that avoided the process of amino protection and deprotection. Sodium Nα-octanamide lysine (C8), sodium Nα-capramide lysine (C10) and sodium Nα-lauramide lysine (C12) can self-assemble into vesicles spontaneously. As a result, not only do they have potential in drug delivery system but also they may be used as bio-based surfactants applied in cosmetics and other industries.
PROTEINOID COMPOUNDS, PROCESS OF PREPARING SAME AND USES THEREOF
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Sheet 23 of 36, (2017/04/11)
Proteinoid compounds characterized by a molecular weight (Mw) of at least 15,000 Da, processes of preparing such compounds and methods of use thereof, are provided. A method of monitoring the presence and metastases of cancer in a body of an individual is further disclosed.
