46911-83-5Relevant articles and documents
Synthesis of α-Amino Acid N-Carboxyanhydrides
Laconde, Guillaume,Amblard, Muriel,Martinez, Jean
, p. 6412 - 6416 (2021/08/30)
A simple phosgene- and halogen-free method for synthesizing α-amino acid N-carboxyanhydrides (NCAs) is described. The reaction between Boc-protected α-amino acids and T3P reagent gave the corresponding NCA derivatives in good yield and purity with no detectable epimerization. The process is safe, is easy-to-operate, and does not require any specific installation. It generates nontoxic, easy to remove byproducts. It can apply to the preparation of NCAs for the on-demand on-site production of either little or large quantities.
Block copolymer [(l-GluA-5-BE)-: B -(l-AspA-4-BE)]-based nanoflower capsules with thermosensitive morphology and pH-responsive drug release for cancer therapy
Amgoth, Chander,Chen, Shuai,Malavath, Tirupathi,Tang, Guping
supporting information, p. 9258 - 9268 (2020/11/03)
Herein, the synthesis of an amino-acid-based di-block copolymer (di-BCP) in-between an l-glutamic acid-5-benzyl ester and l-aspartic acid-4-benzyl ester [(l-GluA-5-BE)-b-(l-AspA-4-BE)] has been reported. However, the synthesis of di-BCP of [(l-GluA-5-BE)-b-(l-AspA-4-BE)] was carried out through the facile modified ring-opening polymerization (ROP) without using any surfactants and harmful chemicals. Interestingly, the synthesized [(l-GluA-5-BE)-b-(l-AspA-4-BE)] has been used to design nanoflower capsules (NFCs) with surface-functionalized nanoflakes and petals. Notably, the simple solvent propanol has been used as a dispersing medium for the di-BCP-based powder to observe morphology of NFCs. Moreover, these amino-acid-based NFCs are biocompatible, biodegradable, and bio-safe for mankind usage. Consequently, di-BCP-based NFCs show changes in morphology with different temperature conditions, i.e., at ~10 °C, ~25 °C (RT), and ~37 °C (body temperature). Furthermore, the average thickness of the surface-functionalized nanopetals has been calculated as ~324 nm (in diameter). Similarly, the average distance between petals is calculated as 3.6 μm and the pore depth is ~21 nm. Additionally, the porosity throughout the surface of capsules in-between nanopetals is an advantageous characteristic feature to improve the drug/paclitaxel (PTX) loading capacity. It is a unique and novel approach to design NFCs, which are a potential payload for nanomedicine and cancer therapy. Furthermore, NFCs were used to evaluate the loading efficacy of drugs and showed ~78% (wt/wt%) of the PTX loading. Moreover, NFCs showed ~74% drug release at physiological body temperature. Thus, NFCs showed remarkable release at acidic pH medium. However, PTX released from NFCs showed greater cell inhibition (i.e., ~79%) with an increase of the PTX concentration after 24 h incubation over HeLa (human epithelial cervical cancer) cells. Besides, PTX released from NFC showed significant (~34%) cell killing capacity. Such promising NFCs are recommended for breast, liver, and lung cancer therapeutics.
Preparation method of drug-loaded nano-micelle capable of releasing anti-cancer drug in tumor matrix as well as product and application of drug-loaded nano-micelle
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Paragraph 0058-0060, (2019/12/25)
The invention relates to a preparation method of a drug-loaded nano-micelle capable of releasing an anti-cancer drug in a tumor matrix as well as a product and an application of the drug-loaded nano-micelle, which belongs to the technical field of drug carriers. The preparation method comprises the following steps: the beta-benzyl aspartate is prepared, benzyloxycarbonyl aspartic anhydride is prepared, a polyaspartic acid benzyl ester polymer is prepared, a carboxylation-polyaspartic acid benzyl ester polymer is prepared, a carboxyl-polyaspartic acid dimethylethylenediamine polymer is prepared, a polyaspartic acid dimethylethylenediamine-polyaspartic acid benzyl ester polymer is prepared, a poly(aspartic acid-dimethylethylenediamine)-poly (aspartic acid-mercaptoethylamine) polymer is prepared, and drug-loaded nano-micelle for releasing an anti-cancer drug in a tumor matrix is prepared. The drug-loaded nano-micelle prepared by the preparation method has double sensitivities of pH sensitivity and reduction sensitivity, can accurately release drugs, and effectively improves the tumor treatment effect.