Preparation and physicochemical characterization of camptothecin conjugated poly amino ester–methyl ether poly ethylene glycol copolymer

Abstract

In the present study, camptothecin grafted poly amino ester-methyl ether polyethylene glycol (CPT-PEA-MPEG) as a novel copolymer was synthesized by Michael reaction at different ratios of MPEG and CPT (60 : 40 and 80 : 20). The microemulsion was used to prepare nanomicelles, and in vitro cytotoxicity was performed on the HT29 cell line, and cell survival was measured by MTT assay. The syntheses were confirmed by 1 H NMR and FT-IR. Several characterization methods including CMC, particle size, size distribution, and transmission electron microscopy were performed to evaluate features of prepared nanomicelles. Low critical micelle concentration, small particle size and IC 50 of 0.1 mg ml À1 at MPEG to CPT ratio of 60 : 40 make this micelle a promising drug delivery carrier. CPT-PAE-MPEG nanomicelles at a MPEG : CPT ratio of 60 : 40 can be a suitable choice to improve the physiochemical properties of CPT and its therapeutic effect, while it can be potentially used as a nano-carrier for other anticancer drugs to purpose a dual drug delivery.

All-Trans Retinoic Acid Grafted Poly Beta-Amino Ester Nanoparticles: A Novel Anti-angiogenic Drug Delivery System

“…The purified product was dried in a vacuum oven. 16 The final ATRA-g-PBAE copolymer (4) was synthesized with a yield of 50%. The reaction is shown in Figure 1, and the structure was proved by FT-IR, 1…”

“…13 PBAEs have low cytotoxicity and pH-responsive solubility profile, 14 which make them an excellent candidate for gene delivery 15 and cytoplasmic delivery of anti-cancer drugs in the form of nano-carrier. 16 Particle size and surface charge of nano-carriers are key factors, which affect blood circulation time, tumor penetration, and cellular uptake of NPs. 17 Due to small size of NPs, they can increase blood circulation times leading to greater opportunity to accumulate at tumor sites and increasing therapeutic efficacy.…”