Effect of a nano-sized natural clinoptilolite modified by the hexadecyltrimethyl ammonium surfactant on cephalexin drug delivery

The use of porous materials as host systems for medical applications has been considered in recent years. The aim of this work is to construct an efficient adsorbent for the adsorption and delivering of cephalexin. For this pupose, pretreated natural nano-sized clinoptilolite (NZ) was modified by the cationic hexadecyltrimethyl ammonium surfactant (HDTMA), and the obtained modified zeolite nanoparticles (SMZ) were used to design systems for storage and release of cephalexin (CPX). The adsorbed and released extents of the drug onto/from the modified zeolite were determined by UV–Vis spectroscopy. The results showed that both decreasing the particle size of clinoptilolite and modifying its surface significantly increase the adsorbed drug extent. All the compounds were characterized by SEM, TEM, FT–IR, TG/DTG, and XRD. TG/DTG and also FT–IR results showed sufficient loading amounts of HDTMA and CPX onto the raw and modified zeolite, respectively. It was proven by means of TG that the composites are more stable thermally when the admicelles contain cephalexin in their interior. IR spectroscopy studies indicated that the zeolite structure remained unchanged after the modification with the surfactant and after the cephalexin drug has been loaded. Due to the presence of hydroxyl and amine groups in the cephalexin structure, pH plays an important role on the adsorbed CPX extent, so that the maximum adsorbed CPX was observed at pH = 12. While the delivery of CPX was better at pH = 2, because at alkaline pHs, the anionic carboxylate form of CPX has higher attractive force with the positive head of the surfactant on the SMZ. Hence, the stomach's acidic pH is appropriate for drug delivery. The effects of some cations in the delivery extent confirm that the diet can significantly affect the delivery of the CPX from the proposed adsorbent.     

Thermo-responsive gelatin-functionalized PCL film surfaces for improvement of cell adhesion and intelligent recovery of gene-transfected cells

Efficient local gene transfection on a tissue scaffold is dependent on good cell-adhesion characteristics. In this work, the thermo-responsive gelatin-functionalized polycaprolactone (PCL) films were proposed for improvement of cell adhesion and intelligent recovery of gene-transfected cells. Functional copolymer brushes (PCL-g-P(NIPAAm-co-MAAS)) were first prepared via surface-initiated ATRP of N-isopropylacrylamide (NIPAAm) and methacrylic acid sodium salt (MAAS) from the initiator-funcationalized PCL surfaces. The pendant carboxyl end-groups of the PCL-g-P(NIPAAm-co-MAAS) surface were subsequently coupled with gelatin via carbodiimide chemistry to produce the thermo-responsive gelatin-functionalized PCL surface. The thermo-responsive gelatin-functionalized PCL film surface can improve cell adhesion and proliferation above the LCST of P(NIPAAm) without destroying cell detachment properties at lower temperatures. The dense transfected cells can be recovered simply by lowering culture temperature. The thermo-responsive gelatin-functionalized PCL films are potentially useful as intelligent adhesion modifiers for directing cellular functions within tissue scaffolds.     

Multiscale Control of Hierarchical Structure in Crystalline Block Copolymer Nanoparticles Using Microfluidics

Hierarchical semicrystalline block copolymer nanoparticles are produced in a segmented gas‐liquid microfluidic reactor with top‐down control of multiscale structural features, including nanoparticle morphologies, sizes, and internal crystallinities. Control of multiscale structure on disparate length scales by a single control variable (flow rate) enables tailoring of drug delivery nanoparticle function including release rates.

     

Duplex dual-labeled fluorescence probe-based melting curve and endpoint genotyping assays for genotyping of rs2000999 and haptoglobin gene deletion

Haptoglobin (Hp) is a hemoglobin-binding serum glycoprotein. Some variations in the Hp gene (HP) or Hp-related gene (HPR), including a single-nucleotide polymorphism in intron 2 of HRP, rs2000999, and a complete deletion of the HP gene (HP^del), one of the rare variants of HP, have been reported to correlate with the serum cholesterol concentration as well as the serum Hp concentration. In this study, we developed a duplex dual-labeled fluorescence probe-based method to simultaneously determine the rs2000999 G > A polymorphism by melting curve genotyping and the zygosity of HP^del by endpoint genotyping. This method was then validated by using the genomic DNA from 94 Japanese subjects for whom genotypes of rs2000999 and HP^del zygosity had already been determined. The results obtained with this method were in perfect agreement with the previous ones. Thus, the present method enables us to estimate these two polymorphisms in relatively large-scale groups of subjects, especially in Asian populations where the HP^del is distributed.     

近红外二区活体荧光成像在肿瘤诊疗中的应用

由于具备组织穿透深度深和时空分辨率高等优势, 近年来近红外二区(Near-infrared-Ⅱ, NIR-Ⅱ, 1000~1700 nm)荧光成像技术得到了快速发展, 其在肿瘤临床诊断和治疗的潜力更是引发了广泛关注. 本文首先阐释了NIR-Ⅱ窗口荧光成像的原理及其优势, 随后根据结构分类归纳总结了现有荧光团的特征, 重点介绍了荧光探针在性能优化上的进展以及在肿瘤早期检测、 术中导航和光疗中的应用, 最后讨论了现有NIR-Ⅱ 荧光探针的局限以及临床转化面临的挑战, 并对未来的发展方向进行了展望.     

Theoretical investigation of functionalized fullerene nano carrier drug delivery of fluoxetine

In recent years, fullerene nanoparticles have received extensive attention due to their unique physical and chemical properties. Properly modified fullerene nanoparticles have excellent biocompatibility and significant anti-tumor activity and anti-depression, which makes them have broad application prospects in the field of cancer anti-depression. The present study used the density functional theory (DFT) calculations to perform a theoretical examination of the interaction of fluoxetine (F) as medicine with the functionalized fullerene O and NO (F–O and F–NO surface in gas phase physiological media. According to DFT calculations, adsorption energies were ?3396.6350645, ?3540.2952907, ?6778.526894, and ?6952.251487 kJ for F/P complexes (fullerene O and NO (F–O and F–NO surface) respectively, proposing the possibility of the adsorption process of F molecule onto the fullerene surface concerning the energetic perspective. Calculations of electronic parameters aimed at determining the molecule's reactivity. Bandgap of F–O and F–NO were 0.03715, 0.04328 respectively, by this value we can recognize the reactivity of complexes.     

Characterization and in vitro release kinetics of chitosan based biocomposites from Scotch Bonnets

The main aim of this study is to formulate the combination of the bioactive composite containing chitosan/β -tricalcium phosphate (CH/β-TCP) as potential drug delivery platforms for the sustained release of antibiotics. Herein the mode of amoxicillin (AMX) maintained in the β-TCP/chitosan composite was characterized using XRD, FT-IR to confirm the phase purity and functional groups. SEM was used to examine the size and shape of particles. The SEM images of the biocomposites after drug release confirmed that they are biodegradable. In vitro drug release experiments in PBS (pH 7.4) revealed a sustained release profile in a neutral medium. Drug release profiles were evaluated according to five different kinetic models including Zero Order, First Order, Higuchi, Hixon Crowel, and Korsmeyer-Peppas. The release profile was best expressed by the Korsmeyer Peppas model because the results showed high linearity. Overall, the positive effect of chitosan coating on the drug elution profile of β-TCP as carriers for the controlled delivery of antibiotics was regarded as biocompatible for the controlled drug delivery system.     

Microgels as drug carriers for sonopharmacology

The ultrasound-induced cleavage of covalent and non-covalent bonds to activate drugs (sonopharmacology) is a promising concept to gain control over the action of active pharmaceutical ingredients by an external trigger. Previously, linear polymer architectures bearing drug payloads were exploited for drug release by using the principles of polymer mechanochemistry. In this work, the carrier design is altered by the polymer topology to improve the ultrasound-triggered release of covalently anchored drugs from polymer scaffolds. We use microgels crosslinked by mechanoresponsive disulfides and copolymerized with Diels-Alder adducts of furylated payload molecules and acetylenedicarboxylate. Force-induced thiol formation induces a Michael-type addition liberating the payload from the microgels. The use of microgels significantly reduces sonication times compared to linear polymer chains and shields the cargo efficiently from non-triggered activation using ultrasound that produces inertial cavitation at a frequency of 20 kHz as model condition.     

肉豆蔻酸单萜醇酯对布南色林经皮透过的影响

本文以环状单萜醇α-萜品醇、L-薄荷醇及链状单萜醇香叶醇、香茅醇为先导化合物,采用酰氯酯化法合成肉豆蔻酸α-萜品醇酯(TER-C14)、肉豆蔻酸-L-薄荷醇酯(MEN-C14)、肉豆蔻酸香叶醇酯(GER-C14)和肉豆蔻酸香茅醇酯(CIT-C14),并考察单萜醇及其肉豆蔻酯作为促透剂对布南色林(Blo)的促透效果。通过体外经皮渗透实验、体外释放实验和分子模拟技术初步探究单萜醇及其肉豆蔻酯的促透机制。结果显示,当GER-C14或CIT-C14为促透剂时,均有显著的促透效果(P<0.05),并且24h经皮累积透过量是空白组的4.84倍和4.45倍。促透机制为肉豆蔻酸单萜醇酯破坏药物与神经酰胺之间的氢键相互作用,增加脂质迁移率和药物的自由能,从而促进药物的渗透。肉豆蔻酸单萜醇酯有望作为新型促透剂在经皮给药系统中广泛应用。