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.     

Structure and Performance Modulation of Self-Adhesive SIS/C5 Electrospun Membranes for Transdermal Drug Delivery北大核心CSCD

Electrospun membranes are widely utilized to enhance the water vapor permeability and drug delivery performance of transdermal drug delivery patches. Due to the lack of adhesion property,however,most of them cannot closely contact with skin,which impedes the delivery of drugs to the skin,thus affecting the transdermal administration. C5 resin is used to endow poly（styrene isoprene styrene）（SIS）electrospun membranes with pressure-sensitive adhesion property. Investigation is performed on how to control the structure,adhesion properties and drug delivery performance of SIS/C5 electrospun membranes loaded with synthetic capsaicin via compositions,drugs and electrospinning conditions. The results demonstrate that the electrospun membrane with a SIS/C5 ratio of 2∶1 has excellent water vapor permeability（7. 17×10－3 g/（h·cm2）and adhesion properties（180（°）peel strength is 0. 2 kN/m,tack force is 0. 64 N/cm2 ,holding power is greater than 7 days）. The synthetic capsaicin has good compatibility with the SIS/C5 electrospun membranes,in which no drug crystallizes and the drug loading is beneficial to improve the water vapor permeability. As the drug loading is 8%,the tack force is 0. 6～0. 8 N/cm2 ,the 180（°）peel strength is 0. 2～0. 3 kN/m,the holding power is greater than 7 days,and no residue is left during peeling tests. In vitro drug release indicates that the drug has a behavior of sustained release with a 24-hour cumulative release rate of greater than 50% for all SIS/ C5 electrospun membranes,meeting the requirements of transdermal drug delivery patches. © 2022, Science Press (China). All rights reserved.     

Self-assembly in magnetic supramolecular hydrogels

Most recent advances in the synthesis of supramolecular hydrogels based on low molecular weight gelators (LMWGs) have focused on the development of novel hybrid hydrogels, combining LMWGs and different additives. The dynamic nature of the noncovalent interactions of supramolecular hydrogels, together with the specific properties of the additives included in the formulation, allow these novel hybrid hydrogels to present interesting features, such as stimuli-responsiveness, gel-sol reversibility, self-healing and thixotropy, which make them very appealing for multiple biomedical and biotechnological applications. In particular, the inclusion of magnetic nanoparticles in the hydrogel matrix results in magnetic hydrogels, a particular type of stimuli-responsive materials that respond to applied magnetic fields. This review focuses on the recent advances in the development of magnetic supramolecular hydrogels, with special emphasis in the role of the magnetic nanoparticles in the self-assembly process, as well as in the exciting applications of these materials.     

Effect of thermal annealing on a bilayer polyvinyl alcohol/polyacrylic acid electrospun hydrogel nanofibres loaded with doxorubicin and clarithromycin for a synergism effect against osteosarcoma cells

Polyvinyl alcohol/polyacrylic acid (PVA/PAA) bilayer hydrogel nanofibres were successfully fabricated by electrospinning and physically crosslinked via heat treatment. The effects of the thermal annealing process on the structure, morphology, swelling, thermal properties and hydrophilicity of electrospun nanofibres were investigated. In addition, these membranes were also used to incorporate doxorubicin and clarithromycin for osteosarcoma treatment, one in each layer. These drugs were used because it is hypothesized in this work that a synergism occurs between both drugs. So, these membranes were analyzed towards their dual-drug release and potential cytotoxicity towards the U2OS human osteosarcoma cell line. Moreover, the water contact angle, disintegration, swelling and weight loss studies confirmed the rapid swelling and improved water stability of the annealed PVA/PAA bilayer nanofibres. The annealed bilayer nanofibres exhibited an increase in the average diameter and degree of crystallinity. In addition, the results revealed that a variation occurred in the degree of hydrophilicity of annealed PVA/PAA bilayer nanofibres. The PAA nanofibres surface exhibited higher hydrophilicity than the PVA nanofibres surface. Drug delivery presented to be as fast rate release for clarithromycin and slow-rate release for doxorubicin, which may be advantageous because both drugs exhibited to be synergetic for certain dosages presenting the combination of the drugs higher than 50% of cell inhibition, while these membranes had higher inhibition values (up to 90%), which was attributed to the PAA but also the drugs. These unique properties are of potential interest in drug delivery applications for dual drug delivery where the tunability of surfaces is desirable.     

Gelatin-coated gold nanoparticles as an effective pH-sensitive methotrexate drug delivery system for breast cancer treatment

The present study investigates the synthesis and effectiveness of gold/gelatin nanoparticles (NPs) biopolymer as a carrier for methotrexate (MTX) drug. Two different shapes of gold particles, including spherical AuNPs (50 & 100 nm) and gold nanorods (AuNRs) with three different sizes (20, 50 and 100 nm length) were synthesized using the chemical reduction method. The effect of AuNPs size and shape on the entrapment efficiency (E.E), the release rate of the drug, and cellular uptake were investigated. The surfaces of both AuNPs and AuNRs were coated with a gelatin biopolymer, and the stability and property of the generated compounds were studied. Moreover, MTX as a chemotherapeutic agent was loaded on the gelatin-coated AuNPs/AuNRs complexes. The physicochemical properties of the gelatin-coated AuNPs/AuNRs complexes were studied using ultraviolet-visible (UV–Vis) spectroscopy, dynamic light scattering (DLS), scanning electron microscopy (SEM), transmission electron microscopy (TEM), and Fourier transform infrared (FT-IR) spectroscopy. The E.E and MTX release behavior from the complexes at pH values of 7.4 and 5.4 and temperatures of 37 and 40 °C were investigated in vitro. The cytotoxic effects of AuNPs, AuNPs-Gelatin, AuNPs-Gelatin-MTX, AuNRs, AuNRs-Gelatin, AuNRs-Gelatin-MTX and free MTX were studied. The results indicated that the E.E of AuNPs was higher than that of AuNRs. The highest release rate of the drug was related to the AuNR1-gelatin complex (pH 5.4 and temperature of 40 °C). In addition, MTX loaded AuNR2-gelatin showed the highest cytotoxic effect on the MCF-7 breast cancer cell line so that even its cell cytotoxicity was more than that of the free drug.     

Synthesis,spectral and quantum mechanical studies and molecular docking studies of Schiff base (E)2-hydroxy-5-(((4-(N-pyrimidin-2-yl)sulfamoyl)phenyl)imino)methyl benzoic acid from 5-formyl salicylic acid and sulfadiazine

A new Schiff base (E)2-hydroxy-5-(((4-(N-pyrimidin-2-yl)sulfamoyl)phenyl)imino)methyl benzoic acid (5FSADA) compound was synthesized by condensation of 5-formyl salicylic acid and sulfadiazine, and the product formed was characterized using FTIR and UV–Visible spectroscopy. The geometry was optimized using DFT. The FTIR were computed from DFT and is compared with experimental spectra, followed by detailed vibrational assignment, which shows that the experimental and simulated data is in close agreement. The UV–Vis spectrum calculated using TD-DFT, IEFPCM solvation model with DMSO as solvent. Wave function based properties like localized orbital locator, electron localization function and non-covalent interactions has been studied extensively. The physical properties (ADMET) of the compound 5FSADA indicated that the compound has excellent drug likeness and PASS studies showed that it has anti-infective properties, which is confirmed by a docking score of −9.0 ​kcal/mol.     

The intragastrointestinal fate of paclitaxel-loaded micelles: Implications on oral drug delivery

The goal of the present study is to elucidate the intragastrointestinal fate of micellar delivery systems by monitoring fluorescently labeled different micelles and the model drug paclitaxel (PTX). Both in vitro and ex vivo leakage studies showed fast PTX release in fluids while micelles remained intact, except in fed-state simulated intestinal fluid and fasted-state pig intestinal fluid, thus referring to the intact absorption of micelles and PTX leakage in the gastrointestinal tract with d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) micelles showing higher stability than other micelles. All groups of micelles were absorbed intact in Caco-2 and Caco-2/HT29-MTX cell models and the absorption of TPGS micelles was found to be higher than other micelles. The transport of the micelles across Caco-2/Raji (1.6%–3.5%), Caco-2 (0.8%–1%), and Caco-2/HT29-MTX (0.58%–1%) cell monolayers further verified the absorption of micelles and their subsequent transport; however, more TPGS micelles transported across cell monolayers than other groups. Moreover, the histological examination also confirmed that micelles entered the enterocytes and were transported to basolateral tissues and TPGS showed the stronger ability of penetration than other groups. Thus, these results are succinctly presenting the absorption of intact micelles in GIT confirmed by imaging evidence with prior leakage of the drug, uptake by enterocytes and the transport of micelles that survive the digestion by enterocytes and mainly by microfold cells in material nature dependent way with TPGS showing better results than other groups. In conclusion, these results identify the mechanism by which the gastrointestinal tract processes micelles and point to the likely use of this approach in the design of micelles-based therapies.     

Fabrication,characterization and in vivo evaluation of dexpanthenol sustained-release nanofibers for wound healing

In this study, wound dressings consisting of dexpanthenol (Dex)-loaded electrospun nanofibers were fabricated using polyvinyl alcohol (PVA)/sodium alginate (SA), and chitosan as the core and the shell, respectively. Considering the remarkable properties of chitosan, it was used as a shell against drug release and to improve the thermal stability, and tensile strength of the scaffold. By comparing the thermogravimetric, and tensile strength results of nanofibers with and without shell, it was revealed that the presence of chitosan in the shell side could improve the thermal stability and increased the tensile strength by about three times. The isotherm models of dexpanthenol release from the PVA/SA/Dex-CS scaffold was best described by the Langmuir model. Besides, Fourier transform infrared, scanning electron microscopy, and X-ray diffraction techniques were performed to characterize nanofibers. Furthermore, an in vivo investigation of a wound dressing with dexpanthenol showed better healing compared to the wound dressings without dexpanthenol.     

Progress on intelligent hydrogels based on RAFT polymerization: Design strategy,fabrication and the applications for controlled drug delivery

Although intelligent hydrogels have shown bright potential application in biomedical fields,they were prepared by conventional methods and still face many serious challenges,such as uncontrollable stimulus-response and low response sensitivity.Recently,RAFT polymerization provides a versatile strategy for the fabrication of intelligent hydrogels with improved stimulus-response properties,owing to the ability to efficiently construct hydrogel precursors with well-defined structure,such as block copolymer,graft copolymer,star copolymer.In this review,we summarized the recent progress on intelligent hydrogels based on RAFT polymerization with emphasis on their fabrication strategies and applications for controlled drug delivery.     

Imitation of drug metabolism in cell co-culture microcapsule model using a microfluidic chip platform coupled to mass spectrometry

In this work,a multi-functional analysis platform by coupling a microfluidic chip to a mass spectrometry(MS) detector was described.We constructed a three-dimensional tumor-endothelial co-culture model for simulating drug resistance during tumor treatment.On this specially designed integrated platform,the first step was to prepare heterogeneous cell-encapsulated alginate microcapsules for threedimensional co-culture,and the second step was to achieve on-line perfusion culture and continuous drug stimulation on chip.It facilitates cell proliferation analysis and the collection of metabolism medium.After micro solid phase extraction column(SPE) pretreatment,subsequent mass spectrometry could detect drug metabolism.The high activity of two kinds of cells(A549 and HUVEC) shows the biocompatibility of the platform.Paclitaxel was used as a model drug,the distinctions of drug absorption between the mono-culture group and co-culture group were clearly observed by electrospray ionization quadrupole time-of-flight mass spectrometry(ESI-Q-TOF MS).Therefore,the integrated platform has shown promise as a high throughput,low cost for cell metabolism research and drug screening processes.