A living therapeutic system based on attenuated Salmonella was developed via metabolic engineering using an aggregation-induced emission (AIE) photosensitizer MA. The engineered bacterial could localize in the tumor tissues and...
Herein, the various polymer properties and the underlying mechanism for the functionalization and surface modification of polymer nanoparticles have been discussed. There are numerous polymer particles designed and developed for various applications. The synthesis and characterization of different types of polymers followed by the engineering of nanoparticles and capsules depend on various factors. There are too many polymerization methods approached for the development of nanoparticles with desired surface properties. The ring-opening polymerization (ROP), emulsion polymerization (EP), atom transfer radical polymerization (ATRP), and free radical micro initiation are the significant approaches for the polymerization reactions. The polymer nanoparticle functionalization and modification of their surfaces based on requirements is an essential task. The solvent concentration, pH, temperature, and sonication have played a vital role to tune the morphology of polymer nanoparticles and capsules. Different characterizations such as FTIR, NMR (1 H and 13 C), HRMS, and MALDI-TOF are used for preliminary structural and confirmations. Further, SEM, FE-SEM, TEM, AFM, BET, XRD, Raman, EDAX, TGA-DSC, DLS, and zeta potential were used for morphological and thermal properties.
We have proposed and classified the HCC tumor of HCC tumor-bearing BALB/c nude mice to four stages. Cyclodextrin-sorafenib-chaperoned inclusion complexes were prepared and applied to treat advanced HCC tumor-bearing mice.
Puerarin (PUE) is a Chinese traditional medicine known to enhance glucose uptake into the insulin cells to downregulate the blood glucose levels in the treatment of type II diabetes. Nevertheless, the bioavailability of pristine PUE is limited due to its poor solubility and low intestinal permeability. In this work, we demonstrate that the solubility of PUE can be significantly enhanced via its co-crystallization with L-Proline (PRO). Two crystalline phases, namely, the solvate-free form [PUE][PRO] (I) and the solvated form [PUE]2[PRO]∙EtOH∙(H2O)2 (II) are isolated. These two phases are characterized by single-crystal X-ray diffraction (SCXRD), powder X-ray diffraction (PXRD), Fourier-transformed infrared (FT-IR) spectra, nuclear magnetic resonance (NMR), and thermogravimetric analysis in association with differential scanning calorimetry (TGA-DSC). The solubility and dissolution rate of both I and II in water, gastrointestinal tract at pH 1.2, and phosphate buffer at pH 6.8 indicates a nearly doubled increase as compared to the pristine PUE. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay of pristine PUE, I and II against murine colon cancer cell lines CT-26 and human kidney cell lines HEK-293 indicated that neither compound exhibits obvious cytotoxicity after 24 h. This work showcases that the readily available and biocompatible PRO can be a promising adjuvant to enhance the physicochemical properties of PUE toward orally administered drug formulation with improved pharmacokinetics.
Sorafenib (Sor) is an oral multi-kinase inhibitor, but its water solubility is very low. To improve its solubility, sorafenib hydrochloride hydrate, sorafenib hydrobromide and sorafenib hydrobromide hydrate were prepared in the mixed solvent of the corresponding acid solution, and tetrahydrofuran (THF). The crystal structures of sorafenib hydrochloride trihydrate (Sor·HCl.3H2O), 4-(4-{3-[4-chloro-3-(trifluoro-methyl)phenyl]ureido}phenoxy)-2-(N-methylcarbamoyl) pyridinium hydrochloride trihydrate, C21H17ClF3N4O3+·Cl−.3H2O (I), sorafenib hydrochloride monohydrate (Sor·HCl.H2O), C21H17ClF3N4O3+·Cl−.H2O (II), its solvated form (sorafenib hydrochloride monohydrate monotetrahydrofuran (Sor·HCl.H2O.THF), C21H17ClF3N4O3+·Cl−.H2O.C4H8O (III)), sorafenib hydrobromide (Sor·HBr), 4-(4-{3-[4-chloro-3-(trifluoro-methyl)phenyl]ureido}phenoxy)-2-(N-methylcarbamoyl) pyridinium hydrobromide, C21H17ClF3N4O3+·Br− (IV) and sorafenib hydrobromide monohydrate (Sor·HBr.H2O), C21H17ClF3N4O3+·Br−.H2O (V) were analysed. Their hydrogen bond systems and topologies were investigated. The results showed the distinct roles of water molecules in stabilizing their crystal structures. Moreover, (II) and (V) were isomorphous crystal structures with the same space group P21/n, and similar unit cell dimensions. The predicted morphologies of these forms based on the BFDH model matched well with experimental morphologies. The energy frameworks showed that (I), and (IV) might have better tabletability than (II) and (V). Moreover, the solubility and dissolution rate data exhibited an improvement in the solubility of these salts compared with the free drug.
Sorafenib is an oral multi-target kinase inhibitor that has been used to treat unresectable hepatocellular carcinoma and advanced renal cell carcinoma. The aim of the study was to prepare gum Arabic-chitosan (GA-CS) and gum Arabic-modified chitosan (GA-MCS) microcapsules containing sorafenib as the core phase by complex coacervation. The fluorescence microscopy, dynamic light scattering (DLS), drug loading, and encapsulation efficiency of the microcapsules were clarified. The GA-MCS microcapsule was successfully performed at approximate pH of 4 with a 1% modified chitosan -to-5% gum Arabic ratio of 5:1 (v/v), while the GA-CS microcapsule was successfully prepared at pH 3.5 with a volume ratio of 1% chitosan -to-5% gum Arabic 1:1 (v/v). Sorafenib was encapsulated in the microcapsules as shown through the fluorescence microscopy images. The formation of GA-CS and GA-MCS microcapsules with hydrodynamic sizes of 6.31 μm and 6.56 μm, respectively, was successfully achieved. The drug loading and encapsulation efficiency of the GA-MCS microcapsule was greater than that of the GA-CS microcapsule. The findings indicated that the GA-MCS microcapsule could be an appropriate formation to load sorafenib with a high encapsulation yield.
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