ADMET and DMPK最新文献

Introduction: Olanzapine (OLZ) is a psychotropic class drug commonly used to treat schizophrenia, bipolar disorder, and acute manic episodes. It has less water solubility, resulting in a slow dissolution rate and oral bioavailability. Therefore, the development in oral dosage forms is required to enhance the drug solubility.

Method: The solid dispersion of olanzapine is prepared by spray drying technique. The solution of polyvinylpyrrolidone K-30 (PVP K-30), mono amino glycyrrhizinate pentahydrate (GLY), OLZ and silicon dioxide were dissolved in distilled water and ethanol and spray dried to get the solid dispersion. Solid dispersion was characterized for surface morphology, solubility, encapsulation efficiency (EE), X-ray diffraction (X-RD), Differential Scanning Calorimeter (DSC) and drug-polymer interaction by Fourier transforms infrared spectroscopy.

Results: The amorphous nature of the drug's incorporation in solid dispersion was confirmed by X-RD analysis. Prepared solid dispersion showed higher solubility, 11.51 mg, than pure OLZ (0.983 mg ml^-1), while the range of EE was found to be between 64 to 90 %.

Conclusions: The solubility and dissolution rate of the OLZ can effectively increase by spray-dried solid dispersion. Plackett-Burman screening design plays a vital role in understanding the effect of independent variables on EE and solubility.

Background and purpose: The reciprocal translocation of the ABL gene from chromosome 9 to chromosome 22 near the BCR gene gives rise to chronic myelogenous leukemia (CML). The translocation results in forming the Philadelphia chromosome (BCR-ABL) tyrosine kinase. CML results in an increase in the number of white blood cells and alteration in tyrosine kinase expression. CML prognosis includes three stages, namely chronic, accelerated, and blast. The diagnosis method involves a CT scan, biopsy, and complete blood count. However, due to certain disadvantages, early diagnosis of CML is not possible by traditional methods. Nanotechnology offers many advantages in diagnosing and treating cancer.

Experimental approach: We searched PubMed, Scopus and Google Scholar using the keywords Philadelphia chromosome, bionanotechnology, tyrosine kinase pathway, half-life, passive targeting, and organic and inorganic nanoparticles. The relevant papers and the classical papers in this field were selected to write about in this review.

Key results: The sensitivity and specificity of an assay can be improved by nanoparticles. Utilizing this property, peptides, antibodies, aptamers, etc., in the form of nanoparticles, can be used to detect cancer at a much earlier stage. The half-life of the drug is also increased by nanoformulation. The nanoparticle-coated drugs can easily escape from the immune system.

Conclusion: Depending on their type, nanoparticles can be categorized into organic, inorganic and hybrid. Each type has its advantages. Organic nanoparticles have good biocompatibility, inorganic nanoparticles increase the half-life of the drugs. In this review, we highlight the nanoparticles involved in treating CML.

Background and purpose: Chitosan, a chitin deacetylation product, has been applied in nanoparticle or nano-chitosan for medical applications. However, the chitin extraction from crustacean shells and other natural resources, chitin deacetylation, and crosslinking of the chitosan forming the nano-chitosan mostly involve hazardous chemical and physical processes. The risks of these processes to human health and the environment attract the attention of scientists to develop safer and greener techniques. This review aims to describe the progress of harmless chitosan synthesis.

Experimental approach: All strongly related publications to each section, which were found on scientific search engines (Google Scholar, Scopus, and Pubmed), were studied, selected, and then used as references in writing this review. No limitation for the publication year was applied. The publications were searched from April 2022 - June 2023.

Key results: Nano-chitosan could be synthesized in harmless techniques, including the preparation of the chitosan raw materials and crosslinking the chitosan polymer. Enzymatic processes in shell deproteination in the chitin extraction and deacetylation are preferable to reduce the negative effects of conventional chemical-physical processes. Mild alkalines and deep eutectic solvents also provide similar benefits. In the nano-chitosan synthesis, naturally derived compounds (carrageenan, genipin, and valinin) show potency as safer crosslinkers, besides tripolyphosphate, the most common safe crosslinker.

Conclusion: A list of eco-friendly and safer processes in the synthesis of nano-chitosan has been reported in recent years. These findings are suggested for the nano-chitosan synthesis on an industrial scale in the near future.

Background and purpose: The aim of the work was to compare the interactions of three newly synthesized non-toxic starch derivatives, with varied anionic and non-ionic functional groups with methylene blue (MB) as a model cationic drug, and selection of starch derivative with highest affinity to the MB.

Experimental approach: The native potato starch (SN), modified via acetylation (SM1), esterification and crosslinking (SM2) and crosslinking (SM3), was evaluated in MB adsorption studies and assessed by FTIR, PXRD, and DSC.

Key results: The adsorption of MB on SM2 and SM3 matched the BET isotherm model, which confirmed physisorption on the low-porous surface. In the case of SM1, adsorption took place via electrostatic attraction between the heterogeneous adsorbent surface and the adsorbate, as demonstrated by the Freundlich plot. The FTIR confirmed vibrations assigned to N=C stretching bonds at 1600 cm^-1 in the case of MB adsorbed on the SN and SM2. The most intense PXRD peaks belonged to SN and the least to SM2. In the DSC study, the thermal stability via ΔT was assessed, with SM2 of lowest ΔT value (179.8 °C).

Conclusion: SM2 presented the best adsorption capacity, followed by SM3 and the weakest SM1. The interactions were confirmed in the adsorption studies and may reflect applications of the modified starches as drug carriers. In the FTIR study, a probable interaction between the OH^- groups of SM2 and N⁺ of MB was revealed. The most amorphous structure was shown for SM2, which was correlated with the lowest thermal stability provided by the DSC study.