A Systematic Review of Functionalized Polymeric Nanoparticles to Improve Intestinal Permeability of Drugs and Biological Products.

BACKGROUND: The oral route is the most frequently used and the most convenient route of drug administration since it has several advantages, such as ease of use, patient compliance, and better costeffectiveness. However, physicochemical and biopharmaceutical limitations of various active pharmaceutical ingredients (API) hinder suitability for this route, including degradation in the gastrointestinal tract, low intestinal permeability, and low bioavailability. To overcome these problems, while maintaining therapeutic efficacy, polymeric nanoparticles have attracted considerable attention for their ability to increase drug solubility, promote the controlled release, and improve stability. In addition, the functionalization of nanocarriers can increase uptake and accumulation at the target site of action, and intestinal absorption, making it possible to obtain more viable, safe and efficient treatments for oral administration. OBJECTIVE: This systematic review aimed to seek recent advances in the literature on the use of polymeric nanoparticles functionalization to increase intestinal permeability of APIs that are intended for oral administration. METHODS: Two bibliographic databases were consulted (PubMed and ScienceDirect). The selected publications and the writing of this systematic review were based on the guidelines mentioned in the PRISMA statement. RESULTS: Out of a total of 3036 studies, 22 studies were included in this article based on our eligibility criteria. The results were consistent for the application of nanoparticle functionalization to increase intestinal permeability. CONCLUSION: The functionalized polymeric nanoparticles can be considered as carrier systems that improve the intestinal permeability and bioavailability of APIs, with the potential to result, in the future, in the development of oral medicines.

A Systematic Review of the Anti-inflammatory Effects of Gallium Compounds.

BACKGROUND: Inflammation is an essential response provided by the immune system, ensuring the survival during microbial infection, tissue injury and other noxious conditions. However, prolonged inflammatory processes are often associated with severe side effects on health. OBJECTIVE: This systematic review aimed to provide the evidence in the literature of the preclinical and human anti-inflammatory activity of gallium compounds from 2000 to 2019 focused on elucidating the mechanisms involved in the inflammatory process. METHODS: Seven bibliographical databases were consulted (PubMed, Medline, ScienceDirect, Scopus, Springer, Web of Science, and EBSCOhost). The selection of appropriate publications and writing of this systematic review were based on the guidelines mentioned in the PRISMA statement. Moreover, the assessment of the methodological quality of the selected studies was also performed. RESULTS: From a total of 3018 studies, 16 studies were included in this paper based on our eligibility criteria, which showed promising and consistent results. CONCLUSION: Further research concerning specific inflammatory conditions is required.

Development of Pediatric Orodispersible Tablets Based on Efavirenz as a New Therapeutic Alternative.

BACKGROUND: Efavirenz is the most used medication in the treatment of Acquired Immunodeficiency Syndrome (AIDS). The limited number of pediatric antiretroviral formulations approved by regulatory agencies is the most significant obstacle to adequate and efficient pharmacotherapy for this group of patients. The efavirenz has excellent therapeutic potential, but has low aqueous solubility/bioavailability. METHODS: To minimize these limitations, multicomponent systems with ß-cyclodextrin and polyvinylpyrrolidone K-30 were obtained. Due to the limited number of pediatric antiretroviral formulations, the development of a pediatric orodispersible tablet is an alternative that is thought easy to administer, since it disintegrates rapidly in the oral cavity. The multicomponent systems were obtained by the method of kneading and characterized by solubility test, X-ray diffraction, differential scanning calorimetry and infrared absorption spectroscopy by Fourier transform. The orodispersible tablets were prepared by direct compression. The quality control of hardness, friability, disintegration, and dissolution was performed. The influence of the components of the formulation on the characteristics of the tablets was evaluated through a 22 factorial design added with three central points, to compare the effect of the dependent variables on the responses. RESULTS: An increase in drug solubility was observed, with a decrease in crystallinity. Besides that, an excellent dissolution profile presented with more than 83% of the drug's content dissolved in less than 15 minutes. Satisfactory disintegration time and friability were observed. CONCLUSION: It was observed that reduced concentrations of mannitol decreased the hardness and disintegration time of the formulations. The orodispersible tablet composed of efavirenz: ß- cyclodextrin: polyvinylpyrrolidone, favors greater absorption and bioavailability. It has several advantages for pediatric patients, as the dosage form disintegrates quickly in the mouth and does not require water for administration, thereby improving patient compliance with the treatment.