Use of Nanocarriers Containing Antitrypanosomal Drugs for the Treatment of Chagas Disease.

Chagas disease, caused by the Trypanosoma cruzi parasitic protozoan, is a neglected tropical disease (NTD) of significant incidence in Latin America. Transmission to humans and other mammals is mainly via the vector insect from the Reduviidae family, popularly known as the kissing bug. There are other transmission means, such as through congenital transmission, blood transfusions, organ transplantations, and the consumption of contaminated food. For more than 50 years, the disease has been treated with benznidazole and nifurtimox, which are only effective during the acute phase of the disease. In addition to their low efficacy in the chronic phase, they cause many adverse effects and are somewhat selective. The use of nanocarriers has received significant attention due to their ability to encapsulate and release therapeutic agents in a controlled manner. Generally, their diameter ranges from 100 to 300 nanometers. The objective of this scoping review was to perform a search of the literature for the use of nanocarriers as an alternative for improving the treatment of Chagas disease and to suggest future research. Bibliographic searches were carried out in the Web of Science and PubMed scientific databases from January 2012 to May 2023, using the "Chagas disease and Trypanosoma cruzi and nanoparticles" keywords, seeking to gather the largest number of articles, which were evaluated using the inclusion and exclusion criteria. After analyzing the papers, the results showed that nanocarriers offer physiological stability and safety for the transport and controlled release of drugs. They can increase solubility and selectivity against the parasite. The in vitro assays showed that the trypanocidal activity of the drug was not impaired after encapsulation. In the in vivo assays, parasitemia reduction and high survival and cure rates in animals were obtained during both phases of the disease using lower doses when compared to the standard treatment. The scoping review showed that nanocarriers are a promising alternative for the treatment of Chagas disease.

Development, physicochemical evaluation, and in vivo permeation studies of topical formulations containing 0.1% tacrolimus

Abstract The objective of this paper was to develop and evaluate two semi-solid pharmaceutical forms containing 0.1% tacrolimus: cream (CRT01) and gel (GLT01). For the evaluation of physicochemical stability, at times 0, 30, 60 and 90 days, at 23°C and at 40°C, High Performance Liquid Chromatography coupled with a Diode Array Detector (HPLC-DAD) was employed. This method was developed and validated for tacrolimus quantification. The occlusivity test and skin permeation assay were also performed, using an animal model (Wistar rats), and the CRT01 and GLT01 were compared to the 0.1% tacrolimus ointment (PFU01) obtained from the University Pharmacy, Federal University of Rio de Janeiro, Brazil. CRT01 and GLT01 presented a homogeneous aspect and consistency adequate for topical products, along with sensory characteristics above PFU01. They also presented adequate physicochemical stability for 90 days and a lower occlusive effect than PFU01 (p<0.05). CRT01 showed greater affinity for the skin when compared to PFU01 and GLT01, with low systemic absorption. The CRT01 semi-solid formulation was considered the most adequate one to treat patients with atopic dermatitis or other dermatologic inflammatory diseases, promoting rational use of tacrolimus

University Pharmacy: from the foundation to the Pandemic times of Covid-19

Abstract The University Pharmacy Program (FU), from the Federal University of Rio de Janeiro (UFRJ), was created based on the need to offer a curricular internship to students of the Undergraduate Course at the Faculty of Pharmacy. Currently, it is responsible for the care of about 200 patients/day, offering vacancies for curricular internships for students in the Pharmacy course, it has become a reference in the manipulation of many drugs neglected by the pharmaceutical industry and provides access to medicines for low-income users playing an important social function. Research is one of the pillars of FU-UFRJ and several master and doctoral students use the FU research laboratory in the development of dissertations and theses. As of 2002, the Pharmaceutical Care extension projects started to guarantee a rational and safe pharmacotherapy for the medicine users. From its beginning in 1982 until the current quarantine due to the COVID-19 pandemic, FU-UFRJ has been adapting to the new reality and continued to provide patient care services, maintaining its teaching, research, and extension activities. The FU plays a relevant social role in guaranteeing the low-income population access to special and neglected medicines, and to pharmaceutical and education services in health promotion.

In vitro approaches to antioxidant screening for the development of a sunscreen formulation

Abstract The incorporation of antioxidants into sunscreens may provide additional skin photoprotection against the harmful photobiological effects of ultraviolet radiation. The present study evaluated the applicability of a screening approach to the assessment of the antioxidant and photoprotective properties of vitamin C, vitamin E, and coenzyme Q10 and then determined the performance of the most effective antioxidant in a sunscreen formulation. Antioxidant activity was assessed by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, 2,2`-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assay, and oxygen radical absorbance capacity (ORAC) assay, and the photoprotective potential was investigated by the yeast photoprotection assay. The antioxidant with the best effect was incorporated into sunscreen formulations which were evaluated for 120 days regarding their in vitro photoprotective parameters. Vitamin C showed high antioxidant capacity as well as a photoprotective potential against simulated solar irradiation applied for times longer than 1 h. Although the Sun Protection Factor, UVA/UVB ratio and critical wavelength did not differed significantly (p<0.05) between the formulation blank and the formulations containing 0.5% or 1% vitamin C, formulations with vitamin C kept their photostability for 6 months. Consequently, the proposed screening approach seems to be promising for the development of an antisolar photostable formulation containing vitamin C as an antioxidant.

Medication Errors in Compounding Pharmacy / Erros de Medicação em Farmácia de Manipulação

Abstract The traditional role of compounding pharmacies is to make drugs prescribed by physicians for patients with needs that cannot be met by commercially available drugs. Medication errors have attracted attention of health authorities since they compromise the patient's assistance, enhance morbidity rates and increase the healthcare costs. This study analyzed medication errors that occurred in a compounding pharmacy school in order to identify types and periodicity and to outline strategies in the service delivery process to mitigate such errors. This is a retrospective descriptive study carried out from March to June of 2018 and based on the analysis of occurrences recorded by the service sector of a magistral pharmacy school in Rio de Janeiro. The errors were classified according to the stage in the pharmaceutical assistance process and reached 124 records, with an average of 1.03 occurrence/day. The main causes were prescription errors (95 occurrences or 76.60%), administering (12 occurrences or 9.68%), labeling (7 occurrences or 5.65%), dispensing (7 occurrences or 5.65%) and handling (3 occurrences or 2.42%). The errors in the prescription stage, the most frequent ones, were potential but intercepted and cleared before they resulted in a harmful outcome. This study identified medication errors in a magistral pharmacy. The errors were potential but intercepted and resolved before they resulted in a harmful outcome. The results points to the need for systematic surveillance of adverse events in a more active way and for standardizing the procedures throughout the process, from assessing the medical prescription to guiding the patient for proper administration and storage. (AU)

Resumo O papel tradicional das farmácias de manipulação é manipular medicamentos prescritos por médicos para pacientes com necessidades que não podem ser atendidas pelos medicamentos disponíveis no mercado. Os erros de medicação são eventos que vêm recebendo grande destaque entre autoridades sanitárias por contribuírem com o aumento das taxas de morbidade e dos custos do sistema de saúde, comprometendo a qualidade da assistência prestada ao paciente. as it involves legal and ethical aspects of impact on professional practice. Errors in the administration of medications point out the responsibility of the nursing category. An adequate performance of this role enables the prevention of real errors. The purpose of this study was to analyze nursing responsibilities in the administration of medications through a bibliographical research in the Medline and Lilacs data bases (1997/1999O presente estudo teve por objetivo analisar os principais erros de medicação observados em uma Farmácia Escola magistral localizada no sudeste do Brasil. Foi desenvolvido um estudo descritivo retrospectivo no período de março a junho de 2018, baseado na análise das ocorrências de erros de medicação registradas no período. Os erros foram classificados de acordo com as etapas da assistência farmacêutica. Um total de 124 registros foram verificados no período, com média diária de 1,03 ocorrências/dia. As principais causas destes registros foram em 95 (76,60%) devido a erros de prescrição, 3 (2,42%) referentes à erros de manipulação dos medicamentos, 7 (5,65%) erros de rotulagem, 7 (5,65%) erros de dispensação, e 12 (9,68%) referentes à erros de administração do medicamento pelo paciente. Os erros de maior frequência foram relacionados à escrituração da prescrição. Os erros verificados eram potenciais e foram interceptados e resolvidos antes que resultassem em um desfecho danoso. Os resultados indicaram a necessidade de avançar para uma vigilância sistemática de eventos adversos de forma mais ativa e padronização das condutas relacionadas aos processos desde a avaliação da qualidade da prescrição até a orientação para administração e guarda adequada do medicamento pelo paciente. (AU)

Development and characterization of a nanoemulsion containing propranolol for topical delivery.

BACKGROUND: Propranolol (PPN) is a therapeutic option for the treatment of infantile hemangiomas. This study aimed at the development of nanoemulsion (NE) containing 1% PPN, characterization of the system, and safety studies based on ex vivo permeation, cytotoxicity, and biodistribution in vivo. METHODS: The formulation was developed and characterized in relation to the droplet size, polydispersity index (PDI), pH, zeta potential, and electronic microscopy. Ex vivo permeation studies were used to evaluate the cutaneous retention of PPN in the epidermis and dermis. Cytotoxicity studies were performed in fibroblasts, macrophages, and keratinocytes. In vivo biodistribution assay of the formulations was performed by means of labeling with technetium-99m. RESULTS: NE1 exhibited droplet size of 26 nm, PDI <0.4, pH compatible with the skin, and zeta potential of -20 mV, which possibly contributes to the stability. Electron microscopy showed that the NE presented droplets of nanometric size and spherical shape. NE1 provided excellent stability for PPN. In the ex vivo cutaneous permeation assay, the NE provided satisfactory PPN retention particularly in the dermis, which is the site of drug action. In addition, NE1 promoted cutaneous permeation of the PPN in small amount. In vivo biodistribution showed that the radiolabeled formulation remained in the skin and a small amount reached the bloodstream. NE1 presented low cytotoxicity to fibroblasts, macrophages, and keratinocytes in the concentrations evaluated in the cytotoxicity assay. CONCLUSION: We concluded that the formulation is safe for skin administration; however, cutaneous irritation studies should be performed to confirm the safety of the formulation before clinical studies in patients with infantile hemangiomas.

Evaluation of octyl p-methoxycinnamate included in liposomes and cyclodextrins in anti-solar preparations: preparations, characterizations and in vitro penetration studies.

PURPOSE: Awareness of the harmful effects of ultraviolet radiation has led to the increasing use of sunscreens, thus, the development of safe and effective antisolar preparations is important. The inclusion of sunscreen molecules in different release systems, like liposomes (lipo) and cyclodextrins (CD) is therefore required. METHODS: The in vivo sun protection factor (SPF), water resistance, and in vitro transdermal penetration test of octyl p-methoxycinnamate (OMC) in different dispersions, such as OMC encapsulated in liposomes (lipo/OMC), OMC encapsulated in ß-cyclodextrins (ß-CD/OMC), OMC encapsulated in both release systems (lipo/OMC and ß-CD/OMC), and an OMC-free formulation were determined. RESULTS: Although the formulation containing only the lipo/OMC system revealed high value of in vivo SPF (11.0 ± 1.3) and water resistance (SPF = 10.3 ± 2.2), the formulation containing both release systems (lipo/OMC + ß-cyclodextrin/OMC) showed the best result in the in vivo SPF test (11.6 ± 1.6). In the penetration test, the formulation containing the lipo/OMC system had better performance, since a high amount of OMC in the epidermis (18.04 ± 1.17 µg) and a low amount of OMC in the dermis (9.4 ± 2.36 µg) were observed. These results suggest that liposomes interact with the cells of the stratum corneum, promoting retention of OMC in this layer. CONCLUSION: According to our study, the lipo/OMC system is the most advantageous release system, due to its ability to both increase the amount of OMC in the epidermis and decrease the risk of percutaneous absorption.