Turkish Journal of Pharmaceutical Sciences最新文献

Objectives: The study was aimed to formulate resveratrol (RSV) loaded microsponges to deliver drug at the wound site and incorporate it in the Moringa oleifera Lam. (Moringaceae) gel base to provide an appropriate moist environment for wound management. RSV, a stilbenoid that activates sirtuins and cell-signaling regulators involved in the process of wound healing.

Materials and methods: Microsponges were prepared by oil in oil emulsion solvent diffusion method by optimizing the independent variables; drug: polymer ratio and volume of internal phase solvent and their effects on entrapment efficiency and particle size. Formulation batches were evaluated for drug content, production yield, entrapment efficiency, and in vitro drug release. The microsponges were further incorporated into M. oleifera gum gel, which was then evaluated for spreadability, viscosity, ex vivo diffusion study and in vivo studies using an excision wound model in rats.

Results: Scanning electron microscopy revealed spherical and porous nature of the microsponges in vitro-release study of the optimized batch of RSV microsponges showed 80.88% drug release within 8 h. Differential scanning calorimetry results revealed no drug and polymer interaction during the formation of microsponges. An ex vivo diffusion study through goat skin revealed sustained release of RSV through porous microsponges embedded in the gel base at the wound site. An in vivo study performed using an excision wound model showed wound healing and closure within day 8. Histopathology showed increased re-epithelization and reduced ulceration in RSV microsponge gel-treated group compared with sham operated.

Conclusion: RSV microsponge gel delivered the drug at the wound site and the gel base provided a moist environment and influenced cell adhesion, thereby promoting faster wound healing.

Objectives: Aromatase is an enzyme that catalyzes the conversion of androgens to estrogens. While inhibition of aromatase is a useful approach for treating breast cancer, it may also have toxicological consequences due to its endocrine disrupting/modulating effect. In this study, sensitivity and performance of two in vitro assays -a cell free and a cell-based- for evaluating aromatase activity were investigated by testing known aromatase inhibitors and partial validation of the methods was performed. Advantages and disadvantages of these methods are also discussed.

Materials and methods: Aromatase activity was evaluated via two in vitro models; direct measurement with a cell-free assay using a fluorescent substrate and recombinant human enzyme and indirect evaluation with a cell-based assay where cell proliferation was determined in estrogen receptor positive human breast cancer cells (MCF-7 BUS) in the absence of estrogen and the presence of testosterone.

Results: In the cell-free direct measurement assay, reference compounds ketoconazole and aminoglutethimide have been shown to inhibit the aromatase enzyme with half-maximal inhibitory concentration (IC₅₀) values concordant with literature. In cell-based indirect measurement assay, only ketoconazole dose-dependently inhibited cell proliferation with 3.47 x 10^-7 M IC₅₀. Inter-assay and intra-assay reproducibility of both methods was found to be within acceptable deviation levels.

Conclusion: Both methods can be successfully applied. However, to evaluate the potential aromatase activity of the novel compounds in vitro, it seems better to perform both the cell-based and the cell-free assays that allows low-moderate biotransformation and eliminate cytotoxicity potential, respectively.

Biopharmaceutical classification system (BCS) is an advanced tool used for classifying medicines based on dissolution, water solubility, and intestinal permeability, which affect the absorption of active pharmaceutical ingredients (API) from immediate-release solid oral forms. It is useful to the formulation researchers to develop novel dosage forms based on modernistic rather than experimental approaches. The current review focuses on the fundamentals, objectives, guidance of BCS, characteristics of BCS drugs, their importance and applications of BCS. This review explains the challenges in drug development in terms of solubility and in vivo disposition. In the current review, new strategies for improving BCS II drug solubility as well as biopharmaceutical drug disposition properties which are utilized throughout the early stages of drug development and commercialization are mainly discussed.

Objectives: Vaccines are anticipated to control the ongoing coronavirus disease-2019 (COVID-19) pandemic, however, their acceptance is critical for the desired benefit. This study assessed risk perceptions of COVID-19, acceptability of its vaccine and socio-demographic associations of its acceptability in Nigeria.

Materials and methods: A cross-sectional web-based study was conducted among 420 participants in Nigeria's six geopolitical regions, using a three-part questionnaire. The questionnaire link was distributed via snowball method to consenting participants through online platforms. Study outcome measures were acceptance of COVID-19 vaccine, and risk perception of COVID-19 by study participants. Descriptive and inferential statistics were performed using Microsoft Excel and SPSS version 24. p values ≤0.05 were considered statistically significant.

Results: A total of 410 respondents participated in the study and high-risk perception of severe acute respiratory syndrome-coronavirus-2 infection (COVID-19) was seen in 127 (66.1%) respondents. Vaccine acceptance was high in 233 (56.8%) respondents and was significantly associated with geo-political region (p=0.028). A moderate positive relationship (r: 0.3) was found between risk perception and acceptability of COVID-19 vaccine and the correlation was statistically significant (p=0.000).

Conclusion: High-risk perception of COVID-19 was found in over half of the respondents, and COVID-19 vaccine acceptance rate was a little more than 50%. However, the study noted regional association with vaccine acceptance among study participants. Therefore, strategic and targeted messaging on vaccine acceptance should be prioritized by stakeholders, to ensure successful vaccine implementation.

Objectives: Mushrooms are fungi with nutritional and health benefits. Lentinus squarrosulus Mont., an edible fungus, has traditional usage and relevance in local therapy for managing metabolic diseases. In that view, this study aimed to evaluate the in vitro anti-obesity, anti-diabetic, and cytotoxic potential of the chloroform/methanol extract (CME) and aqueous extract (AE) of the mushroom.

Materials and methods: L. squarrosulus was identified using molecular biology tools. The CME and AE were obtained sequentially and, then, subjected to α-amylase, α-glucosidase, and lipase inhibitory enzyme assays as well as total phenolic content (TPC) and flavonoid content (TFC) estimations. The cytotoxic potential of extract fractions of L. squarrosulus was assessed using the brine shrimp lethality assay.

Results: The molecular identification of the mushroom displayed that the internal transcribed spacer sequence was an equivalent match to that of L. squarrosulus with a high percentage similarity, and thus assigned a unique accession number (KT120043.1). The CME of L. squarrosulus had higher TPC, TFC, and α-glucosidase inhibitory activity than AE. Furthermore, AE of the mushroom showed a higher lipase inhibitory potential with an IC₅₀ value of 22.28 ± 0.65 μg/mL than the CME, while that of the reference, i.e. orlistat was 2.28 ± 0.34 μg/mL. However, these extracts exhibited very low or no α-amylase inhibitory and cytotoxic activity at the tested concentrations.

Conclusion: This study reveals that CME of L. squarrosulus, rich in polyphenols and flavonoids, possesses considerable α-glucosidase and lipase inhibitory activities.