Journal of Pharmaceutical Innovation最新文献

Purpose

Posaconazole (PSZ) is BCS class-II drug that displays variable bioavailability upon oral administration due to extremely low and pH-dependent solubility.

Method

The present investigation was aimed to formulate and evaluate liquisolid pellets of PSZ for improving its dissolution. Liquisolid pellets were prepared using Transcutol® HP, Neusilin® US2, and Aerosil® 200 as non-volatile liquid, carrier, and coating materials respectively. A 3² full factorial design having excipient ratio (R) and spheronization speed as independent variables and the cumulative amount of drug dissolved at 135 min and 165 min as dependent variables were used for the process optimization.

Result

The results of regression analysis indicated a significant effect of selected independent variables on the dependent variables (p-value < 0.05). Differential scanning calorimetry (DSC) studies revealed that the PSZ remained in an amorphous or molecular dispersed state within the liquisolid pellets. Powder X-ray diffraction (PXRD) analysis indicated a significant reduction in crystallinity of the entrapped drug compared to pure drugs. The Fourier-transform infrared (FTIR) analysis demonstrated the stability of the drug within the optimized pellets. SEM images confirmed uniform and well-shaped spherical liquisolid pellets.

Conclusion

During In-vitro dissolution studies, the cumulative amount of the drug dissolved from the prepared pellets was less than 5% during the acid stage (750 ml 0.01 N HCL) whereas the improvement was significant during the buffer stage (750 ml 0.01 N HCL + 250 ml 0.2 M pH 6.8 Phosphate buffer + 1.46% polysorbate 80).

Purpose

Alginate beads intended to float in the stomach have several advantages over the traditional oral dosage forms. However, the formulation of these beads to deliver hydrophilic drugs such as captopril is a big challenge in terms of entrapment efficiency (EE) and extending the drug release. Here, we investigated the feasibility of using the double emulsion (DE) technique during the preparation of alginate floating beads to enhance the EE. This technique allows the incorporation of captopril into the oil droplets, the floating agent within the beads, which provides a hydrophobic barrier preventing drug loss.

Methods

Different DE beads were prepared using ionotropic gelation methods and compared with ordinary oil-entrapped beads based on the floating properties, EE, and drug release.

Results

The results revealed that all the prepared beads have comparable floating properties, however, the EE was significantly increased from 11% for ordinary beads to 25% for DE beads. Moreover, the release of captopril from DE beads was markedly prolonged in comparison to that from ordinary beads. The SEM images clearly showed that the use of surfactant, tween 80, has a significant effect on the prepared beads through stabilizing the primary emulsion, maintain the drug dispersed within the oil droplets, and producing smooth beads with well-crosslinked surface and small well-dispersed oil droplets.

Conclusion

The findings of this study highlighted the potential of DE alginate beads as a promising drug delivery system, addressing the challenges associated with hydrophilic drug encapsulation.

The ability to formulate optimum drug-loaded carriers is a challenge that impedes virtuous drug delivery and stability. Nano micelles (NMs) are highly prospective carriers due to their minute dimensions and exceptional biocompatibility. This study investigated a more efficient and straightforward fabrication method for surfactant nano micelles than the conventional solvent vaporization process. The objective was to develop and validate the Direct Method, an expedited approach for producing surfactant NMs. Tween 20, was employed to simulate the solubility of various drugs in Surfactant, including azithromycin monohydrate, fusidic acid, and metronidazole. Four distinct concentrations of the medication were employed. The polydispersity index and micellar diameter were employed to compare and contrast the two methodologies. No significant differences (p < 0.05) were observed between the outcomes obtained from both methods, irrespective of the concentrations of the drugs. The Direct Method exhibited comparable levels of efficiency to the conventional approach. The study effectively established the Direct Method as a rapid and efficient substitute for surfactant NMs synthesis.

Background

Hypertension poses a global health challenge, contributing significantly to mortality and cardiovascular diseases in both developed and low- to middle-income nations. Conventional oral tablets often fail to provide the rapid onset required for acute conditions, prompting exploration of alternative non-parenteral routes.

Main Body

This review focuses on sublingual administration as a viable option, given its potential for rapid drug absorption due to the sublingual cavity's higher permeability. Sublingual tablets offer advantages such as improved bioavailability, minimal adverse effects, and ease of use. However, formulating effective sublingual tablets presents challenges distinct from conventional tablets QbD, or quality by design, is a methodical approach to formulation development., offering benefits like high-quality pharmaceuticals, regulatory flexibility, and post-approval modification management. The QbD process involves defining quality target product profiles, understanding manufacturing processes, identifying critical material attributes, and optimizing key process parameters. This systematic approach ensures a design space that allows for constant improvement throughout the pharmaceutical product lifecycle.

Conclusion

This review aims to consolidate studies on sublingual administration of antihypertensive drugs, incorporating a systematic risk assessment approach within the QbD framework. By applying QbD principles to optimize sublingual tablet formulations, this approach promises efficient drug product development, reducing the need for extensive testing while ensuring affordability and effectiveness. Despite numerous literature reviews on sublingual tablets, this review uniquely addresses the systematic implementation of QbD for sublingual tablet development, filling a gap in the current pharmaceutical research landscape. The exploration of risk identification, analysis, and evaluation of critical quality attributes enhances our understanding of antihypertensive sublingual tablets' development, providing a valuable resource for pharmaceutical scientists and researchers.

Graphical Abstract

Purpose

Fluocinolone acetonide is a potent anti-inflammatory corticosteroid commonly used to treat atopic dermatitis. Its commercially available topical formulations (cream/ointment) must be administered frequently. The study aimed to develop a fluocinolone acetonide-liquid crystal nanoparticles (FA-LCN) based gel for treating atopic dermatitis.

Methods

FA-LCN were produced using a top-down method and statistically optimized by a 2³ full-factorial design with concentrations of glyceryl monooleate, Poloxamer 407 and sonication time as independent variables, while entrapment efficacy (EE), particle size (PS) and in vitro drug release (DR) as dependent variables.

Results

The optimized batch with an average particle size of 265.3 nm, zeta potential of -47.3 mV and encapsulation efficiency of 98.6% was incorporated into Carbopol 940-based gel. The globular nanoparticles were confirmed by TEM analysis, and their formation was supported by FTIR data. In vitro studies of FA-LCN gel showed 96 ± 1.65% release at the end of 30 h. In vivo studies revealed no skin irritation after the application of FA-LCN gel. FA-LCN (0.5%w/w) gel showed faster healing, substantially reduced earflap thickness, and lower WBC counts compared to the FA-LCN 0.1% gel and the marketed formulation in albino Wistar rats challenged with DNCB. Additionally, the FA-LCN 0.5% gel (3.08 ± 0.16 µg/cm²) exhibited greater drug deposition in the skin compared to the FA-LCN 0.1% (2.12 ± 0.11 µg/cm²) gel and the marketed formulation (1.01 ± 0.19 µg/cm²).

Conclusions

Therefore, FA-LCN-based gel could be a viable option for chronic dermatological treatment for atopic dermatitis with a reduced application frequency.

Purpose

This study aims to improve curcumin’s solubility and anti-cancer effectiveness by utilizing deep eutectic solvents (DES)-based liquisolid nanoparticles. This study aims to develop mesoporous silica nanoparticles (MSNs) containing curcumin and evaluate their therapeutic efficacy against the HCT 116 human colon cancer cell line.

Methods

The study focused on developing different DES formulations using Menthol and Capric Acid, evaluating the effectiveness of surfactants such as Labrasol and Tween 80 in enhancing curcumin dissolution, and synthesizing curcumin-loaded MSNs. The stability of nanoparticles in deep eutectic solvents (DES) and their pharmacological impact on colon cancer cells were thoroughly assessed.

Results

The solubility of curcumin was significantly enhanced through the use of deep eutectic solvent (DES) formulations, specifically when Tween 80 was employed as a surfactant. The in vitro tests showed that curcumin-loaded MSNs with Tween 80 demonstrated strong anti-cancer activity, as indicated by an IC50 value of around 100 µM.

Conclusion

The study effectively shows that DES-based MSNs can greatly improve curcumin’s solubility and anti-cancer effectiveness. Tween 80, as a surfactant, enhances its therapeutic potential, indicating promising prospects for future clinical applications in cancer treatment.

Purpose

The main purpose of this study is to introduce a new adjuvant treatment for H. pylori that aims to enhance therapy outcomes. The research question is how to create a controlled-release gastro-retentive floating system using a combination of chitosan (CS) and beeswax (BW) and to evaluate the release behavior of curcumin as an active ingredient.

Methods

In this study, a new formula combining CS and BW was developed through a hot melting process to create a controlled-release gastro-retentive floating system. Response surface methodology (RSM) was employed to determine the optimal conditions and concentrations of CS and BW to produce the desired floating system. Parameters such as mixing time, processing melting temperature, and concentration of BW were evaluated.

Results

The study found that the optimal parameters for the CS/BW formulation were determined as follows: a mixing time of 3 min, a processing melting temperature of 92.2 °C, and a BW concentration of 13.3% (w/w). Curcumin was incorporated into the optimal tablet, and its release behavior was evaluated. The results showed a full floating behavior of the tablet and a zero-order release behavior in acidic conditions.

Conclusions

The study successfully introduced a new adjuvant treatment for H. pylori that utilizes a controlled-release gastro-retentive floating system. The combination of CS and BW, along with the incorporation of curcumin, showed promising results in terms of floating behavior and release kinetics. This new treatment approach has the potential to enhance therapy outcomes for H. pylori infections.

Purpose

The study of nanoparticles for antibacterial, antifungal, and anticancer action is an important sector in nanoscience. The use of plant extracts in nanoparticle synthesis is among the most simple, cost-effective, and ecologically acceptable strategies. The goal is to use Artocarpus altilis fruit extract to generate plant-mediated silver nanoparticles for its biological activity.

Methods

Phytochemical profiling of methanolic extract of Artocarpus altilis fruit was carried out. UV visible spectroscopy and scanning electron microscopy (SEM) are used to characterize the sample. The disc diffusion method was used to interpret antimicrobial activity. The MTT assay was used to determine the cytotoxicity.

Results

The presence of flavonoids, terpenoids, phenolic compounds, and others was discovered by phytochemical profiling. UV-visible spectroscopy was used to establish the existence of AgNPs, and a maximum absorbance range was obtained. The optimized nanoparticles were shown to have a spherical shape by the SEM pictures. Using the disc diffusion method, the defined AgNPs demonstrated antibacterial efficacy against Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, and Staphylococcus aureus at various doses, as well as antifungal efficacy against Aspergillus fumigates. When compared to doxorubicin, the lung cancer cell lines (A549 cell line) demonstrated potential anticancer activity of silver nanoparticles.

Conclusion

We discovered that silver nanoparticles made from Artocarpus altilis fruit extract have a similar effect to ciprofloxacin. The cytotoxic activity anticipated against the lung cancer cell line (A549 cell line) shows that the percentage of cell viability is identical to that of doxorubicin which indicates the potential for the treatment of lung tumors.

Purpose

The growing demand for effective pharmaceutical treatments, notably amidst health challenges like COVID, highlights the urgency for improved drug production techniques. This study examines the simulation of the Sulzer SMX static mixer in laminar conditions for the continuous pharmaceutical manufacturing of significant pharmaceuticals, notably imatinib.

Methods

Computational fluid dynamics (CFD) were employed to assess the SMX static mixer’s hydrodynamics and mixing performance. Emphasis was on mixing efficiency and residence time distributions (RTD) in a mixer with SMX elements. We refined the model’s reliability and explored the correlation between friction factor and Reynolds number. The Definitive Screening Design (DSD) was used to determine major factors impacting mixer dynamics.

Results

We established a novel correlation between friction factor and Reynolds number. The study reveal that lower flowrates significantly impact mixing efficiency, with different solvents inducing mixing delays. The RTD study identified the total inlet flowrate’s influence on distribution, with higher flowrates leading to more distinct RTD profiles and decreased axial mixing. The screening analysis highlighted flowrate’s dominance over other factors in determining mixing efficiency and residence time.

Conclusions

Through precise computational fluid dynamics (CFD) simulations, the study affirms the robustness of the developed model and underscores the novel correlation between the friction factor and Reynolds number. Insights into flow rate’s pivotal role in dictating mixer efficiency and residence time distribution are discerned, culminating in a comprehensive guide for refining static mixer operations for optimized drug manufacturing.