Journal of Pharmaceutical Innovation最新文献

Purpose

The present study aims to use central composite design (CCD) to fabricate HPMC/PEO orodispersible nanofibers with optimized nanofiber diameter and mechanical strength.

Method

The CCD was used for modeling and optimization of the effect of HPMC (2–4%) and PEO (1–3%) concentrations (numerical factors, each one with three levels) and PEO MW (categorical factor with three levels, 300K, 900K, and 2M) based on average nanofiber diameter (in the range of 150–350 nm) and mechanical strength (maximize). The optimized formulation was used to fabricate orodispersible films containing risperidone. The drug was dispersed (F1) and dissolved (F2) in polymeric solutions. The nanofibers were characterized in terms of morphology and diameter (by SEM), thermal behavior (using TGA and DSC), crystallinity (using XRD), and mechanical properties (tensile strength). Disintegration time, folding endurance, and drug release were also studied.

Result

The CCD design showed that a quadratic model predicted nanofiber diameter and a reduced cubic model described mechanical strength. The CCD results revealed that an increase in HPMC/PEO concentrations and PEO MW led to a higher nanofiber diameter. Moreover, for all PEO MWs examined, an increase in PEO concentration corresponded to a reduction in the tensile strength of the nanofibers. HPMC concentration increase positively affected tensile strength at 300K, while this influence became negative at 900K and for most concentration levels at a PEO MW of 2M. The optimized formulation (with the most desirability) was determined to be 2.3% HPMC and 1.3% PEO with 900K MW, with 249.20 nm fiber diameter and 16.96 MPa mechanical strength. The fabricated optimized formulation showed 243.51±40.12 nm diameter and 13.75±2.14 MPa tensile strength. Both drug-containing nanofibers (F1 and F2) were uniform and smooth, with appropriate thermal behavior and mechanical properties, and showed no significant differences in diameter. F1 and F2 formulations disintegrated within 5 s, with the release of 70% and 91% of loaded drug within 6 min, respectively.

Conclusion

The CCD seems a promising approach for designing nanofibers with optimal characteristics.

The paradigm shift in pharmacovigilance from simple observation to active global data monitoring has presented opportunities and threats to the national regulatory authorities. This work tried to analyze the pharmacovigilance systems of the United States, the European Union, and India with an idea of their strategic differences and paths to modernization. Analysis revealed various developmental levels. The US FDA’s Sentinel Initiative signifies a really well-developed, distributed active surveillance model; while the EU’s system, through EudraVigilance, interfaces centralized spontaneous reporting with structured proactive studies. In contrast, India’s government initiative, the Pharmacovigilance Programme of India (PvPI), although rapidly growing, is largely passive, facing underreporting and infrastructure limitations. We have concluded that the future pharmacovigilance rests not on a single model but on a hybrid approach strategically incorporating real-world evidence (RWE) along with artificial intelligence (AI). It has proposed a transnational framework based on the following three pillars: AI-driven signal amplification for transitioning current systems, such as India’s, from passive data collection to active risk detection; an adaptive regulatory convergence for harmonization of standards while taking into account regional contexts; and interoperable data architecture to enable global collaboration. This work outlines very clear routes for converting active surveillance into passive-surveillance capacity and upgrading pharmacovigilance to the age of digitalization.

Silk sericin, a hydrophilic protein derived from Bombyx mori cocoons, has attracted increasing interest due to its antioxidant, moisturizing, and enzyme-inhibitory properties. Efficient extraction is essential to preserve its biofunctional potential. In this study, sericin was extracted using hot water and 1.25% (w/v) citric acid using autoclave-based heating to achieve pressurized conditions above 100 °C. A Box-Behnken Response Surface Methodology (RSM) was applied to systematically evaluate the effects of extraction parameters (temperature and time) and to optimize five key response variables: yield, purity, molecular weight and polydispersity index (PDI), total antioxidant capacity (ABTS), and α-glucosidase inhibition activity. The results revealed that higher temperatures (125 °C) produced the maximum sericin yield, while moderate conditions (115 °C for 45 min) ensured better preservation of antioxidant and antidiabetic activities. Hot acid extraction resulted in significantly enhanced purity and enzymatic inhibition compared to hot water extraction. Sericin fractions above 7 kDa exhibited the strongest bioactivity, as reflected by lower IC₅₀ values in both ABTS and α-glucosidase inhibition assays. The optimized hot water citric acid-based method yielded 24.00% sericin with 100.00% purity and an IC₅₀ of 0.67 mg/mL for α-glucosidase inhibition. This study compares hot water and hot acid autoclave extractions using Box-Behnken design and evaluates their effects on sericin yield, purity, and bioactivities. Citric acid-based extraction produced higher purity and stronger α-glucosidase inhibition, while hot water extraction preserved antioxidant potential more effectively. These findings support the use of citric acid as an eco-friendly and scalable extraction agent and highlight the potential of sericin in biomedical and nutraceutical applications.

Purpose

Topical eye drops are common for treating eye diseases, often requiring multiple daily doses. Silica Matrix technology enables drug delivery systems that release drugs over time. This study aimed to develop and characterize a silica-based eye drop, as well as a 14-day tolerance and toxicity assessment to evaluate its potential as a drug carrier in ophthalmology.

Methods

Silica Eye Drop is a silica-based composite containing silica microparticles, made via sol-gel chemistry and spray drying, along with silica hydrogel. The product was terminally sterilised by gamma irradiation and characterised by particle size, silica content, in vitro dissolution time, droplet size, applicability, endotoxin content, sterility, and short-term stability. Four New Zealand rabbits received one drop daily in one eye’s conjunctival sac for 14 days, while the other eye served as a control. During the study, eye conditions, blood chemistry, and postmortem histology were monitored.

Results

The final formulation contained 23% (w/w) silica microparticles (average diameter 3.21 μm) and 77% (w/w) silica hydrogel, with 18.2 wt% silica, dissolving in 24 h. The average droplet volume was 31.3 ± 4.4 µl, easily dispensed manually from a single-dose unit with acceptable size variability. A 2-month stability study showed no major changes in product properties. Finally, in the rabbit toxicity study, both the treated and untreated eyes showed similar tolerability levels.

Conclusions

The Silica Eye Drop was successfully developed and manufactured. Easy to use with consistent quality, it demonstrated the safety and potential of silica platform technology for a carrier material in topical ophthalmic products.

~ 100 Word Summary

In this study, a novel silica-based eye drop formulation was described and evaluated. Silica microparticles were synthesised and incorporated through a Fill and Finish process, followed by sterilization and characterization for particle size, silica content, dissolution, droplet size, microbiological purity, and short-term stability. In vivo tolerability was assessed in four New Zealand rabbits over 14 days with daily administration. The optimised formulation contained 23% (w/w) silica microparticles and 77% (w/w) silica hydrogel (18.2 wt% silica). Microparticles (D50 = 3.21 μm) fully dissolved within 24 h. No adverse ocular effects occurred, confirming excellent safety, stability, and therapeutic potential.

25–30 Word Teaser

A novel Silica Eye Drop formulation was developed, showing full dissolution in 24 h and good tolerability in rabbits, highlighting its promise for future ocular therapies.

Purpose

This study presents a novel strategy to enhance Olaparib delivery for ovarian cancer using statistically optimized silica nanocarriers. It provides enhanced drug loading capacity, moderate cytotoxicity, and controlled release compared to conventional nanoparticles. These advantages help reduce systemic toxicity and increase therapeutic accessibility in BRCA-mutated tumors.

Methods

Silica nanocarriers were synthesized using the Sol-Gel method and optimized via Box-Behnken Experimental Design, focusing on template concentration, silica precursor, and catalyst volume. Their impact on particle size, drug loading, and zeta potential was systematically assessed. Advanced characterization techniques (FTIR, XRD, TEM, SEM, DLS) confirmed structural and functional attributes, while ovarian cancer cell line studies validated cytotoxicity and therapeutic potential.

Results

Olaparib-loaded silica nanocarriers were successfully optimized using Box-Behnken Experimental Design, resulting in high drug loading (44.34 ± 0.4%), nanoscale particle size (98.6 ± 0.09 nm), and a stable negative zeta potential (-23.11 ± 0.2 mV). Advanced characterization confirmed effective encapsulation and a transition of Olaparib from crystalline to amorphous form, enhancing its solubility. The formulation exhibited sustained, diffusion-controlled drug release, achieving 63.9 ± 0.02% over 12 h. It also showed selective cytotoxicity against ovarian cancer cells with minimal effects on normal cells, underscoring its promise for cancer-specific cytotoxic applications.

Conclusion

This study developed a novel Olaparib-loaded silica nanocarrier system using statistical optimization. The formulation showed high drug loading, sustained diffusion-controlled release, and enhanced solubility through crystalline-to-amorphous transformation. It demonstrated selective cytotoxicity against ovarian cancer cells with minimal toxicity to normal cells, highlighting its potential for ovarian cancer therapy.

This review explores the interactions between packaging materials and pharmaceutical or biological products, emphasizing their critical role in maintaining product quality, stability, and patient safety. The surface characteristics, chemical composition, and physical properties of packaging materials can significantly influence pharmaceutical integrity through mechanisms such as sorption, leaching, additive migration, and material degradation. A comprehensive overview of the major classes of packaging materials is presented, focusing on their compatibility, stability, and impact on the preservation of therapeutic agents. For instance, studies have shown that inadequate packaging protection can reduce the shelf life of certain formulations from nearly six years to only 21 days. Particular attention is given to extractable and leachable compounds that may migrate from packaging components into formulations, their associated risks, and the analytical techniques employed for their detection and quantification. Advances in modern analytical methodologies have greatly improved the sensitivity and precision of assessing these interactions, thereby enabling more accurate evaluation of packaging–product compatibility. Beyond conventional materials, this review also addresses innovative and sustainable packaging solutions, including nanocomposites, biodegradable polymers, and smart systems designed to enhance product protection and functionality. By highlighting the dynamic interplay between packaging systems and sensitive biological environments, this work provides an updated perspective on current challenges and emerging trends in pharmaceutical packaging science. Overall, this review provides practical guidance for formulation scientists and packaging developers in selecting safe, compatible, and sustainable packaging systems for modern therapeutic products.

Objective

The present research aims to establish an RP-HPLC method for the simultaneous estimation of Sulopenem etzadroxil and Probenecid in a synthetic mixture and a combined dosage form by Design of Experiment and green chemistry approach.

Methods

The Box-Behnken design with quadratic model and response surface methodology was adopted to ensure the effect of independent variables (Temperature, flow rate, and percentage of aqueous mobile phase) on the responses or dependent variables (RT of both drugs, resolution, and USP plate count of both drug peaks) to optimize the method confirmation of design space and robustness. The effective separation of Sulopenem etzadroxil and Probenecid was achieved with Interstil column C18 (250 × 2.1 mm,1.8 μm), 0.1% orthophosphoric acid: acetonitrile (38:62 v/v) at a flow rate of 1.0mL/min, column temperature of 32 °C, and isocratic elution at 210 nm. The elution of Sulopenem etzadroxil and Probenecid was noticed at 2.52 and 3.00 min, with considerable system suitability and resolution with the optimized conditions. The greenness assessment of the eco-friendly nature of the developed method was determined by the green analytical tools like the Green Analytical Procedure Index, Analytical Greenness, and the Analytical Eco Scale.

Results

Sulopenem etzadroxil and Probenecid showed good linearity from 12.5 to 75 µg/mL with R² of 0.999 and 0.999, respectively. The % RSD for both intraday and inter-day precision was determined to be in the range of 0.5 to 0.9. The detection and quantification limits of Sulopenem etzadroxil and Probenecid were calculated to be 0.011 µg/mL, 0.034 µg/mL, and 0.010 µg/mL, 0.032 µg/mL, respectively, by the standard deviation method. The stability-indicating property of the current method could be established by the forced degradation studies. The degradants produced by the stressed sample were distinctly separated from the peaks of Sulopenem etzadroxil and Probenecid. An analytical greenness score of 0.81 out of 1, a score of 81 out of 100 in the analytical eco scale, and 70% of green zones and 20% of yellow zones in the Green Analytical Procedure Index diagram confirm the greenness and environmental sustainability of the method.

Conclusion

The quicker elution time and excellent sensitivity of both Sulopenem etzadroxil and Probenecid, with good eco-friendly nature, make this method sustainable for regular analysis of Sulopenem etzadroxil and Probenecid.

Graphical Abstract

Objectives

Guided by Quality by Design principles, this study aimed to develop a fluidized bed coating process to prepare curcumin solid dispersion pellets (CUR-SDP) with high flowability, encapsulation efficiency, and content uniformity, and improve curcumin (CUR) solubility and stability.

Methods

Hansen solubility parameter analysis and anti-crystallization experiments were conducted to select PVP K30 as the optimal carrier. The Plackett-Burman design was used to identify the critical variables affecting CUR-SDP preparation, followed by optimization using the Box-Behnken design to determine the best formulation and process conditions.

Results

Compared to CUR and the physical mixture, the solubility of CUR-SDP was significantly enhanced. XRD and DSC analysis confirmed that CUR was transformed into an amorphous state during the preparation process and FTIR analysis revealed hydrogen bonding between CUR and PVP K30. Saturated solubility determination showed that CUR-SDP’s thermodynamic dissolution equilibrium concentration was significantly increased, while in vitro dissolution revealed markedly improved dissolution rate. Stability studies confirmed its excellent stability.

Conclusions

The results demonstrated that CUR-SDP prepared by fluidized bed coating technology significantly enhanced solubility of CUR, while exhibiting excellent flowability and storage stability. The findings suggest that the fluidized bed coating technique is a promising method for preparing CUR-SDP.

Background

Ireland is a globally recognised trading nation, providing high-quality meat, milk, and dairy products. To remain viable and grow over time, the Irish agricultural sector must prioritise animal health to maximise productivity, as parasite infections represent a major production-limiting issue.

Objective

This study aimed to formulate plasticised solid dispersion tablets containing oxfendazole (OXF), a broad-spectrum benzimidazole anthelmintic, with improved dissolution behaviour and an extended-release profile. The work addresses the challenge posed by the poor aqueous solubility and limited dissolution of OXF, factors that restrict its therapeutic performance, and introduces a semi-continuous manufacturing strategy to overcome these limitations.

Methods

An innovative pharmaceutical approach employing a semi-continuous manufacturing process that integrates hot-melt extrusion (HME) with micro-injection moulding (µIM) was investigated. Two solid dispersion formulations were developed and evaluated: SDF 1, consisting of PEO 95% and OXF 5% (w/w), and SDF 2, consisting of PEO 52.3%, OXF 2.7%, and PCL 45% (w/w/w).

Results

In vitro drug release studies using high-performance liquid chromatography (HPLC) showed that SDF 1 achieved an ~ 8-fold enhancement in drug dissolution compared to a commercial OXF tablet. SDF 2 demonstrated a ~ 4-fold increase in drug release over a three-day period, attributable to its extended-release characteristics. Biocompatibility was assessed through cell viability assays, confirming that the plasticised tablets produced by melt-processing techniques are non-toxic.

Conclusion

HME coupled with µIM are novel pharmaceutical manufacturing techniques with potential to scale up to mass production. These advanced OXF formulations present a promising therapeutic strategy for the control of helminthiasis in grass-fed cattle, supporting enhanced animal health and agricultural sustainability.

Background

Hibiscus rosa-sinensis L, a widely used medicinal plant, has been traditionally recognized for its therapeutic properties, prompting investigations into its phytochemical composition and bioactivity.

Purpose

This study investigates the extraction and characterization of phytochemicals from H. rosa-sinensis L., focusing on their potential antioxidant, antimitotic, and antiproliferative activities.

Methods

The extraction was conducted using various solvents by maceration method. Then different dilutions of extracts were used to carry out phytochemical analysis and bioactivities assessment.

Results

The yield analysis revealed that n-butanol produced the highest extraction yield (6.05%), while chloroform yielded the lowest (3.6%). Qualitative and quantitative assessments confirmed the presence of flavonoids, tannins, and phytosterols, with High-Performance Liquid Chromatography (HPLC) revealing Myricetin and Quercetin as the predominant flavonoids in the acetone extract, highlighting their potential health benefits due to their antioxidant properties. Furthermore, the antioxidant activity was highest in the acetone extract (71.13 ± 0.03%) at a concentration of 2 mg/ml. The antimitotic activity was assessed using Allium cepa root tips, where the methanolic extract showed the strongest action, reducing the mitotic index significantly to 10% at 0.25 mg/ml. The presence of chromosomal abnormalities, such as micronuclei and fragmented nuclei, confirmed the cytotoxic effects of the extracts. Additionally, the chloroform extract exhibited the lowest cell viability (25 ± 0.557%) in antiproliferative assays against yeast models, suggesting a significant cytotoxic potential.

Conclusion

The study concludes that H. rosa-sinensis possesses considerable antioxidant, antimitotic, and antiproliferative properties, warranting further exploration of its phytochemical constituents for potential therapeutic applications in drug discovery.