Drug Development and Industrial Pharmacy最新文献

Objective: To prepare astragaloside IV dripping pills (ASDP) and assess their therapeutic effects on mice with doxorubicin hydrochloride-induced dilated cardiomyopathy (DCM). Significance: Astragaloside IV (AS) exhibits pharmacological effects in treating cardiovascular diseases, however, its clinical application is hindered by poor solubility and low bioavailability. The study sheds light on new therapeutic strategy of DCM and development of AS formulations. Methods: The ASDP prepared by solid dispersion technology were optimized and characterized through scanning electron microscopy (SEM), X-ray diffraction (XRD), differential scanning calorimetry (DSC), as well as evaluations of appearance, average weight, hardness, disintegration time, drug content, solubility and dissolution behavior. The therapeutic effects of ASDP on mice with doxorubicin hydrochloride-induced DCM were performed via echocardiography, heart weight index measurements, pathological examination of heart tissues, and determination of serum levels of angiotensin II (Ang II), B-type natriuretic peptide (BNP), and suppressor of tumorigenicity 2 (ST2). Results: ASDP presented as round, white pills with an average weight of 27.61 mg, a short disintegration time (approximately 3 min), a hardness of 4.9 ± 0.2 N and drug content of 64.5 ± 0.12mg/g. Compared to AS, ASDP significantly improved solubility and dissolution rate. In the doxorubicin hydrochloride-induced DCM mouse model, ASDP alleviated cardiac dysfunction and hypertrophy, reduced necrosis, and decreased serum levels of Ang II, BNP and ST2. Conclusion: ASDP, which enhance the solubility and dissolution of AS, demonstrate significant therapeutic efficacy against DCM, suggesting their potential as a promising candidate for DCM treatment.

Objective: In order to optimize the extraction of Teucrium polium (TP) and chicken bile (Bi), evaluate their biological activities and formulate a micro-emulgel for hemorrhoidal therapy.

Significance: Teucrium polium and chicken bile have been historically valued for their traditional medicine for treating hemorrhoids. Therefore, they were used for the development of pharmaceutical formulation.

Methods: A Box-Behnken Design (BBD) was employed to determine the optimal extraction parameters for Teucrium polium, including ethanol/water ratio, extraction time, and material/solvent ratio as factors. The biological activities of both TP and Bi extracts, including antioxidant, antibacterial and anti-inflammatory properties were assessed. The simplex lattice design was used to optimize the formulation of micro-emulgel of both extracts by studying the effect of the surfactant/co-surfactant ratio as well as the oil and water on the spreadability and viscosity of the micro-emulgel. The micro-emulgel was then characterized.

Results: The Teucrium polium extract demonstrated strong antioxidant and antimicrobial activities, while chicken bile exhibited remarkable anti-inflammatory effect. The optimal micro-emulgel had a good consistency and stability.

Conclusion: These findings suggest the potential for these natural extracts to be formulated into topical therapies for hemorrhoidal treatment, supporting their traditional use in medicine.

Objective: To provide a comprehensive evaluation of mucilage-based nanocarriers as emerging platforms for targeted cancer therapy, focusing on their design, functionalization, and therapeutic potential.

Significance: Mucilage, a plant-derived biopolymer composed of natural polysaccharides, possesses inherent biocompatibility, biodegradability, and unique physicochemical characteristics such as high-water retention, gel-forming ability, and stimuli-responsiveness. These properties position mucilage as an ideal material for controlled drug delivery in oncology, offering potential improvements over conventional nanocarriers. However, despite these advantages, the application of mucilage in nanocarrier design remains underexplored, with limited consolidation of existing knowledge and comparative performance data-representing a significant research gap in the field of natural polymer-based drug delivery systems.

Methods: This review synthesizes current advances in the fabrication and functionalization of mucilage-based nanocarriers using techniques such as emulsion solvent evaporation, nanoprecipitation, and green synthesis. It also examines surface modifications, including ligand conjugation and pH-sensitive linker integration, aimed at enhancing tumor-targeted delivery and intracellular drug release.

Results: Preclinical studies demonstrate that mucilage-based nanocarriers enable efficient encapsulation of hydrophobic drugs, improve solubility and pharmacokinetic profiles, and promote targeted drug accumulation at tumor sites. These systems show prolonged circulation times and reduced systemic toxicity compared to traditional nanocarriers.

Conclusions: This review highlights the novelty of mucilage-based systems as a sustainable and multifunctional nanoplatform for cancer therapy. While demonstrating clear therapeutic potential, these systems face challenges including variability in mucilage composition, scalability of production, long-term stability, and regulatory standardization. Future efforts should focus on developing standardized extraction methods, predictive design models, and fostering multidisciplinary collaborations to fully realize the clinical potential of these systems in precision oncology.

Objective: The current study aimed to formulate naringenin nanoparticles (NNPs) with chitosan polymer and investigate their protective effect against cognitive deficit induced by streptozotocin (STZ) in swiss albino mice.

Methods: The interactions of naringenin with the possible targets involved in the pathogenesis of cognitive deficit were predicted using AutoDock vina and predicted its absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties with SwissADME and ProTox-II web servers. NNPs were formulated with chitosan using the ionotropic gelation method and coated with tween 80. The cognition functions of NNPs were evaluated by Elevated Plus Maze (EPM) and Novel Objective Recognition test (NORT) in STZ-induced cognitive deficit in mice at doses 50 and 100 mg/kg equivalent to pure drug, i.p. The effect of NNPs on various antioxidant enzymes (glutathione, superoxide dismutase, catalase, and mitochondrial complexes (1-4)) in cortex and hippocampus region of the brain was also estimated by biochemical methods.

Results: In silico study revealed better binding interactions as well as good binding affinity of naringenin with all the studied targets compared to rivastigmine. The formulated coated NNPs displayed good drug entrapment efficiency (75.412%) and a good in vitro release that followed the Korsmeyer-Peppas model (R² = 0.962). Furthermore, in-vivo studies displayed a learning and memory-enhancing effect of NNPs in EPM and NORT models compared to naringenin alone. A significant increase in the level of antioxidant enzymes revealed that the protective effects of naringenin nanoformulation might be mediated by its potent antioxidant and mitochondrial restoring properties.

Conclusion: Collectively, these studies suggested that the nanoformulation of naringenin is worthwhile for the management of cognitive improvement and other neurological problems.

Objectives: The advent of nanotechnology has transformed drug development, providing innovative solutions for designing and administering therapeutic agents with improved accuracy and efficacy in managing diabetes. This review aims to critically analyze the progress, mechanisms, and therapeutic uses of nanotechnology-based treatments against the diseases.

Significance: The application of nanotechnology in diabetes therapy represents a significant breakthrough in contemporary medicine. By facilitating precise, controlled, and responsive drug delivery systems, nanotechnology-based treatments present considerable advantages over traditional methods.

Key findings: Glipizide sustained-release nanoparticles, repaglinide-loaded polymeric systems, and metformin-loaded alginate nanocapsules are just a few of the nanoformulations that have shown markedly improved pharmacokinetics and therapeutic efficacy in preclinical models. In addition to lowering the frequency of doses, these nano-delivery methods extended glycemic control and enhanced oral bioavailability. Niosomes and solid lipid nanoparticles are two examples of formulations that have demonstrated promise in overcoming physiological obstacles such poor intestinal absorption and enzymatic breakdown. When taken as a whole, these results highlight how revolutionary nanotechnology can be for managing diabetes.

Conclusion: The development of new nano formulations shows great promise in preventing hyperglycemia and improving diabetes management; however, challenges, such as biocompatibility, scalability, and regulatory approval pose substantial obstacles to clinical implementation. Nevertheless, the expanding roles of nanotechnology in diabetes therapy present transformative opportunities, highlighting the necessity for ongoing interdisciplinary research to refine these nanotherapeutics for safe and effective clinical applications.

Objective: This study aims to develop and evaluate the wound-healing and anti-inflammatory potential of Ash-ZnO NPs and Ash-ZnO NPs gel formulation, synthesized using Saraca asoca extract and stabilized in a chitosan matrix. The goal was to overcome the limitations of conventional ZnO nanoparticles, including instability, cytotoxicity, and uncontrolled release.

Significance: Although ZnO nanoparticles possess antimicrobial and regenerative properties, their clinical utility is limited by aggregation and dose-dependent toxicity. The use of Saraca asoca, a medicinal plant rich in flavonoids and phenolics, provides a green synthesis approach that enhances nanoparticle stability and biological activity. Incorporation into a chitosan-based gel further improves topical application by enhancing adhesion, moisture retention, and sustained release. Chitosan also contributes additional healing benefits due to its intrinsic biocompatibility, antimicrobial activity, and role in tissue regeneration.

Methods: Ash-ZnO NPs were synthesized through a green co-precipitation method and formulated into a chitosan hydrogel. In vitro assays, including MTT, scratch wound, and protein denaturation tests, were used to assess cytocompatibility, fibroblast migration, and anti-inflammatory potential. In vivo wound-healing efficacy was evaluated in rats using an excision model, supported by histopathological analysis.

Results: The Ash-ZnO NPs gel exhibited 72.5% inhibition of protein denaturation and achieved 75.63% wound closure within 48 h. Histology confirmed organized tissue architecture and minimal inflammation.

Conclusion: The Ash-ZnO NPs gel represents a promising, biocompatible wound-care formulation that enhances nanoparticle stability, modulates inflammation, and accelerates tissue repair, offering strong potential for clinical dermatological applications.

Objective: The goal of this review is to provide a thorough overview of Boswellic acids (BAs), including their therapeutic potential, pharmacokinetic constraints and how nanotechnology can improve their biological applications.

Significance of review: BAs have the remarkable therapeutic potential, but face limitations due to their poor bioavailability, low solubility and less permeability. This review explores the emerging nanocarrier systems to overcome these issues. It also highlights the clinical studies and key limitations in clinical translation of BAs.

Key findings: In this review, the pharmacokinetic profile, physiochemical parameters and therapeutic effects implicated by BAs have been discussed. Furthermore, this review comprehensively focuses on the nanotechnological advancements conducted on BAs including polymeric nanoparticles, lipid-based nanocarriers, nanocolloids, polymeric micelle and self-nano emulsifying delivery systems (SNEDS). Furthermore, pertinent clinical studies assessing BAs is provided to evaluate their advancement toward practical applications.

Conclusions: Although BAs exhibit significant therapeutic potential, pharmacokinetic restrictions limit their clinical utility. Focussed studies on nanotechnology-based delivery systems, standardized clinical trial design, comprehensive pharmacokinetic, toxicological, and long-term safety assessments are required to optimize these approaches to overcome these barriers.

Objective: This review addresses the challenges in the clinical application of exosomes and explores how engineered exosomes enhance targeting, stability, and therapeutic efficacy through surface modification and advanced drug-loading techniques.

Significance: Exosomes, with their biocompatibility and low immunogenicity, serve as natural nanocarriers. However, limitations such as suboptimal targeting and inconsistent therapeutic effects hinder their clinical translation. Engineered exosomes, leveraging physical, chemical, and peptide-based modification strategies, offer novel solutions to these bottlenecks, paving the way for optimized drug delivery and disease treatment.

Key findings: Engineered exosomes demonstrate superior targeting precision and stability compared to conventional exosomes. Innovative drug-loading technologies significantly improve delivery efficiency and safety. Through targeted delivery and synergistic actions, engineered exosomes enhance treatment outcomes for various diseases. Notwithstanding these advancements, challenges persist in standardizing production processes and evaluating long-term biosafety.

Conclusion: Engineered exosomes overcome the intrinsic limitations of conventional exosomes through targeted modifications and innovative loading approaches, holding substantial promise for clinical drug delivery. While issues of standardization and safety require resolution, their transformative potential in disease therapy warrants continued research and development.

Objective: This study introduces a novel nanoemulsion (NE) system co-loaded with silibinin (SIL) and cabazitaxel (CBX) to address limitations, such as poor solubility, low bioavailability, and systemic toxicities of these agents.

Significance: SIL/CBX-loaded NE enhances the anticancer effects of SIL/CBX against prostate cancer (PCa) in vitro and in vivo, while it could simultaneously reduce the systemic toxicity of SIL/CBX.

Methods: The NE-SIL/CBX was prepared using oleic acid as the oil phase, Tween-80 and Cremophor RH40 as the surfactants, and Transcutol HP as the cosurfactant.

Results: The optimized NE formulation exhibited a particle size of 204.30 ± 10.20 nm, an encapsulation efficiency exceeding 95.30%, and sustained stability under biological and storage conditions. In vitro studies demonstrated a 6.80-fold improvement in cytotoxicity against PCa cells (IC₅₀ = 6.30 µM) compared to the free SIL/CBX combination, while maintaining 62.10% cell viability in normal cells (HEK293) at 100 µg/mL, indicating reduced off-target toxicity compared to free SIL/CBX combination. In vivo, NE-SIL/CBX reduced tumor volume by 78.90% and tumor weight by 80.00% while maintaining stable liver and kidney function, highlighting its safety. The formulation's controlled drug release (87.60% of drug release for SIL and 78.50% of drug release for CBX after 72 h) and synergistic therapeutic effects significantly (p ˂ 0.05) enhanced efficacy compared to free SIL and CBX.

Conclusion: These findings establish NE-SIL/CBX as a promising platform for PCa treatment, offering improved therapeutic index and reduced systemic toxicity. Future clinical investigations could validate its potential for precision oncology applications.

Objective: Curcumin (CUR) is a natural phenolic compound with potent anticancer properties and potential as a photosensitizer (PS) for photodynamic therapy (PDT). However, its clinical application is limited by poor solubility, low bioavailability, and rapid degradation. To address these challenges, this study introduces curcumin-loaded bovine serum albumin nanoparticles (CUR-BSA NPs) as a pH-responsive drug delivery system for enhanced PDT in breast cancer treatment.

Methods: CUR-BSA NPs were synthesized using the desolvation method and characterized by using Field emission scanning electron microscopy (FESEM), Dynamic light scattering (DLS), Fourier-transform infrared (FT-IR) spectroscopy.

Results: The nanoparticles with size (∼170 nm), zeta potential (-36 ± 2.7 mV), and encapsulation efficiency (47.5%), demonstrated pH-responsive drug release, with higher curcumin release under acidic conditions, mimicking the tumor microenvironment. In-vitro cytotoxicity studies on MCF-7 breast cancer cells revealed that CUR-BSA NPs, in combination with blue light irradiation (420 nm, 30 J/cm²), significantly reduced cell viability to 69% after 48 h, while CUR-BSA NPs show lower cytotoxicity (45% vs. 68%) in the absence of photodynamic therapy. TUNEL assay confirmed apoptosis in 52.4% of treated cells, compared to 4.6% in the control group. Furthermore, CUR-BSA NPs displayed excellent biocompatibility in the absence of light exposure, reducing systemic toxicity.

Conclusion: These findings establish CUR-BSA NPs as a promising nanoplatform for PDT, providing enhanced drug delivery, tumor-targeted release, and improved therapeutic efficacy in breast cancer treatment.