Recent advances in drug delivery and formulation最新文献

Introduction: Fixed-Dose Combinations (FDCs) combine two or more active components into a single dosage form, addressing active ingredient incompatibilities and enabling diverse release profiles through innovative formulation strategies. They enhance patient compliance, target multiple disease pathways for synergistic effects, and are increasingly important for global health priorities.

Methods: This review synthesizes recent literature, regulatory updates, and clinical evidence on FDCs, focusing on advanced formulation approaches, manufacturing processes, market trends, and post-marketing evaluations. Regulatory frameworks from the USFDA, EMA, and CDSCO were compared to identify approval pathway differences and opportunities for harmonization.

Results: Innovative dosage forms, including co-crystallization, soft gelatin capsules with liquid actives, and cardiovascular polypills, have demonstrated improved therapeutic outcomes and costeffectiveness. In India, FDCs dominate antibiotic use both clinically and economically. Comparative regulatory analysis revealed significant procedural variations, potentially impacting global adoption. Clinical and post-market data confirm the safety, efficacy, and practicality of approved FDCs, supporting their role in addressing unmet medical needs.

Discussion: FDCs simplify complex regimens, improve adherence, and can facilitate the introduction of first- and best-in-class medicines. However, challenges include formulation instability, analytical difficulties in multi-component quantification, manufacturing complexity, and compliance monitoring. Balancing innovation with robust regulatory oversight and fostering international collaboration will be essential for maximizing their potential. This review provides a comprehensive understanding of the evolving FDC landscape, guiding stakeholders in strategic development and implementation for improved healthcare outcomes.

Artificial nanomaterials known as nanozymes, which possess inherent enzyme-mimetic characteristics, have transformed environmental research, biomedicine, and catalysis. Compared with natural enzymes, nanozymes are advantageous due to their high stability, low cost, and adaptability. They exhibit oxidation, reduction, peroxidation, and superoxide dismutation activities, which are essential for environmental remediation, disease therapy, and biological diagnostics. Recent developments have further broadened their catalytic capabilities. Nanozyme-based biosensors offer high sensitivity and rapid detection of biomarkers for diseases such as cancer, diabetes, and infectious disorders, significantly improving early disease diagnosis. In therapeutics, nanozymes play a critical role in regulating oxidative stress, enabling targeted drug delivery, and supporting antibacterial treatments. Their ability to mimic peroxidase and catalase activities has greatly enhanced photodynamic therapy, immunotherapy, and neuroprotection strategies. Despite these advances, challenges remain in improving catalytic efficiency, biocompatibility, and target specificity. Safe clinical translation requires addressing issues related to immunogenicity, long-term toxicity, and controlled biodegradability. Advances in surface modification, functionalization, and AI-driven nanozyme design have improved selectivity and therapeutic performance. Integrating nanozymes with bioinformatics, artificial intelligence, and nanomedicine has opened new avenues for precision healthcare, including real-time disease monitoring and personalized treatment strategies. This review highlights the transformative impact of nanozymes in industrial and medical applications by examining recent advances, challenges, and future prospects in the field. With continued development, nanozymes have the potential to revolutionize enzyme-based technologies, making them indispensable to modern science and medicine.

Excess melanin deposition causes hyperpigmentation, a common dermatological disorder that leads to skin discoloration and an uneven skin tone. Traditional therapies such as topical creams and chemical peels have limitations due to insufficient skin penetration, lengthy treatment durations, and potential adverse effects. Transdermal drug administration has emerged as a viable alternative, offering improved therapeutic effectiveness, sustained release, and enhanced drug absorption. Among transdermal systems, microneedle-based patches have gained significant interest because of their ability to deliver active compounds directly through the skin, bypassing the stratum corneum. This study examines recent advancements in transdermal delivery for hyperpigmentation treatment, with a focus on dissolving microneedle (DMN) patches. Research indicates that DMN patches containing niacinamide, glabridin, and tranexamic acid exhibit greater skin-lightening effects than traditional topical formulations. Clinical studies have validated their safety, efficacy, and ability to reduce melasma and post-inflammatory hyperpigmentation with minimal side effects. Furthermore, novel polymeric formulations enhance drug absorption and stability, optimizing therapeutic outcomes. The use of multifunctional components, targeting tyrosinase inhibition, oxidative stress reduction, and melanin transfer, further improves depigmentation efficacy. The paper also highlights how emerging carriers, such as tetrahedral framework nucleic acids (tFNAs), may enhance drug delivery efficiency. As transdermal technologies continue to advance, microneedlebased approaches hold strong potential to transform hyperpigmentation treatment by providing a highly effective, non-invasive, and patient-friendly therapeutic option. Future research should focus on expanding clinical applications and refining formulation parameters to maximize benefits across diverse skin types.

Nanoparticles are now well-known in several medical domains, including biomedical research. On account of their biocompatibility and stability, green synthesis, which is a process for the production of nanoparticles that is favourable to the environment, has garnered substantial attention. The process of green synthesis is not only an environmentally friendly alternative, but also provides a route to the production of potent medicinal molecules. Green nanotechnology has a bright future, as it has the potential to improve medical treatment and promote environmental sustainability by harnessing the force of nature. The therapeutic applications of inorganic nanoparticles derived from natural resources such as bacteria, fungi, and plants are investigated in this review. In the realm of nanoparticles, gold, silver, and platinum are considered the most significant. Each of these three elements possesses distinctive qualities that render it suited for particular medical uses. As a more environmentally friendly and sustainable alternative to conventional medications, the review highlights the promise of green synthesis.

Atopic Dermatitis (AD) is a long-lasting, inflammatory, and itchy skin disease related to asthma, hay fever, and a family history of the condition. It is the most common chronic skin disease in children, affecting 18% of 7-year-olds. The prevalence of AD in children in the United States is 17.2%, which is comparable to that in Europe and Japan. Greater socioeconomic groupings, fewer families, and metropolitan areas all have higher AD prevalence rates. It is thought that a mix of environmental and genetic factors produces the condition. The gene that codes for the skin matrix protein filaggrin is the most strongly linked genetic link currently identified with AD. Increased water loss due to AD-induced breakdown of the skin barrier leads to dry skin, heightening vulnerability to microbial colonization, allergy sensitization, and infection. PDE4, an intracellular enzyme present in inflammatory cells, is greater in persons with active AD and latent allergic rhinitis. Consequently, crisaborole, a PDE4 inhibitor, raises intracellular cAMP levels, activating Protein Kinase A (PKA), suggesting potential therapeutic options for the dysregulated inflammatory cycle associated with this disease. Thus, Crisaborole should be regarded as the safest and most effective option for treating atopic dermatitis. Crisaborole's specific mechanism, safety profile, and effectiveness in interrupting the inflammatory cycle make it an attractive treatment alternative, according to this study. Crisaborole is presented here as a potential remedy to address the research gap: the need for safer, more efficient therapies that target inflammatory pathways in AD.

Introduction: In clinical practice, several commercial drug-eluting stent products have limitations during the early drug-release phase due to the phenomenon of initial burst release (IBR), which may increase the risk of restenosis. This experimental study utilized a multilayer strategy with genipin-crosslinked chitosan as the polymer and curcumin as the drug to address these limitations.

Methods: Based on the forward speed of the rotary drive (7, 8, and 9 mm/s), ultrasonic coating was used to create uniform layers, followed by scanning electron microscopy (SEM) and a release study. Validation of the analytical method confirmed the reliability of the UV-Vis spectrophotometric technique.

Results: The release data modeled with the Korsmeyer-Peppas model show Super Case II transport via relaxation/erosion. The Peppas-Sahlin model indicates that Fickian diffusion dominated the first 6-7 days, after which polymer relaxation became dominant. At 9 mm/s, Fickian diffusion persisted for up to seven days, whereas at 7 and 8 mm/s, it was limited to the first six days.

Discussion: The multilayer system maintains matrix integrity during drug release, preventing initial burst release. Once the mechanism shifts from diffusion to relaxation, no burst is observed. The zero-order model fit confirms that the design reflects a controlled-release profile.

Conclusion: The strategy demonstrates controlled release without initial burst.

Neuropathy, a devastating disorder of the peripheral nervous system, results in pain, numbness, and weakness, profoundly impacting quality of life. Conventional therapies provide insufficient alleviation, requiring targeted drug delivery systems (TDDS) to improve effectiveness and reduce adverse effects. This review examines diverse TDDS methodologies, encompassing intrathecal therapy, radiofrequency ablation, and spinal cord stimulation, in conjunction with innovations in nanotechnology-driven delivery systems. Nanotechnology offers a novel framework for neuropathy treatment, including nanomaterials such as dendrimers, micelles, polymer nanoparticles, liposomes, hydrogels, and quantum dots. These carriers enhance drug encapsulation, cellular absorption, and sustained release, thereby improving therapeutic efficacy and minimizing systemic toxicity. Gene therapy presents a promising approach, targeting the modulation of neuropathic pathways and facilitating neuron regeneration. Although it remains in preliminary research stages, it holds potential for future therapies, especially in diabetic neuropathy. Moreover, transdermal drug delivery offers a non-invasive method to deliver drugs directly to targeted regions, enhancing bioavailability and patient adherence. The integration of nanotechnology, gene therapy, and transdermal administration has the potential to transform neuropathy treatment by providing more accurate and effective medicines. A multidisciplinary approach is essential to fully exploit the promise of TDDS and improve care and quality of life for patients with neuropathy.

Introduction: The objective of the present study was the development and evaluation of Norfloxacin lipid microspheres as topical gels for adjunct therapy to overcome complex clinical challenges presented by moist, thermally coagulated burn wounds.

Methods: Norfloxacin-loaded lipid microspheres were prepared using the melt diffusion technique with Compritol ATO HD5, stearic acid, Tween 20, Span 80, and Transcutol P and incorporated into topical gels formulated with Carbopol 971P NF.

Results: The lipid microspheres exhibited an average size of 65.22+23.39 μm and drug entrapment efficiency of 81.58 ± 0.81%. The scanning electron microscopy confirmed spherical particle morphology, while differential scanning calorimetry indicated the amorphous nature of norfloxacin within the microspheres. In vitro studies demonstrated an extended release of norfloxacin, with 72.33 ± 1.46% released from microspheres and 63.18 ± 1.24% from topical gels after 8 hours. Ex vivo studies revealed 28.16 ± 0.63% of norfloxacin permeating through second-degree burnt porcine skin and 21.12 ± 1.38% through intact porcine skin after 8 hours from topical gels. In vitro antibacterial studies indicated a lower MIC₉₀ for the lipid microspheres compared to the pure drug.

Discussion: The melt diffusion technique yielded micron-sized spherical particles with a drug entrapment efficiency exceeding 80%. In vitro and ex vivo studies confirmed the extended release and enhanced permeation of norfloxacin. Furthermore, in vitro antibacterial evaluations demonstrated increased effectiveness of the microspheres, attributed to improved solubility and sustained drug release.

Conclusions: The approach shows promise in enhancing Norfloxacin availability for managing burn wound complexities. However, preclinical, clinical, and regulatory evaluations are required to establish the utility of the proposed approach. Further investigations into its application for other types of chronic or infected wounds could broaden its therapeutic potential.

Gastroretentive drug delivery systems (GRDDS) have emerged as a focal point of research and development, attracting substantial attention due to their potential to revolutionize oral drug administration. Their ability to enhance the bioavailability and therapeutic effectiveness of orally administered medications, particularly those with narrow absorption windows or susceptible to gastrointestinal degradation, has spurred considerable interest. By extending gastric residence time, GRDDS offers a pathway to optimize drug absorption while minimizing dosing frequency, thereby improving patient compliance and therapeutic outcomes. This comprehensive review delves into the diverse array of gastroretentive drug delivery approaches, providing in-depth insights into their classification, mechanisms of retention, recent innovations with patented technologies, and existing marketed formulations of the domain. Furthermore, it meticulously examines the challenges inherent in GRDDS implementation and elucidates effective strategies to surmount them. From novel formulation techniques to ingenious drug-carrier systems, this review explores the multifaceted landscape of GRDDS development, shedding light on promising avenues for future research and development. By advancing current knowledge and anticipating future trends, this review serves as a valuable resource for researchers, clinicians, and pharmaceutical professionals navigating the dynamic terrain of gastroretentive drug delivery.

Modern technologies such as nanotechnology are being applied in almost every sector to deliver affordable, environmentally friendly products. The integration of nanotechnology in medicine has revolutionized drug delivery systems, with nanotechnology emerging as a promising frontier. This review explores the synthesis and characterization of nanotablet drug formulations designed to enhance their potential across various applications. By employing characterization techniques such as X-ray diffraction, electron microscopy, and physisorption analysis, researchers have developed innovative drug delivery systems like Sophora Alopecuroides nanotablets to treat deadly diseases such as cancer. Evaluation of pre- and post-compression results indicated that nanotablets exhibited good hardness and flow properties, making these formulations potential drug delivery systems for enhanced bioavailability and sustained release properties. Specifically, sublingual sufentanil nanotablets, such as Zalviso®, have demonstrated efficacy in managing moderate to severe pain in healthcare settings when used in conjunction with a PCA device. However, recent regulatory updates indicate changes in the marketing authorization status of Zalviso®. In conclusion, this novel approach for synthesizing nanotablets presents a promising avenue for diverse applications, and based on the results, it is worth considering for future work.