Recent advances in drug delivery and formulation最新文献

This study explores the emerging potential of non-aqueous gels for topical therapy, examining their unique properties, diverse applications, and the challenges involved in their formulation and clinical use. By highlighting these aspects, the article aims to shed light on the future of localized drug delivery and inspire further research and innovation in this promising field. Additionally, the article addresses the critical need for regulatory considerations, stability testing, and patient acceptability. It also emphasizes the role of non-aqueous gels in revolutionizing dermatological and transdermal therapies, particularly by enhancing the stability of drugs that are hydrolyzed in the presence of water.

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.

Background: The extrusion-spheronization process continues to be utilized in pharmaceutical manufacturing, as evidenced by several recent patents and articles. The primary challenge in Pelletization via extrusion spheronization has been to optimize the production process to achieve high yields of spherical pellets ensuring they meet specific quality standards while keeping the production costs low.

Objective: Therefore, this study aimed to identify the ideal parameters for maximizing production rates using a dome extruder while maintaining the desired physical characteristics of the pellets.

Methods: By employing Design of Experiments (DoE) techniques and analyzing critical processing parameters, the research sought to delineate the optimal design space. The pellet formulation comprised Apixaban, microcrystalline cellulose, hypromellose, and sodium bicarbonate, intended to generate gas within the pellets. The study employed a Response Surface Methodology, specifically the Central Composite Face-Centered design, to systematically assess the impact of various process variables on both pellet properties and production rate. Key independent factors included Extruder speed (X1), Spheronization speed (X2), and Spheronization time (X3), which were determined based on the preliminary analyses. Characterization of pellets from each experiment encompassed measurements of sphericity via Aspect ratio (R1), Friability (R2), Bulk density (R3), and Percentage yield within a specific size range (R4).

Results: From the results, it was discerned that extrusion and spheronization speed emerged as critical process parameters within defined spheronization time for maximizing production rates while concurrently maintaining satisfactory pellet properties. Based on the design space analysis, extrusion speed spans from 23 to 27 rpm, while spheronization speed extends from 700 to 900 rpm at 5 min to 7 min of spheronization time, yielding more than 90% of the desired fraction of spherical pellets with good physical properties.

Conclusion: This study successfully optimized process parameters for pellet production using a dome-type extruder, employing a Quality by Design (QbD) approach. Key factors influencing pellet yield and quality-extrusion speed, spheronization speed, and spheronization time-were identified and systematically optimized. These optimized pellets may potentially undergo further coating with polymers to facilitate gastro-retentive or floating drug delivery systems, expanding their applicability in pharmaceutical formulations.

Objective: The objective of the present study is 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 were incorporated into topical gels formulated with Carbopol 971P NF.

Results: Lipid microspheres exhibited an average size of 65.22+23.39 μm and a drug entrapment efficiency of 81.58 ± 0.81%. Scanning electron microscopy confirmed spherical particle morphology, while differential scanning calorimetry indicated the amorphous nature of norfloxacin within the microspheres. In vitro studies demonstrated 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 of lipid microspheres compared to the pure drug.

Conclusions: The approach shows promise in enhancing drug availability for managing burn wound complexities through improved solubility, extended release, and localized delivery. However, preclinical, clinical, and regulatory evaluations are required to establish the utility of the proposed approach. Further investigation 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.

Advanced drug delivery methods have emerged mainly because of the limitations of traditional drug delivery systems like oral and intravenous routes, along with fluctuating concentrations of drugs that have compromised therapeutic outcomes. An implantable drug delivery system (IDDS) presents an attractive alternative: long-term, continuous drug release improves therapeutic efficacy while minimizing toxicity and side effects. IDDS, first presented in the 1930s as subcutaneous hormone pellets, have gained much attention recently in drug delivery due to their controlled release of drugs in a localized and sustained manner. In systemic treatments, drugs administered through IDDS evade first-pass metabolism and enzymatic degradation within the gastrointestinal tract, therefore enhancing drug bioavailability. The most suitable properties of IDDS are its application with drugs that have poor stability or solubility in oral formulations. Even though implantation is invasive, the benefits of infrequent administration, higher patient compliance, and being able to discontinue therapy when side effects are present far outweigh the disadvantages. Today, IDDSs are used in a myriad of therapeutic areas: contraception, chemotherapy, and pain management, to name a few. Future developments in such technologies, fine-tuning these systems further, will revolutionize drug therapy by bringing even better and more patient-friendly drugs with both better efficacy and sustained periods of effects.

New chemical entities with low aqueous solubility and permeability encounter significant challenges in formulation development. Low solubility is further accompanied by slow dissolution and poor bioavailability, which in turn leads to unpredictability in terms of both bioavailability and toxicity. Therefore, a significant amount of exertion is necessary to enhance solubility, dissolution, and eventually bioavailability. Additionally, to enhance the solubility properties and amorphous stability of BCS Class II medications and ultimately increase drug bioavailability, coamorphization has emerged as a promising strategy. Co-amorphous solid dispersions (CASD) are multi-component single-phase amorphous solid dispersions comprising two or more small molecules (usually known as co-formers) that might be a combination of drug-drug or drug-excipients. The selection of appropriate co-formers is critical, and the surface properties of co-amorphous formulations must be carefully evaluated, as they influence physical and chemical stability in addition to dissolution performance. Scaling up and processing co-amorphous formulations into the final dosage forms presents challenges that need to be addressed. This review will largely concentrate on the challenges, improvements, and innovations in physicochemical properties, biological characterization, and advancements of co-amorphous systems. This review will also furnish a comprehensive explanation of both established and emerging approaches utilized in the estimation of physicochemical attributes and characterization of CASD (in vitro and in vivo). Regarding CASD's potential to improve patient outcomes and therapeutic efficacy, it has emerged as a viable approach for drug candidates posing the problems of solubility and bioavailability. This approach has also increased the physical stability of drugs.

Introduction: Transdermal delivery systems and wound dressings are critical components of modern healthcare, continually undergoing refinement to enhance efficacy, biocompatibility, and cost-effectiveness. Natural compounds, particularly those sourced from plants, have emerged as promising candidates for advancing these systems.

Aim and objective: This study aims to investigate the design, therapeutic potentials, and comparative advancements of Isoquinoline Quaternary Alkaloid (IQA) nano-dressings.

Materials and methods: The paper offers a comprehensive analysis of IQA's therapeutic potentials, fabrication techniques, and a comparative assessment against traditional wound care approaches, positioning IQA nano dressings as a paradigm shift in chronic wound management with the potential to enhance patient outcomes significantly.

Result: This review delves into the transformative capabilities of dissolving Isoquinoline Quaternary Alkaloid (IQA) nano dressings, showcasing their potential to revolutionize chronic wound care beyond conventional therapies.

Conclusion: Through the amalgamation of nanotechnology with IQA's intrinsic attributes, such as antimicrobial and anti-inflammatory properties, biocompatibility, and sustained drug release, these nanodressings exhibit promising outcomes in tissue regeneration while minimizing the need for frequent dressing changes.

Background: Type 2 Diabetes Mellitus (T2DM) is a prevalent metabolic disease significantly impacting healthcare, characterized by increased blood glucose levels from the average level due to insulin resistance or a lack of insulin production. Canagliflozin Hemihydrate (CGN) is one of the drugs of choice in the treatment of the disease. However, CGN belongs to BCS class IV making it difficult to formulate into suitable dosage form.

Objective: The purpose of the present study was to systematically optimize and explore the potential of Nanostructured Lipid Carriers (NLCs) to improve the solubility and bioavailability of CGN.

Methods: The emulsification and ultrasonication methods were used for the preparation of CGNloaded NLCs (CGN-NLCs) by employing the Box-Behnken design. The solid lipid to liquid lipid ratio (X1), surfactant concentration (X2), and sonication time (X3) were independent variables, while particle size (Y1) and entrapment efficiency (EE) (Y2) were selected as dependent variables.

Results: The optimized batch showed particle size, zeta potential, Polydispersity Index (PDI), and EE of 221.2 ± 2.25 nm, -37 mV, 0.268 ± 0.024, and 98.2 ± 1.62%. The TEM revealed a homogeneous spherical shape of CGN-NLCs. Further, the DSC and XRD studies revealed reduced crystallinity with complete encapsulation of CGN in NLCs. The in vitro drug release study in simulated intestinal fluid (pH 6.8) showed significant CGN release from CGN-NLCs compared to CGN dispersion. Further, the ex vivo intestinal permeability and in vivo pharmacokinetic study showed a 1.33- fold and 3.81-fold increase in permeability and bioavailability along with improvement in Cmax, Tmax, and [AUC]0-24 as compared to CGN dispersion.

Conclusion: Thus, the prepared CGN-NLCs could be a better viable option for T2DM with improved therapeutic efficacy.

Breast cancer continues to pose a significant global health challenge, with conventional therapies frequently hindered by resistance mechanisms and undesirable side effects. This review investigates the therapeutic potential of polyphenols-naturally occurring compounds recognized for their antioxidant, anti-inflammatory, and anti-cancer properties-as alternative or complementary treatments for breast cancer. We examine the molecular pathways through which polyphenols exert their effects, including their influence on oxidative stress modulation, inflammatory responses, cellular proliferation, apoptosis, and estrogen receptor signalling. Additionally, this review addresses innovative nano-based drug delivery systems such as nanoparticles, liposomes, niosomes, and phytosomes that enhance the stability, bioavailability, and targeted delivery of polyphenols. These advanced formulations aim to overcome challenges related to polyphenol degradation, low solubility, and rapid systemic clearance, thereby enhancing their therapeutic efficacy. Through a detailed analysis, we assess the contributions of various nanocarriers in optimizing the delivery of polyphenols specifically to breast cancer cells while minimizing systemic toxicity. The evidence presented highlights the potential of polyphenols in breast cancer management, further supported by nanoformulations that improve both stability and delivery efficiency.