AAPS PharmSciTech最新文献

{"title":"Innovative Microneedle-based Therapies for the Treatment of Diabetic Wound Healing.","authors":"Sunny Rathee, Richa Dayaramani","doi":"10.1208/s12249-025-03187-4","DOIUrl":"https://doi.org/10.1208/s12249-025-03187-4","url":null,"abstract":"<p><p>Microneedle-based medical devices have gained significant attention as innovative tools for addressing challenges in wound healing, particularly in diabetic wound management. These devices offer a minimally invasive, patient-compliant platform for drug delivery, tissue regeneration, and real-time monitoring. This review provides a comprehensive overview of their design and applications, focusing on their role in modulating biological pathways and enzymatic markers essential for wound repair. Key biological pathways such as VEGF (Vascular Endothelial Growth Factor)-mediated angiogenesis, matrix metalloproteinase (MMP)-driven tissue remodeling, and inflammatory response regulation are discussed to elucidate the mechanisms underlying wound healing. The utility of biochemical markers, including oxidative stress indicators and growth factors, in evaluating wound progression is highlighted. Additionally, microneedles demonstrate unique advantages, such as enhanced bioavailability, precise drug delivery, and integration with biosensors for real-time feedback, making them ideal for chronic wound management. In the context of diabetic wounds, microneedle-based devices address specific challenges like impaired angiogenesis, prolonged inflammation, and delayed healing by facilitating localized delivery of therapeutic agents and monitoring critical biomarkers. Advanced material innovations and emerging technologies further enhance their performance and scalability. This review also examines the regulatory landscape and commercialization prospects of microneedle systems while outlining future directions, including novel materials and synergistic therapies. By bridging technological advancements with clinical needs, microneedle-based devices hold the potential to revolutionize wound care and improve outcomes in diabetic and other chronic wound conditions.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 6","pages":"187"},"PeriodicalIF":3.4,"publicationDate":"2025-07-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144590211","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Optimization and Evaluation of Colchicine Patch Formulation Based on Box-Behnken Design.","authors":"Wenliang Dong, Jiahao Feng, Xiang Liu, Jianlu Qu, Cunhao Li, Lian Li, Shunnan Zhang, Wenlong Li","doi":"10.1208/s12249-025-03158-9","DOIUrl":"https://doi.org/10.1208/s12249-025-03158-9","url":null,"abstract":"<p><p>This study aimed to optimize colchicine (COL) transdermal patches to enhance key quality attributes, including adhesion, drug release, and transdermal penetration. The goal was to develop a formulation with improved performance based on BOX-Behnken Design (BBD) optimization. The BBD method was used to design experiments evaluating the effects of three key variables: COL content, penetration enhancer content (azone and propylene glycol), and the solvent evaporation time at 80 °C. A total of 17 randomized experiments were conducted. Patches were assessed for initial adhesion force, peel strength, drug release in vitro for 48 h, and transdermal penetration using texture analysis, in vitro release testing (IVRT), and in vitro permeation testing (IVPT). Fourier-Transform Infrared Spectroscopy (FT-IR) was employed to check for interactions between formulation components, and stability was evaluated under accelerated storage conditions. The optimized formulation included 9.8% COL, 5% azone, and 5% propylene glycol, with evaporation performed for 23 min at 80 °C. This formulation achieved an adhesion index close to the predicted value. In vitro drug release and transdermal permeation pattern for 48 h followed the Weibull equation, with measured cumulative release of 27.62 mg and cumulative penetration per unit area of 256.34 µg/cm², confirming the effectiveness of the optimization. FT-IR analysis showed no significant interactions among components, and accelerated stability testing demonstrated the formulation's robustness over time. The use of BBD for formulation optimization resulted in a transdermal system of COL, highlighting its suitability for avoiding the side effects associated with oral colchicine.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 6","pages":"188"},"PeriodicalIF":3.4,"publicationDate":"2025-07-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144590212","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Novel Luteolin-Zein Nanocomposite Incorporated in Hyaluronic Acid/Sodium Alginate Scaffold as Potential Immunomodulation for Pressure Ulcer Wounds.","authors":"Nouran M Atia, Yasmine M Shahine, Ossama Y Abdallah, Mohamed S Abdel Ghany, Mona A Moustafa","doi":"10.1208/s12249-025-03181-w","DOIUrl":"https://doi.org/10.1208/s12249-025-03181-w","url":null,"abstract":"<p><p>Luteolin (LUT) is a brilliant anti-inflammatory drug having a potential role in wound healing. Nevertheless, its clinical application is inadequate due to its hydrophobicity and poor skin permeation. Pressure ulcers are chronic wounds that have limited and definite treatments. This work aimed to develop a LUT-zein nanocomposite in a bioactive polymeric scaffold as a topical treatment for pressure ulcer wounds by assessing its effect on the pressure ulcers' immune microenvironment. LUT loaded scaffolds were prepared and evaluated regarding particle size, zeta potential, swelling & erosion capacity. Structure elucidation was performed using transmission electron microscopy (TEM) and scanning electron microscopy (SEM). The scaffold (F6) that utilized hyaluronic acid (HA) and sodium alginate (SA) in a concentration of 4:1 revealed the most promising results and it was selected for the in vivo studies. The scaffold (F6) showed a nanosize (240.00 ± 8.54 nm) and a negative ZP (-38.2 ± 2.49 mV). SEM revealed a vastly porous structure in both cross-sections and surface views. In vivo wound healing potential and histological study were evaluated using male Sprague Dawley rats. This is the first study to design LUT-Zn nanpcomposite loaded in HA/SA scaffolds to enhance healing rate and decrease ulcer formation. The selected scaffold showed superior efficacy in modulating the immune microenvironment of the pressure ulcer wound in-vivo as it significantly inhibited IL17A secretion, upregulated IL13 and VEGF, increased miRNA-223 expression, and reduced cell apoptosis within the wound microenvironment, making it a promising treatment for chronic pressure ulcers. The elaborated F6 scaffold could be considered as a talented nanotherapy for enhanced pressure ulcer healing and wound closure rate.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 6","pages":"185"},"PeriodicalIF":3.4,"publicationDate":"2025-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144558752","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Gallic Acid-Loaded Transethosomal Gel for Enhanced Topical Delivery and Sustained Therapeutic Efficacy in Psoriasis Management: Formulation, Optimization, In Vitro and Ex Vivo Assessment.","authors":"Tenzin Sonam Dongsar, Tenzin Tsering Dongsar, Abdulrhman Alsayari, Shadma Wahab, Garima Gupta, Prashant Kesharwani","doi":"10.1208/s12249-025-03179-4","DOIUrl":"https://doi.org/10.1208/s12249-025-03179-4","url":null,"abstract":"<p><p>Psoriasis is a chronic, non-communicable inflammatory skin disorder for which current treatments are largely limited to symptomatic management. These approaches were often challenged with limitations like inadequate skin penetration, frequent dosing requirements, potential toxicity, and low patient adherence, ultimately compromising therapeutic outcomes and affecting patients' health. To obviate the flaws that are hindering the clinical success, nanotechnology has transpired as a revolutionary treatment alternative. Here, we have fabricated a gallic acid encased transethosomal-loaded gel (GA-TE-loaded gel) for the therapeutic management of psoriasis. The optimized gallic acid encased transethosome (GA-TE) displayed an average particle size of 288.9 ± 12.4 nm, a polydispersity index (PDI) of 0.30 ± 0.04, a zeta potential of -38.3 ± 3.2 mV, and an entrapment efficiency (%EE) of 72.55 ± 4.8% (mean ± SD, n = 3). In vitro release studies revealed a biphasic profile for the GA‑TE-loaded gel, an initial burst followed by a sustained phase, achieving 77.3% release of gallic acid over 24 h., compared to the conventional GA-loaded gel (96.36% release at 4 h.). Furthermore, ex-vivo permeation studies and confocal laser scanning microscopy (CLSM) confirmed superior skin permeability by the GA-TE-loaded gel. The dermatokinetic study further validated that encapsulation of GA within the transethosomal vesicle significantly augments the transportation of therapeutic agent within the epidermal and dermal layers in contrast to conventional drug loaded gel. The nanoformulation exhibited a good safety profile and negligible irritative potential, as evidenced by the low irritation score (IrS) value obtained during the HET-CAM irritation assay. These outcomes suggest that the GA-TE-loaded gel offers significant potential as a future treatment alternative for addressing psoriasis.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 6","pages":"183"},"PeriodicalIF":3.4,"publicationDate":"2025-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144558750","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Nanocubospray of Epigallocatechin Gallate for Prevention of Oral Submucous Fibrosis.","authors":"Chetan Hasmukh Mehta, Varalakshmi Velagacherla, Suman Manandhar, Yogendra Nayak, Karkala Sreedhara Ranganath Pai, Shruthi Acharya, Usha Yogendra Nayak","doi":"10.1208/s12249-025-03180-x","DOIUrl":"https://doi.org/10.1208/s12249-025-03180-x","url":null,"abstract":"<p><p>NanoCubes loaded film-forming spray (NanoCuboSpray) is a new formulation that can be explored for nanoscale drug delivery. In the present work, epigallocatechin 3-gallate (EGCG) was encapsulated into NanoCuboSpray (NCS) for oral submucous fibrosis (OSF) treatment. The newly formulated EGCG NCS is then evaluated for ex vivo permeation, drug retention, in vivo efficacy, and safety. The developed formulation was homogeneous, viscous, spreadable and mucoadhesive on the buccal mucosa. EGCG NCS had good permeation and buccal mucosal retention in the ex vivo studies. The NCS with 81.81 mg/kg EGCG dose significantly enhanced mouth opening and effectively upregulated collagen and downregulated TGF-β1 in rats with areca nut extract-induced OSF. EGCG NCS demonstrated better improvements in histopathological and antioxidant parameters compared to EGCG hydrogel and betamethasone injection (BTM Inj.). In the safety evaluation, NCS treatment had negligible changes in histopathological features and serum biochemical markers, maintaining results comparable to the normal control group. Therefore, the optimized NCS presents a safer alternative strategy for treating OSF and holds the potential for further evaluation of its clinical efficacy.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 6","pages":"184"},"PeriodicalIF":3.4,"publicationDate":"2025-07-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144558751","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Retraction Note: Design, Synthesis, and In Vitro Evaluation of Low Molecular Weight Protamine (LMWP)-based Amphiphilic Conjugates as Gene Delivery Carriers.","authors":"Sepideh Arabzadeh, Zeinab Amiri Tehranizadeh, Hamideh Moalemzadeh Haghighi, Fahimeh Charbgoo, Mohammad Ramezani, Fatemeh Soltani","doi":"10.1208/s12249-025-03183-8","DOIUrl":"https://doi.org/10.1208/s12249-025-03183-8","url":null,"abstract":"","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 6","pages":"182"},"PeriodicalIF":3.4,"publicationDate":"2025-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144558753","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Topical Foam for Simultaneous Treatment and Decontamination of Chemical Warfare Agents on Dermal Exposure.","authors":"Sonalika Arup Bhattaccharjee, Mohammad Shajid Ashraf Junaid, Meheli Ghosh, Ritesh Srivastava, Mohammad Athar, Ajay K Banga","doi":"10.1208/s12249-025-03177-6","DOIUrl":"https://doi.org/10.1208/s12249-025-03177-6","url":null,"abstract":"<p><p>Being highly toxic and a quick-acting vesicant, even small amounts of lewisite if not decontaminated immediately are rapidly absorbed into systemic circulation via skin exposure, leading to acute poisoning and death. The skin is the first major target to such chemical weapons. Although the stratum corneum provides a barrier lewisite being a lipophilic molecule that readily permeates this barrier. This necessitates, making early and thorough decontamination prior to manifestation of adverse effects. For this, we aimed to decontaminate skin using an antidote-loaded topical foam, followed by treating local and systemic toxicity using the same formulation. Successful incorporation of 1% antidote into a decontaminating topical foam and the delivery of 1.78 ± 0.21 µg/sq cm into dermatomed porcine ear skin within five minutes of application was achieved. Decontamination after five minutes of exposure (88.43%), as well as prolonged exposure (94.53%; 3 h) to methyl salicylate, a warfare chemical simulant, was demonstrated. The developed formulation demonstrated the potential to back-extract simulant from skin tissue but could not purge simulant penetrated systemic circulation. However, systemic delivery of the antidote was demonstrated, establishing the potential to treat the toxicity caused by the remnant warfare chemicals.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 6","pages":"178"},"PeriodicalIF":3.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144537717","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Hot Melt Extruded Aceclofenac-Soluplus® Solid Dispersion: Mechanistic View of Miscibility and Drug-Carrier Interactions for Enhanced Dissolution.","authors":"Likhitha U, Roushan Bharti, Reema Narayan, Chetan H Mehta, Usha Yogendra Nayak","doi":"10.1208/s12249-025-03173-w","DOIUrl":"https://doi.org/10.1208/s12249-025-03173-w","url":null,"abstract":"<p><p>Aceclofenac (ACF), a Non-Steroidal Anti-Inflammatory Drug (NSAID), is formulated with Soluplus® (SOLP) to enhance solubility and bioavailability. This study presents a distinct approach by utilizing Hot Melt Extrusion (HME) to prepare Aceclofenac-Soluplus® solid dispersion (ACF-SOLP), in contrast to the previously investigated nanoemulsion technique. The HME technique facilitates a uniform drug distribution within the polymer matrix, increasing ACF's dissolution rate. Different weight ratios of ACF and SOLP were assessed with 1:8 (HM4), which proved to be the optimal choice. ACF is dispersed within SOLP in its amorphous state, and HM4 exhibited a significant increase in drug release as compared to pure ACF and its physical mixture. In vivo pharmacokinetic data of HM4 demonstrated a drastic improvement in the C_max (7.1 ± 0.14 µg/ml) and AUC (12.1 ± 1.30 µg-h/ml). Further, molecular dynamics simulation revealed that the polymer is widely dispersed within the supramolecular architecture of ACF-SOLP, with ACF positioned centrally, confirming the favorable interactions between the components. Leveraging the hydrophilic nature of the SOLP, the solid dispersion demonstrated enhanced dissolution of ACF, while HME synergistically reinforced the combination. This approach presents a compelling alternative to traditional methods, unlocking new possibilities for formulating poorly soluble drugs.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 6","pages":"180"},"PeriodicalIF":3.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144537712","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Intranasal Delivery: Formulation Factors and Insights Into User Experience.","authors":"Shabbir Lobo, Zhangjie Xi, Debanjan Das, Norell M Hadzimichalis, John A Creek","doi":"10.1208/s12249-025-03171-y","DOIUrl":"https://doi.org/10.1208/s12249-025-03171-y","url":null,"abstract":"<p><p>Improving nasal spray use experience is typically not addressed as a key product requirement even though sensations of bitterness, sourness, astringency, or burning after intranasal application can cause significant repulsion, consumer non-compliance from recommended usage and product rejection. Extensive studies have been carried out by academia and industry alike into the formulation characteristics of sprays and consumer preferences to make nasal sprays more \"acceptable\" by patients. Due to lack of a collative synopsis of these works, this review article attempts to gather and summarize these studies, address the various attributes that impact post spray experience, and provide suggestions towards maximizing user compliance. We systematically categorized a range of factors which can contribute to unpleasant experiences using nasal sprays including anatomical characteristics of the nose, formulation and device properties, formulation components and dosages, etc. Furthermore, we collated relevant information from pharmaceutical and non-pharmaceutical domains to create a comprehensive knowledge base to frame the scope of the issue. Unpleasant sensorial attributes can be controlled by designing the formulation with a thorough understanding of product-device interactions and novel use of excipients. By choosing excipients such as taste masking agents, flavors, and novel polymers the behavior of the product in the nasal canal can be modulated to block the burning, astringent or bitterness sensation on spray use. This paper discusses these factors in comprehensive detail while offering solutions to ensure a superior product experience. The paper also discusses challenges to adoption and compliance strategies of some newer techniques and excipients.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 6","pages":"179"},"PeriodicalIF":3.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144537715","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Innovative Antimicrobial Nanofibers: Natural Integrations for Enhanced Wound Healing and Biofilm Disruption.","authors":"Eman Abdelhakeem, Heba Attia, Mona M Hashem, Mohamed A Abdel Khalek, Shaimaa M Badr-Eldin, Islam M Adel","doi":"10.1208/s12249-025-03178-5","DOIUrl":"https://doi.org/10.1208/s12249-025-03178-5","url":null,"abstract":"<p><p>Wound infections caused by multidrug-resistant bacteria present a substantial challenge in healthcare. Nanofibers, particularly when infused with natural extracts, are emerging as promising platforms for antimicrobial applications. This study investigates the potential of Anastatica hierochuntica extract-loaded electrospun nanofibers prepared with thermoplastic polyurethane for combating infections and promoting wound healing. Electrospinning was utilized to prepare nanofibers infused with Anastatica hierochuntica extract, resulting in uniform rod-shaped structures confirmed by scanning electron microscopy. The hydrophilicity of the nanofibers was assessed through water contact angle (WCA) measurements and swelling tests. Mechanical properties, including strain and stress were evaluated to determine suitability for drug delivery. The formulation with optimal properties, designated as NF20, underwent further investigation. Drug release profiles were analyzed over 72 h, and antimicrobial efficacy was tested against various pathogens, with comparisons made to Silymarin as a standard. A biofilm study evaluated the anti-virulence activity, while wound healing assays assessed the optimized extract loaded nanofibers potential in fostering tissue repair. The extract-loaded nanofibers exhibited enhanced hydrophilicity, with a WCA of 43.1 ± 0.6° and swelling of 216.67 ± 2.36% after 1 h. NF20 demonstrated superior mechanical properties, with strain and stress values of 67.6% and 0.0486 N/mm², respectively. The sustained release profile indicated 73.40 ± 1.31% release after 72 h. Antimicrobial tests revealed significant reductions in minimum inhibitory concentration, minimum bactericidal concentration, and minimum fungicidal concentration against key pathogens. The biofilm study confirmed extract loaded nanofiber's efficacy in inhibiting biofilm formation and disrupting established biofilms. These findings underscore the potential of the extract-loaded nanofiber composed of thermoplastic polyurethane as innovative wound dressings that enhance antimicrobial properties, promote accelerated healing and support tissue regeneration.</p>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 6","pages":"181"},"PeriodicalIF":3.4,"publicationDate":"2025-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144537713","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}