Pharmaceutical Development and Technology最新文献_第10页

Development of gallic acid loaded composite nanovesicles for the topical treatment of acne: optimization, characterization, and clinical investigation. 用于痤疮局部治疗的没食子酸负载复合纳米颗粒的开发：优化、表征和临床研究。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-10-01 Epub Date: 2024-10-02 DOI: 10.1080/10837450.2024.2409812

Shymaa Hatem, Noha H Moftah, Maha H Ragai, Enas El-Maghawry

{"title":"Development of gallic acid loaded composite nanovesicles for the topical treatment of acne: optimization, characterization, and clinical investigation.","authors":"Shymaa Hatem, Noha H Moftah, Maha H Ragai, Enas El-Maghawry","doi":"10.1080/10837450.2024.2409812","DOIUrl":"10.1080/10837450.2024.2409812","url":null,"abstract":"Gallic acid (GA) proved to produce desired effects topically in the treatment of acne, through its antibacterial, anti-inflammatory and antioxidant characteristics. In the current work, nanovesicular systems; aspasomes loaded with GA were prepared, and evaluated on in-vitro and ex-vivo levels. Formulations were coated with chitosan due to its mucoadhesive properties. Results indicated that the size of the formulations ranged between 273.20 and 855.00 nm, with positively charged zeta potential ranging between 30.60 and 34.40 mV, EE% ranging between 57.651% and 95.20% and good stability after 3-months storage. The formulae provided a sustained drug release of 98.22% over 24 h, 5.4-fold higher ex-vivo skin deposition compared to GA solution, and powerful antioxidant potential compared to the control solution and appeared as spherical bilayer vesicles on being examined using transmission electron microscope. A clinical study was carried out on patients suffering from acne, where the reduction percent of comedones, inflammatory, total acne lesions and infiltrate was calculated. Results revealed that aspasomes exhibited reduction percentages of 72.35%, 80.33%, 77.95% and 90.01% ± for comedones, inflammatory lesions, total lesions, and infiltrate, respectively compared to control solution providing an effective topical delivery system for the management of acne.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"899-911"},"PeriodicalIF":2.6,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142351887","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}

引用次数: 0

Sustained linagliptin administration: superior glycemic control and less pancreatic injury in diabetic rats. 持续服用利拉利汀：糖尿病大鼠的血糖控制更佳，胰腺损伤更少。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-10-01 Epub Date: 2024-09-30 DOI: 10.1080/10837450.2024.2407852

Esraa M Zakaria, Shrouk Fayrouz El-Gamal, Samar Mortada Mahmoud, Hanan M El-Nahas, Hany M El-Bassossy

{"title":"Sustained linagliptin administration: superior glycemic control and less pancreatic injury in diabetic rats.","authors":"Esraa M Zakaria, Shrouk Fayrouz El-Gamal, Samar Mortada Mahmoud, Hanan M El-Nahas, Hany M El-Bassossy","doi":"10.1080/10837450.2024.2407852","DOIUrl":"10.1080/10837450.2024.2407852","url":null,"abstract":"While linagliptin is the most potent dipeptidyl peptidase 4 inhibitor, its use is limited due to poor bioavailability and the potential risk of pancreatic injury. Here, we investigated whether the sustained weekly administration of linagliptin could provide better effect compared to frequent daily oral administration. Type 2 diabetes was induced by feeding rats a high fructose/fat/salt diet followed by STZ injection. Compared to the partial glycemic control achieved with daily oral linagliptin, a weekly subcutaneous injection containing about one-fourth of the oral dose produced superior glycemic control, as evidenced by the 4-week postprandial glucose follow-up and oral glucose tolerance test. This was confirmed by the significant increase in serum insulin in the case of the sustained linagliptin administration. Higher levels of the anti-inflammatory cytokine adiponectin and lower triglyceride levels were observed after sustained linagliptin administration compared with daily oral linagliptin. In addition, sustained linagliptin displayed a significant increase in β-cells' insulin immunoreactivity when compared with daily linagliptin. More reduction in collagen deposition and caspase-3 immunoreactivity in pancreatic tissue were observed in sustained linagliptin compared with oral linagliptin. In conclusion, sustained linagliptin administration provided superior glycemic control, which seems to be mediated by more reduction in pancreatic injury.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"874-885"},"PeriodicalIF":2.6,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142293123","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}

引用次数: 0

Preparation and characterisation of esculetin-loaded nanostructured lipid carriers gels for topical treatment of UV-induced psoriasis. 用于局部治疗紫外线诱发的银屑病的埃克替林负载纳米结构脂质载体凝胶的制备和表征。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-10-01 DOI: 10.1080/10837450.2024.2407854

Rawia M Khalil, Mohamed F Abdelhameed, Sally Abou Taleb, Mohamed A El-Saied, Eman Samy Shalaby

{"title":"Preparation and characterisation of esculetin-loaded nanostructured lipid carriers gels for topical treatment of UV-induced psoriasis.","authors":"Rawia M Khalil, Mohamed F Abdelhameed, Sally Abou Taleb, Mohamed A El-Saied, Eman Samy Shalaby","doi":"10.1080/10837450.2024.2407854","DOIUrl":"10.1080/10837450.2024.2407854","url":null,"abstract":"Significance: As an inflammatory and autoimmune skin condition, psoriasis affects 2-3% of people worldwide. Psoriasis requires prolonged treatments with immunosuppressive medications which have severe adverse effects. Esculetin (Esc) is a natural medication that has been utilised to treat psoriasis.Objective: The goal of this work is to improve Esc's solubility by developing novel Esc nanostructured lipid carriers (NLCs) for treating psoriasis and increasing the residence time on the skin which infers better skin absorption.Methods: The particle size, zeta potential and entrapment efficiency (EE) of Esc NLCs were assessed. Incorporating NLCs into gum Arabic gel preparation enhances their industrial applicability, absorption and residence time on the skin. Esc NLC gels were evaluated by in vitro release and in vivo effectiveness on a rat model of UV-induced psoriasis.Results: Esc NLCs showed high EE reaching more than 95% and reasonable particle size ranging between (53.86 ± 0.38 to 236.3 ± 0.11 nm) and were spherical. The release study of Esc NLCs gel demonstrated a fast release of Esc denoting enhanced bioavailability. Compared to free Esc, Esc NLCs gel (F2) could considerably lower the level of CD34 and TNF-α in the skin. The results were validated through histopathological analysis.Conclusion: As Esc NLCs gel (F2) has strong anti-inflammatory properties, our results showed that it presented a significant potential for healing psoriasis.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"886-898"},"PeriodicalIF":2.6,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142308279","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}

引用次数: 0

Revolutionizing treatment for topical fungal infections: evaluating penetration-enhancer-containing vesicles as a fluconazole delivery system: Ex-vivo and in-vivo dermal testing. 局部真菌感染治疗的革命性变革：将含渗透增强剂的囊泡作为氟康唑给药系统进行评估。体外和体内皮肤测试。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-10-01 Epub Date: 2024-08-22 DOI: 10.1080/10837450.2024.2394573

Fatma A Sarhan, Mahmoud E Soliman, Manal Yassin Hamza, Riham I El-Gogary

{"title":"Revolutionizing treatment for topical fungal infections: evaluating penetration-enhancer-containing vesicles as a fluconazole delivery system: Ex-vivo and in-vivo dermal testing.","authors":"Fatma A Sarhan, Mahmoud E Soliman, Manal Yassin Hamza, Riham I El-Gogary","doi":"10.1080/10837450.2024.2394573","DOIUrl":"10.1080/10837450.2024.2394573","url":null,"abstract":"Fungal infections pose a significant challenge in numerous developing nations and worldwide, necessitating urgent solutions. Oral administration of antifungal medications often leads to severe adverse reactions. Hence, employing topical delivery systems is preferred to ensure efficient dermal delivery of antifungal agents while minimizing side effects. Furthermore, the incorporation of penetration enhancers into nanocarriers loaded with antifungal agents has demonstrated enhanced efficacy in combating mycotic infections. Consequently, ultra-deformable penetration enhancer-containing vesicles (PEVs) were developed to explore this promising approach. In this study, Labrasol® and Transcutol® were used as penetration enhancers in formulating ultra-deformable PEVs containing the antifungal agent Fluconazole (FCZ). The PEVs underwent comprehensive characterization, including measurements of particle size (PS), charge, and entrapment efficiency (EE%). The results revealed that the size of tested PEVs ranged from 100 to 762 nm. All particles exhibited a negative charge, with a minimum zeta potential (ZP) of -38.26 mV, and an intermediate entrapment efficiency (EE%) that reached approximately 40%w/w. Ex-vivo studies demonstrated the ability of PEVs to deliver FCZ to the dermis while minimizing transdermal delivery. The selected formula was tested in-vivo using candidiasis-induced rat model and showed a superiority in its antifungal effect against Candida Albicans compared to the drug control. Stability studies were executed for the selected formula, and revealed good stability shown by the insignificant change in the PS, ZP& EE% over a six-month period.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"814-823"},"PeriodicalIF":2.6,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142004951","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}

引用次数: 0

Buccal lidocaine mucoadhesive patches for pediatrics' teething pain: overcoming possible hazards of oral gels. 治疗小儿出牙疼痛的颊用利多卡因粘胶贴剂：克服口服凝胶可能带来的危害。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-10-01 Epub Date: 2024-08-27 DOI: 10.1080/10837450.2024.2393729

George Bebawy, Magda Samir Sokar, Ossama Y Abdallah

{"title":"Buccal lidocaine mucoadhesive patches for pediatrics' teething pain: overcoming possible hazards of oral gels.","authors":"George Bebawy, Magda Samir Sokar, Ossama Y Abdallah","doi":"10.1080/10837450.2024.2393729","DOIUrl":"10.1080/10837450.2024.2393729","url":null,"abstract":"Objectives: The utilization of pharmaceutical products in pediatric medicine, while established for use in adults, often presents uncertainties due to differences in application for children. The FDA discourages the use of local anesthetic gels, notably lidocaine, for teething pain in pediatrics due to concerns regarding potential adverse effects if inadvertently swallowed excessively. Therefore, significant attention is being directed towards modifying available marketed products to make them suitable for pediatric use. Here, we introduce mucoadhesive patches that not only have an adjusted dose of lidocaine but also feature a controlled release profile to manage teething pain with prolonged effect. This design helps to prevent issues related to gel liquefaction and swallowing, thereby reducing the potential hazardous side effects of lidocaine in the pediatric population.Methods: The study involved the development of controlled-release lidocaine HCl-loaded pellets forming a matrix for inclusion in mucoadhesive patches. Characterization was performed to ensure prolonged drug release, particularly during overnight use, aiming to improve pediatric patient compliance and enable precise dosing.Key findings: The mucoadhesive patches exhibited sustained lidocaine release lasting 24 h, potentially offering overnight relief suitable for pediatric application. The analysis of lidocaine content revealed that the developed patches maintained stable levels compared to doses obtained from commercially available oral gels. This finding implies effective pain control without the need for frequent reapplications, alongside controlled doses that decrease the likelihood of side effects.Conclusion: The formulated medicated patches demonstrated consistent lidocaine content, effectively controlled drug release, and consequently, reduced the likelihood of undesired side effects when compared to oral gel administration.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"805-813"},"PeriodicalIF":2.6,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142009247","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}

引用次数: 0

A review on abuse-deterrent formulations: formulation technology and regulatory stands in approval process. 阻断滥用制剂综述：制剂技术和审批过程中的监管立场。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-10-01 Epub Date: 2024-09-03 DOI: 10.1080/10837450.2024.2398526

Jaydip Bhola, Chetan Borkhataria

{"title":"A review on abuse-deterrent formulations: formulation technology and regulatory stands in approval process.","authors":"Jaydip Bhola, Chetan Borkhataria","doi":"10.1080/10837450.2024.2398526","DOIUrl":"10.1080/10837450.2024.2398526","url":null,"abstract":"Drug abuse has become a global health problem over the past few years. Opioid abuse increased with an increase in the prescription of opioids for pain management. Many other classes of drugs are also abused and misused like anti-depressants, stimulants, hallucinogens, anti-psychotic, and anticholinergic drugs. One of the major reasons is that patients falsely diagnosed with depression, anxiety, and severe pain are prescribed these drugs, which are likely to be addictive. Abuse-deterrent formulations are one means to control drug abuse and overdose of prescription opioids. In this review, we explained how abuse-deterrent technology works, key ingredients used in abuse-deterrent formulations, a brief about marketed opioid drug products with abuse-deterrent properties, and the stand of regulatory agencies in the approval process of opioid drug products. In the end, it summarized that pharmaceutical industries and the FDA put their efforts into reducing drug abuse by encouraging the development of ADFs. Most available drug product having abuse-deterrent features contains Polyethylene oxide, which degrades at high temperatures. It requires the attention of the researcher to find an alternate ingredient or process to overcome said problem. From a regulatory point of view, only a few regulatory agencies have published their guidance on ADFs. It is important to convey other regulatory organizations' perspectives on ADFs as well.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"824-831"},"PeriodicalIF":2.6,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142110812","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}

引用次数: 0

Dexibuprofen enteric film-coated tablets: design, characterization and pharmacokinetic analysis in human volunteers. 右布洛芬肠溶薄膜片：设计、表征和人体志愿者药代动力学分析。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-10-01 Epub Date: 2024-09-04 DOI: 10.1080/10837450.2024.2398537

Anas M Hanif, Abdul Rehman, Rabia Bushra, Nousheen Aslam, Shazia Alam, Hamdy M Dawaba, Aya M Dawaba, Ossama M Sayed

{"title":"Dexibuprofen enteric film-coated tablets: design, characterization and pharmacokinetic analysis in human volunteers.","authors":"Anas M Hanif, Abdul Rehman, Rabia Bushra, Nousheen Aslam, Shazia Alam, Hamdy M Dawaba, Aya M Dawaba, Ossama M Sayed","doi":"10.1080/10837450.2024.2398537","DOIUrl":"10.1080/10837450.2024.2398537","url":null,"abstract":"Objective: This study aimed to develop a stable and scalable enteric film-coated tablet for the gastric irritant dexibuprofen.Methods: Utilizing direct compression with super-disintegration (crospovidone), the optimal core batches were coated with Opadry white seal coat and enterically coated with Eudragit®L100 with pigment (Talc), demonstrating a 12% weight increase; release and integrity were assessed using specific pH buffers and SEM, with stability testing confirming a six-month shelf life at 40 °C and 75% RH.Results: The optimized formulation achieved 99.87% release in phosphate buffer within 60 min, maintained integrity for 120 min in acidic conditions, and exhibited superior bioavailability compared to Innovifen with relative bioavailability ≈of 121% and elevated Cmax (18.35 µg/ml compared to 11.1 µg/ml).Conclusion: These results highlight the potential of this formulation to enhance patient safety and efficacy through delayed enteric technology and fast intestinal release.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"832-840"},"PeriodicalIF":2.6,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142133449","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}

引用次数: 0

The pioneering impact of artificial intelligence (AI) on pharmaceutical research and drug development (invited editorial). 人工智能（AI）对制药研究和药物开发的开创性影响（特邀社论）。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-10-01 Epub Date: 2024-10-10 DOI: 10.1080/10837450.2024.2411492

Tansel Comoglu

引用次数: 0

Leveraging artificial intelligence for better translation of fibre-based pharmaceutical systems into real-world benefits. 利用人工智能更好地将纤维制药系统转化为现实世界的效益。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-10-01 Epub Date: 2024-08-24 DOI: 10.1080/10837450.2024.2395422

Francis Brako, Makuochi Nkwo

{"title":"Leveraging artificial intelligence for better translation of fibre-based pharmaceutical systems into real-world benefits.","authors":"Francis Brako, Makuochi Nkwo","doi":"10.1080/10837450.2024.2395422","DOIUrl":"10.1080/10837450.2024.2395422","url":null,"abstract":"The increasing prominence of biologics in the pharmaceutical market requires more advanced delivery systems to deliver these delicate and complex drug molecules for better therapeutic outcomes. Fibre technology has emerged as a promising approach for creating controlled and targeted drug delivery systems. Fibre-based drug delivery systems offer unprecedented opportunities for improving drug administration, fine-tuning release profiles, and advancing the realm of personalized medicine. These applications range from localized delivery at specific tissue sites to systemic drug administration while safeguarding the stability and integrity of delicate therapeutic compounds. Notwithstanding the promise of fibre-based drug delivery, several challenges such as non-scalability impede cost-effectiveness in the mass production of fibre systems. Biocompatibility and toxicity concerns must also be addressed. Furthermore, issues relating to stability, in-vitro in-vivo correlations, degradation rates, and by-product safety present additional hurdles. Pharmacoinformatics shows the impact of technologies in pharmaceutical processes. Emerging technologies such as Artificial Intelligence (AI) are a transformative force, progressively being applied to enhance various facets of pharmacy, medication development, and clinical healthcare support. However, there is a dearth of studies about the integration of AI in facilitating the translation of predominantly lab-scale pharmaceutical technologies into real-world healthcare interventions. This article explores the application of AI in fibre technology, its potential, challenges, and practical applications within the pharmaceutical field. Through a comprehensive analysis, it presents how the immense capabilities of AI can be leveraged with existing fibre technologies to revolutionize drug delivery and shape the future of therapeutic interventions by enhancing scalability, material integrity, synthesis, and development.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"793-804"},"PeriodicalIF":2.6,"publicationDate":"2024-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142009248","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}

引用次数: 0

Preformulation evaluation of selumetinib for topical application: skin distribution and photodegradation analysis using MALDI imaging and LC-MS/MS. 用于局部应用的赛鲁替尼的制剂前评估：利用 MALDI 成像和 LC-MS/MS 进行皮肤分布和光降解分析。

IF 3.4 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-09-19 DOI: 10.1080/10837450.2024.2405829

Edith Nicol,Bernard Do,Marina Vignes,Maxime Annereau,Muriel Paul,Pierre Wolkenstein,David Touboul,Philippe-Henri Secretan

{"title":"Preformulation evaluation of selumetinib for topical application: skin distribution and photodegradation analysis using MALDI imaging and LC-MS/MS.","authors":"Edith Nicol,Bernard Do,Marina Vignes,Maxime Annereau,Muriel Paul,Pierre Wolkenstein,David Touboul,Philippe-Henri Secretan","doi":"10.1080/10837450.2024.2405829","DOIUrl":"https://doi.org/10.1080/10837450.2024.2405829","url":null,"abstract":"Understanding drug behavior within the skin, especially for photosensitive compounds, is crucial for developing effective and safe topical therapies. This study employs Matrix-Assisted Laser Desorption/Ionization Mass Spectrometry Imaging (MALDI-MSI) and Liquid Chromatography-Mass Spectrometry (LC-MS/MS) to investigate the skin permeation and photostability of selumetinib, a MEK inhibitor used in treating type 1 neurofibromatosis (NF1). The highest amounts of selumetinib in the skin sections were obtained when using the gel formulation, suggesting that it is to be preferred to cream formulations to achieve higher permeation of the drug. Our study also revealed that selumetinib is amenable to photodegradation in ex vivo skin explants, and yields one main degradation product, whose degradation is likely triggered by hydrogen abstraction. MALDI-MSI results showed selumetinib and its degradation product concentrate in skin appendages, indicating these structures might serve as drug reservoirs, potentially prolonging retention and efficacy. This study demonstrates that combining MALDI-MSI with LC/MS-MS can highly contribute to the characterization of the fate of photosensitive compounds in the skin, an essential prerequisite to the development of compound-specific photoprotective measures. It will also pave the way for innovative topical delivery strategies for NF1 treatment.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":"188 1","pages":"1-7"},"PeriodicalIF":3.4,"publicationDate":"2024-09-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142257943","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}

引用次数: 0