Pharmaceutical Development and Technology最新文献_第10页

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

Peptide-Functionalized Gold Nanoparticles for Boron Neutron Capture Therapy with the potential to use in Glioblastoma Treatment. 用于硼中子俘获疗法的肽功能化金纳米粒子，有望用于胶质母细胞瘤治疗。

IF 3.4 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-09-17 DOI: 10.1080/10837450.2024.2406044

Zhicheng Zhang,Xin Wang,Qi Dai,Yaxin Qin,Xiaoyan Sun,Minoru Suzuki,Xiaoying Ying,Min Han,Qichun Wei

{"title":"Peptide-Functionalized Gold Nanoparticles for Boron Neutron Capture Therapy with the potential to use in Glioblastoma Treatment.","authors":"Zhicheng Zhang,Xin Wang,Qi Dai,Yaxin Qin,Xiaoyan Sun,Minoru Suzuki,Xiaoying Ying,Min Han,Qichun Wei","doi":"10.1080/10837450.2024.2406044","DOIUrl":"https://doi.org/10.1080/10837450.2024.2406044","url":null,"abstract":"Glioblastoma is a highly aggressive glioma with limited treatment options. Boron neutron capture therapy (BNCT) offers a promising approach for refractory cancers, utilizing boron-10 (10B) and thermal neutrons to generate cytotoxic particles. Effective BNCT depends on selective targeting and retention of 10B in tumors. Current BNCT drugs face issues with rapid clearance and poor tumor accumulation. To address this, we developed gold nanoparticles (AuNPs) functionalized with cyclic arginine-glycine-aspartic acid (cRGD) peptides as a nanocarrier for Sodium Mercaptododecaborate (BSH), resulting in AuNPs-BSH&PEG-cRGD. In vitro, AuNPs-BSH&PEG-cRGD increased 10B content in GL261 glioma cells by approximately 2.5-fold compared to unmodified AuNPs-BSH&PEG, indicating enhanced targeting due to cRGD's affinity for integrin receptor αvβ3. In a subcutaneous glioma mouse model, 6 hours post-intratumoral administration, the 10B concentration in tumors was 17.98 μg/g for AuNPs-BSH&PEG-cRGD, significantly higher than 0.45 μg/g for BSH. The tumor-to-blood (T/B) and tumor-to-normal tissue (T/N) ratios were also higher for AuNPs-BSH&PEG-cRGD, suggesting improved targeting and retention. This indicates that AuNPs-BSH&PEG-cRGD may enhance BNCT efficacy and minimize normal tissue toxicity. In summary, this study provides a novel strategy for BSH delivery and may broaden the design vision of BNCT nano-boron capture agents.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":"7 1","pages":"1-20"},"PeriodicalIF":3.4,"publicationDate":"2024-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142257944","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

Intranasal Delivery of Sulpiride Nanostructured Lipid Carrier to Central Nervous System; In Vitro Characterization and In Vivo Study. 将舒必利纳米结构脂质载体鼻内递送至中枢神经系统；体外表征和体内研究

IF 3.4 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-09-12 DOI: 10.1080/10837450.2024.2404034

Hesham M Tawfeek,Aml I Mekkawy,Ahmed A H Abdelatif,Basmah N Aldosari,Waleed A Mohammed-Saeid,Marwa G Elnaggar

{"title":"Intranasal Delivery of Sulpiride Nanostructured Lipid Carrier to Central Nervous System; In Vitro Characterization and In Vivo Study.","authors":"Hesham M Tawfeek,Aml I Mekkawy,Ahmed A H Abdelatif,Basmah N Aldosari,Waleed A Mohammed-Saeid,Marwa G Elnaggar","doi":"10.1080/10837450.2024.2404034","DOIUrl":"https://doi.org/10.1080/10837450.2024.2404034","url":null,"abstract":"The low and erratic oral absorption of sulpiride (SUL) a dopaminergic receptor antagonist, and its P-glycoprotein efflux in the gastrointestinal tract restricted its oral route for central nervous system disorders. An intranasal formulation was formulated based on nanostructured lipid carrier to tackle these obstacles and deliver SUL directly to the brain. Sulipride-loaded nanostructured lipid carrier (SUL-NLC) was prepared using compritol®888 ATO and different types of liquid lipids and emulsifiers. SUL-NLCs were characterized for their particle size, charge, and encapsulation efficiency. Morphology and compatibility with other NLC excipients were also studied. Moreover, SUL in vitro release, nanodispersion stability, in vivo performance and SUL pharmacokinetics were investigated. Results delineates that SUL-NLC have a particle size ranging from 366.2 ± 62.1 to 640.4 ± 50.2 nm and encapsulation efficiency of 75.5 ± 1.5%. SUL showed a sustained release pattern over 24 h and maintained its physical stability for three months. Intranasal SUL-NLC showed a significantly (p < 0.01) higher SUL brain concentration than that found in plasma after oral administration of commercial SUL product with 4.47-fold increase in the relative bioavailability. SUL-NLCs as a nose to brain approach is a promising formulation for enhancing the SUL bioavailability and efficient management of neurological disorders.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":"8 1","pages":"1-25"},"PeriodicalIF":3.4,"publicationDate":"2024-09-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142218988","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

Co-crystallization of Hesperidin with different co-formers to enhance solubility, antioxidant and anti-inflammatory activities. 将橙皮甙与不同共形物共结晶，以提高其溶解度、抗氧化性和抗炎活性。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-09-01 Epub Date: 2024-07-24 DOI: 10.1080/10837450.2024.2378498

Mahmoud Elshaer, Shaaban K Osman, Ahmed M Mohammed, Gamal Zayed

{"title":"Co-crystallization of Hesperidin with different co-formers to enhance solubility, antioxidant and anti-inflammatory activities.","authors":"Mahmoud Elshaer, Shaaban K Osman, Ahmed M Mohammed, Gamal Zayed","doi":"10.1080/10837450.2024.2378498","DOIUrl":"10.1080/10837450.2024.2378498","url":null,"abstract":"Hesperidin (HSP) is a natural flavonoid glycoside with very low aqueous solubility and a slow dissolution rate, limiting its effectiveness. This study aims to address these issues by creating co-crystals of hesperidin with water-soluble small molecules (co-formers) such as L-arginine, glutathione, glycine, and nicotinamide. Using the solvent drop grinding method, we prepared three different molar ratios of hesperidin to co-formers (1:1, 1:3, and 1:5) and conducted in-vitro solubility and dissolution studies. The results demonstrated that the prepared co-crystals exhibited significantly enhanced solubility and dissolution rates compared to untreated hesperidin. Of particular note, the HSP co-crystals formula (HSP: L-arg 1:5) displayed approximately 4.5 times higher dissolution than pure hesperidin. Further analysis using FTIR, powder x-ray diffraction patterns, and DSC thermograms validated the formation of co-crystals between HSP and L-arginine. Additionally, co-crystallization with L-arginine improved the in vitro anti-inflammatory and antioxidant activities of hesperidin compared to the untreated drug. This study highlights the potential of using water-soluble small molecules (co-formers) through co-crystallization to enhance the solubility, dissolution, and biological activities of poorly water-soluble drugs. Furthermore, in vivo studies are crucial to validate these promising results.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"691-702"},"PeriodicalIF":2.6,"publicationDate":"2024-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141752370","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