Pharmaceutical Development and Technology最新文献_第5页

In vitro skin permeation of flavonoid esters enzymatically derived from natural oils: release mechanism from gel emulsion, stability, and dermatological compatibility. 从天然油中酶解提取的类黄酮酯的体外皮肤渗透性：凝胶乳液的释放机制、稳定性和皮肤相容性。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-12-01 Epub Date: 2024-11-09 DOI: 10.1080/10837450.2024.2424977

Ana Milivojević, Marija Ćorović, Anja Petrov Ivanković, Milica Simović, Katarina Banjanac, Rada Pjanović, Dejan Bezbradica

{"title":"In vitro skin permeation of flavonoid esters enzymatically derived from natural oils: release mechanism from gel emulsion, stability, and dermatological compatibility.","authors":"Ana Milivojević, Marija Ćorović, Anja Petrov Ivanković, Milica Simović, Katarina Banjanac, Rada Pjanović, Dejan Bezbradica","doi":"10.1080/10837450.2024.2424977","DOIUrl":"10.1080/10837450.2024.2424977","url":null,"abstract":"Due to their broad spectrum of biological activities and attractive pharmacological properties, flavonoids are very promising molecules for application in skin care products. In this study, phloridzin and naringin medium- and long-chain fatty acid esters were enzymatically synthesized in reaction with natural oils (coconut and linseed oil) and in vitro transdermal delivery of synthesized esters through artificial Strat-M® membrane was investigated. Experimental results were succesfully fitted using Peppas and Sahlin model which includes the lag phase. Release kinetics of all examined flavonoid esters from gel emulsions through the membrane depended on both diffusion and polymer relaxation effect (0.5<n < 1). The estimated effective diffusion coefficients ranged from 0.168·10-8 to 6.149·10-8 cm2 s-1 for phloridzin esters and from 0.116·10-8 to 4.210·10-8 cm2 s-1 for naringin esters. The effective diffusion coefficients decreased with the increase in ester molecular weight indicating the size-dependent diffusion. All formulation showed good stability, excellent hydration effect, and excellent dermatological compatibility without irritating effect. It can be concluded that gel emulsions with a mixture of flavonoid esters enzymatically synthesized in reaction with vegetable oils can be effectively topically applied as a skin care products.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1121-1132"},"PeriodicalIF":2.6,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142576468","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

Correction. 更正。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-12-01 Epub Date: 2024-11-18 DOI: 10.1080/10837450.2024.2428508

引用次数: 0

Meloxicam-amino acids salts/ion pair complexes with advanced solubility, dissolution, and gastric safety. 美洛昔康-氨基酸盐/离子对复合物，具有更高的溶解度、溶解性和胃安全性。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-12-01 Epub Date: 2024-10-24 DOI: 10.1080/10837450.2024.2417766

Hamdy Abdelkader, Adel Al Fatease, Zeinab Fathalla, Mai E Shoman, Heba A Abou-Taleb

{"title":"Meloxicam-amino acids salts/ion pair complexes with advanced solubility, dissolution, and gastric safety.","authors":"Hamdy Abdelkader, Adel Al Fatease, Zeinab Fathalla, Mai E Shoman, Heba A Abou-Taleb","doi":"10.1080/10837450.2024.2417766","DOIUrl":"10.1080/10837450.2024.2417766","url":null,"abstract":"Amino acids have attracted attention as a potential functional excipient for optimizing biopharmaceutics characteristics of poorly soluble drugs. The amino acids are a diverse class with many functional groups, natural compounds, biocompatible, and low-molecular-weight substances. Two amino acids serine and arginine were investigated with meloxicam. Meloxicam has extremely low solubility; being NSAIDs, gastric upset, and ulcer are common side effects. Solid dispersions were produced by precipitation and physical mixing techniques. The produced combinations underwent in vitro dissolution, docking, DSC, FTIR, XRD, solubility, and gastric ulcer formation studies. Docking indicated ion pair/salt formation between the basic amino acid arginine and meloxicam. Both solubility and dissolution rates were increased by up to 3000-fold and 12-fold, respectively. DSC, FTIR an XRD supported these findings. Rats treated with meloxicam showed loss of surface gastric epithelium integrity and ulceration. The animal group received meloxicam: arginine showed intact gastric mucosa with the surface epithelium and gastric glands well organized and nearly similar to the untreated control. Arginine with the guanidine group that was capable of preserving gastric mucosa after repeated administration for 10 days. This study highlighted the role of arginine as a functional excipient that did not only improve solubility and dissolution rates but ameliorated the long-standing gastric side effects attributed to meloxicam.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1075-1083"},"PeriodicalIF":2.6,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142472338","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

Ionic liquids and their potential use in development and improvement of drug delivery systems: evidence of their tendency to promote drug accumulation in the brain. 离子液体及其在开发和改进给药系统中的潜在用途：有证据表明离子液体有促进药物在大脑中蓄积的倾向。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-12-01 Epub Date: 2024-10-18 DOI: 10.1080/10837450.2024.2417004

William Eades, Shayan Abdolmohammadpourbonab, Linh Dinh, Bingfang Yan

{"title":"Ionic liquids and their potential use in development and improvement of drug delivery systems: evidence of their tendency to promote drug accumulation in the brain.","authors":"William Eades, Shayan Abdolmohammadpourbonab, Linh Dinh, Bingfang Yan","doi":"10.1080/10837450.2024.2417004","DOIUrl":"10.1080/10837450.2024.2417004","url":null,"abstract":"Ionic liquids (ILs) are considered salt in liquid state, which is composed of organic cations and anions with low melting points (<100 °C). ILs have become a major scientific area with an extensive range of applications including chemistry, electrochemistry, and pharmaceutics. ILs have received great research interest in the pharmaceutical field as solvents, anti-solvents, co-solvents, and reagents in synthesis and formulation. While therapeutic ILs have been investigated for oral and trans-dermal drug delivery systems showing promising compatibility with a wide range of therapeutics, enhanced drug permeation through the skin, and cell membrane solvation to open channels to facilitate molecular passage, their potential to cross the challenging blood-brain barrier (BBB) remains an unanswered question. IL-based therapies could potentially be a game changer for improving drug delivery to cellular targets both at and across the BBB. In this review, we discuss (1) the tunable physicochemical properties of ILs; (2) the vast and various applications of ILs in the development and improvement of drug delivery systems; and (3) ILs as a potential approach for increasing drug accumulation in the brain tissue.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1065-1074"},"PeriodicalIF":2.6,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11649452/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142472337","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

In vitro cellular uptake and insulin secretion studies on INS-1E cells of exendin-4-loaded self-nanoemulsifying drug delivery systems. 装载 Exendin-4 的自纳米乳化给药系统对 INS-1E 细胞的体外细胞吸收和胰岛素分泌研究。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-12-01 Epub Date: 2024-11-08 DOI: 10.1080/10837450.2024.2423823

Merve Çelik Tekeli, Yaprak Yalçın, Hasibe Verdi, Yeşim Aktaş, Nevin Çelebi

{"title":"In vitro cellular uptake and insulin secretion studies on INS-1E cells of exendin-4-loaded self-nanoemulsifying drug delivery systems.","authors":"Merve Çelik Tekeli, Yaprak Yalçın, Hasibe Verdi, Yeşim Aktaş, Nevin Çelebi","doi":"10.1080/10837450.2024.2423823","DOIUrl":"10.1080/10837450.2024.2423823","url":null,"abstract":"Exendin-4 (ex-4) is a peptide molecule that regulates blood glucose levels without causing hypoglycemia by providing insulin secretion from beta cells in the pancreas. Self-nanoemulsifying drug delivery systems (SNEDDS) attract attention for oral administration of therapeutic peptide/proteins because they protect therapeutic peptide/proteins from the gastric environment, reduce changes due to food effects, are easy to prepare and scale-up. Ex-4 has no commercial form that can be administered orally. In this study, the cytotoxicity, cellular uptake, and insulin secretion of ex-4 and ex-4/chymostatin (chym) SNEDDS were investigated on INS-1E rat pancreatic beta cells. The effect of ex-4 and ex-4/chym SNEDDS on cell viability in INS-1E cells increased when the dilution ratio higher. Ex-4 and ex-4/chym SNEDDS increased insulin levels in 2.8 mM (low-dose) glucose-induced INS-1E cells 2.21-fold and 2.17-fold compared to control, respectively. Ex-4 and ex-4/chym SNEDDS increased insulin levels in 16.7 mM (high dose) glucose-induced INS-1E cells compared to control, respectively. In cellular uptake studies, coumarin-6 solution penetrated the apical membrane of INS-1E cells and remained in the cytoplasm, while coumarin-6 loaded SNEDDS were visualized in the nuclei of the cell. These findings will likely be useful in the development of new formulations for the oral administration of peptides/proteins.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1101-1110"},"PeriodicalIF":2.6,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142546706","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

Nanoformulated fenbendazole as an attractive approach for treating neurocysticercosis: in vitro and in vivo studies. 纳米配方芬苯达唑作为治疗神经囊虫病的一种有吸引力的方法：体外和体内研究。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-12-01 Epub Date: 2024-11-09 DOI: 10.1080/10837450.2024.2422936

Yngrid Batista da Silva, Giselle Bedogni, Guaraciara de Andrade Picanço, Jéssica Yonara de Souza, Waylla Silva Nunes, Tatiane Luiza da Costa, Geovana Batista de Campos, Lina Vargas Michelena, Claudio Javier Salomon, Marina Clare Vinaud

{"title":"Nanoformulated fenbendazole as an attractive approach for treating neurocysticercosis: in vitro and in vivo studies.","authors":"Yngrid Batista da Silva, Giselle Bedogni, Guaraciara de Andrade Picanço, Jéssica Yonara de Souza, Waylla Silva Nunes, Tatiane Luiza da Costa, Geovana Batista de Campos, Lina Vargas Michelena, Claudio Javier Salomon, Marina Clare Vinaud","doi":"10.1080/10837450.2024.2422936","DOIUrl":"10.1080/10837450.2024.2422936","url":null,"abstract":"Purpose: This work aimed to develop fenbendazole nanocrystals to evaluate their effects on the energetic metabolism of Taenia crassiceps cysticerci, following an intracranial inoculation in mice.Methods: Fenbendazole was nanoformulated by the antisolvent method using poloxamers 188 and 407 as stabilizers. The nanosuspensions were lyophilized without cryoprotectants and the nanocrystals were characterized in terms of particle size, zeta potential, and dissolution performance. The in vivo study was performed in infected animals treated with nanoformulated fenbendazole and raw drug and their metabolic impact was quantified by analyzing specific metabolites.Results: Fenbendazole samples were obtained by nanoprecipitation in > 80% yield. The average particle size of the freeze-dried samples was between 372 nm and 1600 nm. The nanosystems released a greater amount of the drug into the solution, compared to the raw drug. The in vivo studies showed that the fenbendazole-treated groups induced gluconeogenesis, partial blockage of the TCA cycle, and increased protein catabolism. As seen, the nanoformulation presented a greater effect on these parameters than the raw drug leading to remarkable modifications in the metabolism of the parasite, which in turn can influence the overall course of the infection and treatment outcomes.Conclusion: These findings suggest that nanoformulated fenbendazole may be considered a valuable approach for an effective treatment of neurocysticercosis.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1093-1100"},"PeriodicalIF":2.6,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142605848","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

Spray dried polymyxin B liposome for inhalation against gram-negative bacteria. 喷雾干燥多粘菌素 B 脂质体，用于吸入治疗革兰氏阴性菌。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-12-01 Epub Date: 2024-11-19 DOI: 10.1080/10837450.2024.2427186

Thaddeus Harrison Gugu, Emmanuel Maduabuchi Uronnachi, Ekawat Thawithong, Teerapol Srichana

{"title":"Spray dried polymyxin B liposome for inhalation against gram-negative bacteria.","authors":"Thaddeus Harrison Gugu, Emmanuel Maduabuchi Uronnachi, Ekawat Thawithong, Teerapol Srichana","doi":"10.1080/10837450.2024.2427186","DOIUrl":"10.1080/10837450.2024.2427186","url":null,"abstract":"This study aimed to provide an alternative and effective delivery system to combat polymyxin B (PMB) toxicity and bacterial resistance through inhalation therapy. PMB was formulated as liposomal dry powder for inhalation using thin-film hydration and spray-dried methods. PMB formulations were characterized physically. The aerodynamic properties were determined using next-generation impactor (NGI). In vitro drug release was done in a phosphate buffer pH 7.4 for 2 h. Cytotoxicity was evaluated by the MTT cell viability assay. Antimicrobiological activities were done using bioassay and flow cytometry. Particle sizes of the spay-dried formulations were between 259.83 ± 9.91 and 518.73 ± 27.08 nm while the zeta potentials ranged between 3.07 ± 0.27 and 4.323 ± 0.36 mV. The Fourier-transform infrared spectroscopy shows no interaction between PMB and other excipients. Differential scanning calorimetry thermograms revealed amorphousness of the formulated powders and SEM revealed spherical PMB formulations. Similarly, mass media aerodynamic diameter results were 1.72-2.75 nm, and FPF was 25%-26%. The cumulative release of the PMB formulations was 90.3 ± 0.6% within 2 h. The killing kinetics revealed total cell death at 12 and 24 h for Pseudomonas aeruginosa and Escherichia coli, respectively. The PMB inhalation liposome showed better activity and was safe for lung-associated cell lines.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1133-1147"},"PeriodicalIF":2.6,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142605850","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

Bioavailability enhancement of formononetin by incorporation of natural bioenhancer in phospholipid complex. 通过在磷脂复合物中加入天然生物增强剂提高福莫西汀的生物利用率

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-12-01 Epub Date: 2024-11-17 DOI: 10.1080/10837450.2024.2427838

Arun Agarwal, Shailesh Dadge, Richa Garg, Rakesh Kumar Sharma, Divya Chauhan, Roshan Katekar, Shivam Rathaur, Kalyan Mitra, Jiaur R Gayen

{"title":"Bioavailability enhancement of formononetin by incorporation of natural bioenhancer in phospholipid complex.","authors":"Arun Agarwal, Shailesh Dadge, Richa Garg, Rakesh Kumar Sharma, Divya Chauhan, Roshan Katekar, Shivam Rathaur, Kalyan Mitra, Jiaur R Gayen","doi":"10.1080/10837450.2024.2427838","DOIUrl":"10.1080/10837450.2024.2427838","url":null,"abstract":"Formononetin (FNT) has limited application due to poor water solubility and substantial phase II metabolism. In the present study, we used phospholipid complex (PC) containing FNT and UDP-glucuronosyltransferase (UGT1A1) inhibitor piperine (PIP) to overcome FNT limitations. We characterized and compared both FNT-PC and FNT-PIP-PC complexes. Our data showed both groups improved FNT water solubility and oil-water partition coefficient. NMR, DSC, and SEM were performed to identify the interaction and the geometrical nature of complex. When compared, FNT-PIP-PC released more FNT in in vitro release and permeation through Caco-2 monolayer than FNT-PC and pure FNT. In vitro data was consistent with the in vivo pharmacokinetic profile that showed increased, Cmax and AUC(0-24) by 7.16 and 23.33-fold and 29.65 and 23.33-fold at 5 and 10 mg/kg in FNT-PIP-PC, compared to pure FNT. Additionally, co-treatment of PIP and FNT improved in vitro pharmacological action in dexamethasone-induced osteoporosis. Thus, our study showed addition of PIP in FNT-PC further increases FNT water solubility and protects it from phase II metabolism, leading to enhanced bioavailability with improved pharmacological activity.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1148-1161"},"PeriodicalIF":2.6,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142625992","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

Transforming canagliflozin solubility using lipidic carrier and its pharmacokinetic study. 脂质载体转化卡格列净溶解度及药动学研究。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-12-01 Epub Date: 2024-12-05 DOI: 10.1080/10837450.2024.2436184

Rutuja Deshmukh, Subhash Deshmane, Atish Sawant, Snehal Deshmane, Shirish Jain

{"title":"Transforming canagliflozin solubility using lipidic carrier and its pharmacokinetic study.","authors":"Rutuja Deshmukh, Subhash Deshmane, Atish Sawant, Snehal Deshmane, Shirish Jain","doi":"10.1080/10837450.2024.2436184","DOIUrl":"10.1080/10837450.2024.2436184","url":null,"abstract":"The European Medicine Agency has approved canagliflozin (CGF) drug to improve glycemic control in patients with type II diabetes. Our study aimed to enhance the solubility and pharmacokinetics of canagliflozin. Since crystalline canagliflozin is insoluble in water, its absolute bioavailability is less than 65%. Gelucire 50/13 was used as a lipid-based drug carrier to create solid dispersions of canagliflozin. SEM, PXRD, and DSC analysis all pointed to canagliflozin as having a crystal structure. Fusion and solvent evaporation methods were used to prepare the solid dispersions. In solid dispersions, the medication was found to be amorphized according to SEM, DSC, and PXRD studies. The water solubility of canagliflozin increased significantly by 11-23 fold using the solvent evaporation approach and by 12-25 fold using the fusion method. The pharmacokinetic parameters are improved at higher concentrations of gelucire. With pure canagliflozin, the AUC values climbed over 4 h (tmax) to 23440 µgh/mL, while with GDF 1:7, they grew to 52217. Gelucire 50/13 is an excellent option as a biomaterial carrier for drug delivery systems that use solid dispersion because it enhances biological membrane penetration. By dispersing the canagliflozin and gelucire, bioavailability may be enhanced by the fusion process that achieves molecular binding.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1175-1184"},"PeriodicalIF":2.6,"publicationDate":"2024-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142786438","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

Caspofungin formulations for buccal and sublingual mucosae anti-fungal infections: physicochemical characterization, rheological analysis, release and ex vivo permeability profiles. 用于颊黏膜和舌下黏膜抗真菌感染的卡泊芬净制剂：理化特性、流变分析、释放和体内外渗透性概况。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2024-11-01 Epub Date: 2024-10-17 DOI: 10.1080/10837450.2024.2415545

Noelia Pérez-González, José A Morales-Molina, Ana C Calpena-Campmany, Lyda Halbaut, María J Rodríguez-Lagunas, Nuria Bozal-de Febrer, Eliana B Souto, Mireia Mallandrich, Beatriz Clares-Naveros

{"title":"Caspofungin formulations for buccal and sublingual mucosae anti-fungal infections: physicochemical characterization, rheological analysis, release and ex vivo permeability profiles.","authors":"Noelia Pérez-González, José A Morales-Molina, Ana C Calpena-Campmany, Lyda Halbaut, María J Rodríguez-Lagunas, Nuria Bozal-de Febrer, Eliana B Souto, Mireia Mallandrich, Beatriz Clares-Naveros","doi":"10.1080/10837450.2024.2415545","DOIUrl":"10.1080/10837450.2024.2415545","url":null,"abstract":"Aim: Oral candidiasis is often challenging due to limited effectiveness of topical treatments. This study aimed to develop novel caspofungin formulations for administration onto the oral mucosa to enhance drug retention and efficacy.Method: Five caspofungin (2%, w/v) formulations were developed to assess their permeability, retention and mucoadhesiveness. Ex vivo permeability assays were performed on buccal and sublingual mucosae, and histological analyses conducted to evaluate tissue tolerance.Results: Formulation composed of chitosan demonstrated the highest retention in both buccal (5183.24 ± 587.32 µg/cm2) and sublingual (1090.72 ± 110.26 µg/cm2) mucosae. Other formulations exhibited significantly lower retention, ranging from 7.53 ± 0.81 to 1852.10 ± 193.24 µg/cm2 in buccal mucosa and 1.64 ± 0.14 to 317.74 ± 31.78 µg/cm2 in sublingual mucosa. Chitosan-based formulation exhibited the highest mucoadhesive strength, with values of 5179.05 ± 31.99 mN/cm2 for buccal and 7026.10 ± 123.41 mN/cm2 for sublingual mucosae, and also superior extensibility, which facilitates application in the oral cavity. All formulations showed antifungal activity against Candida spp., and histological analyses revealed minor epithelial alterations.Conclusion: The developed formulations offer distinct advantages for treating oral candidiasis, with chitosan formulation emerging as the most promising due to its superior retention, mucoadhesion force, and spreadability, making it a potential candidate for further clinical investigation.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1042-1063"},"PeriodicalIF":2.6,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142472335","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