Journal of Pharmacy and Pharmaceutical Sciences最新文献

{"title":"Harnessing DNA polymerase beta defect enhances synthetic lethality and treatment response in gastric cancer cells: implication for immunotherapy.","authors":"Aashirwad Shahi, Shengyuan Zhao, Dawit Kidane","doi":"10.3389/jpps.2025.15360","DOIUrl":"10.3389/jpps.2025.15360","url":null,"abstract":"<p><p>Gastric cancer remains a highly prevalent and accounts for a notable proportion of global cancer mortality. Both Intrinsic and exogenous agents can exacerbate reactive oxygen species (ROS) related oxidized DNA base lesions and single stranded DNA breaks (SSBs). Base excision repair (BER) serves as the primary defense mechanism for repairing DNA damage induced by oxidative stress. DNA polymerase beta (Pol β) plays a critical role in BER and non-homologous end joining repair pathways. The Pol β is the first perform gap-filling DNA synthesis by its polymerase activity and then cleave a 5'-deoxyribose-5-phosphate (dRP) moiety via its dRP lyase activity. Furthermore, defect in POLB promotes genetic liability of the cancer cells for different targeted and synthetic lethality-based treatment strategies. In this review, we have provided a potential example to illustrate the mechanistic insight how PARP1 inhibitor (Olaparib) induces replication associated double strand breaks in POLB deficient cells and DNA mediated innate immune signal activation that likely enhances immune based therapy. Based on our previously published data and the current recent findings, POLB status of the patient likely provide genetic indicators to stratify gastric cancer patient. Overall, in this review article, we presented a new direction to highlight the opportunity to exploit POLB genetic defect in cancer cells to enhance treatment response and to explore synergistic effect to target gastric cancer cells that harbor aberrant DNA polymerase beta function with immune based therapeutic strategy.</p>","PeriodicalId":50090,"journal":{"name":"Journal of Pharmacy and Pharmaceutical Sciences","volume":"28 ","pages":"15360"},"PeriodicalIF":5.5,"publicationDate":"2026-01-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12815885/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146020647","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}

{"title":"Formulation and Evaluation of Apigenin-Loaded Topical Organogel for the Wound Healing","authors":"Athmar Dhahir Habeed Alshohani","doi":"10.62472/kjps.v16.i27.147-156","DOIUrl":"https://doi.org/10.62472/kjps.v16.i27.147-156","url":null,"abstract":"Wound healing is a complicated process that requires the use of many medications including anti-inflammatory and antioxidants. A naturally occurring flavonoid, apigenin can be found in a variety of fruits, vegetables, and medicinal plants that has versatile benefits and medical uses including wound healing, antioxidant, antiaging and others. Organogel is one of the promising topical drug delivery strategies which have many potentials in drug delivery effect. Organogel will be used for the topical delivey of apigenin. Different organogels were prepared by using lecithin, isopropyl myristate, pluronic F127, PEG 400 and water. The formulations were evaluated for their gelation temperature, pH, drug content, viscosity and drug release. The results demonstrated that without PEG 400 only 55% of the drug was released after 6 hours while 91% was released when PEG 400 was used. Formulation F5 was the optimum formula with appropriate viscosity (3372 mPs), pH (6.33), drug content (91%) and 27◦C gelation temperature. Drug release was around 91% within 6 hours. The formulated APN topical organogel will have the potential to improve wound healing by delivering the medication to the wound site in a sustained and localized approach.","PeriodicalId":50090,"journal":{"name":"Journal of Pharmacy and Pharmaceutical Sciences","volume":"16 27","pages":"147-156"},"PeriodicalIF":0.0,"publicationDate":"2025-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147909050","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}

{"title":"Intrahepatic cholestasis of pregnancy associated with azathioprine: first quantitative disproportionality analysis using the FDA adverse event reporting system.","authors":"Yonghoon Kwon, Nai Lee, Yun Kim","doi":"10.3389/jpps.2025.15527","DOIUrl":"10.3389/jpps.2025.15527","url":null,"abstract":"<p><strong>Introduction: </strong>Azathioprine (AZA) is an immunosuppressant approved for renal transplant rejection and rheumatoid arthritis. Recent FDA alerts have raised concerns about its link to intrahepatic cholestasis of pregnancy (ICP), a condition with serious maternal and fetal risks. This study used disproportionality analysis as a hypothesis-generating approach to evaluate the reporting association between AZA and ICP during pregnancy and to compare AZA with other drugs previously implicated in ICP.</p><p><strong>Methods: </strong>A retrospective pharmacovigilance study was conducted using the FDA Adverse Event Reporting System (FAERS) reports from 1968 to Q2 2024. Disproportionality analysis was performed using reporting odds ratios (RORs), with statistical significance defined as a lower limit of the 95% confidence interval (CI) >1 and at least three unique cases. Subgroup analyses were conducted by pregnancy status and underlying autoimmune indications, and comparative analyses were performed against drugs previously reported to induce ICP.</p><p><strong>Results: </strong>Among 35,576 AZA-related reports, 67 specifically documented ICP. A strong signal was detected for ICP ROR025 = 153.0; IC025 = 5.8; EBGM05 = 144.37), ranking among the highest AZA-associated adverse events. In pregnant women, ICP also showed a significant signal (ROR025 = 5.46; IC025 = 1.93; EBGM05 = 5.31). Subgroup analyses by indication revealed elevated risks in Crohn's disease (ROR025 = 66.99; IC025 = 4.8; EBGM05 = 64.73), and Colitis ulcerative (ROR025 = 9.01; IC025 = 1.95; EBGM05 = 9.95). Comparative analyses demonstrated that AZA had a higher proportion of ICP cases than other drugs reported to induce ICP.</p><p><strong>Conclusion: </strong>This pharmacovigilance analysis identifies a disproportionality signal suggesting a possible association between AZA and intrahepatic cholestasis of pregnancy. These hypothesis-generating findings underscore the importance of cautious use and clinical vigilance when prescribing AZA to women of reproductive age.</p>","PeriodicalId":50090,"journal":{"name":"Journal of Pharmacy and Pharmaceutical Sciences","volume":"28 ","pages":"15527"},"PeriodicalIF":5.5,"publicationDate":"2025-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12748001/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145879349","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}

{"title":"Pharmacological increases in circulating ketones fail to alleviate the hypertrophic cardiomyopathy present in the Tafazzin knockdown mouse model of Barth syndrome.","authors":"Tanin Shafaati, Amanda A Greenwell, Christina T Saed, Seyed Amirhossein Tabatabaei Dakhili, Jordan S F Chan, Linyue Dong, Magnus J Stenlund, Sally R Ferrari, Ruth Han, Jennifer Kruger, Farah Eaton, Keshav Gopal, Sandra T Davidge, Gavin Y Oudit, John R Ussher","doi":"10.3389/jpps.2025.15688","DOIUrl":"10.3389/jpps.2025.15688","url":null,"abstract":"<p><strong>Objective: </strong>Mutations in the <i>tafazzin</i> gene lead to impaired remodeling of cardiolipin, thereby impairing mitochondrial function and causing Barth syndrome (BTHS), a rare X-linked genetic disorder characterized by cardiomyopathy. Previous studies in a mouse model of BTHS, secondary to knockdown of <i>Tafazzin</i> (TazKD mice), also observed perturbations in mitochondrial substrate metabolism and a hypertrophic cardiomyopathy. BTHS may be characterized by increased cardiac ketone metabolism, as myocardial protein expression of the ketolytic enzyme, β-hydroxybutyrate dehydrogenase 1 (BDH1), was markedly increased in TazKD mice. We therefore determined whether increasing ketone supply in TazKD mice may have therapeutic utility against their cardiac abnormalities.</p><p><strong>Methods: </strong>We treated TazKD mice and their wild-type littermates with either the sodium-glucose cotransporter-2 inhibitor, empagliflozin (10 mg/kg), or a ketone ester (KE; 1719 mg/kg) once daily for 7-week, and performed ultrasound echocardiography to assess cardiac structure and function.</p><p><strong>Results: </strong>Treatment of TazKD mice with either empagliflozin or a KE increased circulating ketone levels. However, neither approach proved capable of alleviating the cardiac hypertrophy present in TazKD mice, as their increased left ventricular wall thickness and decreased left ventricular diameter remained comparable to that observed in vehicle control treated animals. We also observed that empagliflozin and KE treatment did not impact key markers of cardiac hypertrophy in TazKD mice.</p><p><strong>Conclusion: </strong>Increasing circulating ketone levels did not alleviate the cardiac hypertrophy in TazKD mice, suggesting that such an approach would not improve outcomes in BTHS.</p>","PeriodicalId":50090,"journal":{"name":"Journal of Pharmacy and Pharmaceutical Sciences","volume":"28 ","pages":"15688"},"PeriodicalIF":4.3,"publicationDate":"2025-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12711585/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145806317","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}

{"title":"Compounding and stability studies of liquid oral formulations of beta-blockers (bisoprolol, betaxolol, and nadolol) for paediatric patients.","authors":"Laura Dubois, Cyrielle Bouguergour, Romain Paoli-Lombardo, Caroline Castera-Ducros, Christophe Jean, Mélanie Fuchs, Patrice Vanelle, Pascal Rathelot, Thierry Terme, Christophe Curti","doi":"10.3389/jpps.2025.15387","DOIUrl":"10.3389/jpps.2025.15387","url":null,"abstract":"<p><p>In paediatric wards, bisoprolol, betaxolol, or nadolol can be administered orally at non-licensed dosages. To provide paediatric patients with appropriate treatment, batches of beta-blocker oral suspensions must be compounded, which involves subsequent stability studies. A stability-indicating HPLC-UV method and microbiological analyses were validated. Experimental batches were compounded (betaxolol hydrochloride 1 mg.mL^-1, bisoprolol hemifumarate 0.5 mg.mL^-1 and nadolol 10 mg.mL^-1). Bisoprolol hemifumarate 0.5 mg.mL^-1 and nadolol 10 mg.mL^-1 needed the addition of citric acid (3 mg.mL^-1) and potassium sorbate (3 mg.mL^-1) to ensure preservative efficacy. Betaxolol hydrochloride 1 mg.mL^-1 was stable for 2 months when stored at 2-8  °C, for 1 month after opening at 2-8 °C, and for 15 days when stored at 25 °C/60% RH. Bisoprolol hemifumarate 0.5 mg.mL^-1 was stable for 2 months when stored at 2-8 °C, for 1 month after opening at 2-8 °C, and for 15 days when stored at 25 °C/60% RH. Nadolol 10 mg.mL^-1 was stable for 3 months when stored at 2-8 °C, for 1 month after opening at 2-8 °C, and for 15 days when stored at 25 °C/60% RH. Hospital pharmacies can compound batches of beta-blocker liquid oral suspensions and store them for secure dispensing and administration.</p>","PeriodicalId":50090,"journal":{"name":"Journal of Pharmacy and Pharmaceutical Sciences","volume":"28 ","pages":"15387"},"PeriodicalIF":5.5,"publicationDate":"2025-12-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12705468/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145776299","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}

{"title":"Reuse of unused medications: a cross-sectional study on public willingness and influencing factors.","authors":"Faten Alhomoud, Sakinah Alalwyat, Lama Alanzi, Farah Kais Alhomoud, Sarah Khayyat, Khalid A Alamer, Basmah Alfageh, Mohra Aladwani, Abdullah A Alhifany","doi":"10.3389/jpps.2025.15249","DOIUrl":"10.3389/jpps.2025.15249","url":null,"abstract":"<p><p>Medication waste is a significant global concern with environmental, economic, and healthcare implications. In Saudi Arabia, approximately 25.8% of dispensed medications are wasted, resulting in an annual cost of $150 million. Re-dispensing unused medications has been proposed to reduce this waste; however, its feasibility depends on public acceptance, regulatory frameworks, and assurances of safety. This study aimed to assess the Saudi public's willingness to accept re-dispensed medications returned unused to pharmacies and to identify factors influencing this willingness. A descriptive cross-sectional survey was conducted online across Saudi Arabia. The questionnaire, adapted from a validated tool by McRae et al. McRae et al. (Pharmacy (Basel), 2021, 9(2): 77) and translated into Arabic, explored demographics, medication practices, storage and disposal, and attitudes towards medication waste and re-dispensing. The survey was distributed via social media. Data were analyzed using SPSS version 29, including chi-squared tests and binary logistic regression. A total of 405 participants completed the survey, primarily female (64%) and aged 25-44 years (43%). About 64% reported having unused medications at home, most commonly stored in bedrooms (55.1%) and kitchens (53.6%). Disposal practices included keeping medicines for future use (62.5%), discarding them with household waste (45.7%), sharing them with others (21.5%), and returning unused medications to a pharmacy (8.4%). Approximately 60% were willing to accept re-dispensed tablets and 55% capsules, whereas fewer accepted other dosage forms. Key factors influencing acceptance included pharmacist verification of quality and integrity (79.3%), informed consent (77.3%), expiry dates (77%), and intact packaging (74.8%). Most participants (68.1%) indicated they would return unused medicines if a re-dispensing program were implemented, and half (50.6%) believed all medications, not only expensive ones, should be considered. Significant predictors of willingness included age (P < 0.001), employment status (P = 0.004), regular prescription use (P = 0.046), and concern about waste (P < 0.001). Younger participants showed higher acceptance, while employed individuals, retirees, and regular medication users were more hesitant. The findings indicate cautious yet notable public support for medication re-dispensing in Saudi Arabia, particularly for oral solid dosage forms, provided rigorous safety measures are assured. Policymakers should consider these insights to guide initiatives aimed at reducing medication waste.</p>","PeriodicalId":50090,"journal":{"name":"Journal of Pharmacy and Pharmaceutical Sciences","volume":"28 ","pages":"15249"},"PeriodicalIF":5.5,"publicationDate":"2025-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12702787/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145769630","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}

{"title":"Hypoglycemia and associated cardiovascular diseases, morbidity and mortality in patients with type 2 diabetes mellitus in university teaching hospitals in Rwanda.","authors":"Jean Baptiste Nyandwi, Pierre Celestin Munezero, Charles Uwambajimana, Gift Crucifix Pender, Jonathan Katandula, Théoneste Umumararungu, Jean Paul Sinumvayo, Ibrahim Eleha Suleiman, Tolessa Muleta Daba, Vedaste Kagisha, Marie Françoise Mukanyangezi, Ahmed Adebowale Adedeji","doi":"10.3389/jpps.2025.14880","DOIUrl":"10.3389/jpps.2025.14880","url":null,"abstract":"<p><strong>Background: </strong>Hypoglycemia is a common yet underrecognized complication in patients with type 2 diabetes mellitus (T2DM), often linked with increased cardiovascular (CV) morbidity and mortality. Despite its clinical importance, there is a limited data on the association between hypoglycemia, CV events, and mortality among T2DM patients in Rwanda. This study investigated the occurrence of hypoglycemia and its association with CV diseases, morbidity, and mortality in T2DM patients attending two university teaching hospitals in Rwanda.</p><p><strong>Methods: </strong>A retrospective study was conducted using secondary data from 267 T2DM patients attending Kigali University Teaching Hospital (CHUK) and Butare University Teaching Hospital between 2015 and 2020. Socio-demographic and clinical data, including anti-diabetic medications, hypoglycemia episodes, CV events, and comorbidities, were extracted from medical records and analyzed using Python. Binary regression was used to determine significant predictors of hypoglycemia.</p><p><strong>Results: </strong>Hypoglycemia occurred in 112 (41.9%) patients during their hospitalization or hospital admissions. The use of insulin was significantly associated with hypoglycemia (OR = 1.590, CI: 1.100-2.290, p = 0.010). The mean age of patients who experienced hypoglycemia is 54.2 (±12.1) years. Hypoglycemia occurrence was higher in males (59.8%) group compared to females (40.2%) (p = 0.007). Cardiovascular conditions were common (73.8%), with hypertension being the most prevalent (85.4%). Insulin was the most frequently used anti-diabetic therapy (42.3%). A significant association was found between hypoglycemia and subsequent CV complications. Management of hypoglycemia predominantly involved the use of 50% dextrose solution.</p><p><strong>Conclusion: </strong>Hypoglycemia is a frequent and clinically significant occurrence among T2DM patients in Rwanda, particularly associated with insulin therapy and CV comorbidities. Enhanced clinical monitoring and individualized treatment regimens are essential to mitigate hypoglycemia-related complications and reduce mortality. It is important to conduct a larger studies to support the evidence based findings and address the current methodological constraints.</p>","PeriodicalId":50090,"journal":{"name":"Journal of Pharmacy and Pharmaceutical Sciences","volume":"28 ","pages":"14880"},"PeriodicalIF":5.5,"publicationDate":"2025-11-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12695719/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145758262","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}

{"title":"Standard formulas and individualised parenteral nutrition preparations in very low birth weight infants.","authors":"Laurie Dez, Stéphane Haÿs, Gilles Leboucher, Romain Garreau, Jean-Charles Picaud, Thomas Briot","doi":"10.3389/jpps.2025.15310","DOIUrl":"10.3389/jpps.2025.15310","url":null,"abstract":"<p><strong>Background/objectives: </strong>Optimal nutrition in very low birth weight (VLBW) infants is associated with improved clinical outcomes. When parenteral nutrition (PN) with a marketing authorisation is not appropriate, hospital pharmacies can prepare more suitable PN preparation. This corresponds to standard preparations (i.e., available at any time with a fixed composition) or individualised ones (i.e., available after a period of prescription, preparation, and pharmaceutical control). In France, 12 standard formulas to be compounded were proposed by a national consortium in 2018. The objective of the present study was to evaluate whether individualised PN preparations ordered in our hospital are substitutable by one of the 12 standard formulas.</p><p><strong>Methods: </strong>All PN prescriptions for VLBW infants made in 2021 in our hospital were retrospectively extracted. For each prescription, the theoretical intakes that an infant would have received if a standard preparation had been administered were calculated. Standard and individualised preparations were compared using the Mann-Whitney U test for each component. Secondly, the relative difference between the expected intakes and effectively intakes was calculated for each component.</p><p><strong>Results/discussion: </strong>Over the study period, 1708 prescriptions were identified (corresponding to 1708 PN individualised preparations). Most infants were extremely low birth weight infants. Based on the methods of comparison, none of the 12 standard formulas fitted with targeted intakes achieved with individualised PN preparations ordered, whereas prescriptions did fit with international guidelines.</p><p><strong>Conclusion: </strong>The study highlights how it is difficult to establish nationally standard PN formulas for VLBW infants; the development of local standard formulas seems therefore relevant.</p>","PeriodicalId":50090,"journal":{"name":"Journal of Pharmacy and Pharmaceutical Sciences","volume":"28 ","pages":"15310"},"PeriodicalIF":5.5,"publicationDate":"2025-11-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12672384/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145679340","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}

{"title":"Development of a submicron emulsion-based delivery system to improve the anti-inflammatory activity of urolithin A.","authors":"Elisabetta Esposito, Valentyn Dzyhovskyi, Federico Santamaria, Lorenza Marvelli, Paola Boldrini, Paolo Mariani, Alessia Pepe, Maria Grazia Ortore, Mascia Benedusi, Giuseppe Valacchi, Luca Ferraro","doi":"10.3389/jpps.2025.15553","DOIUrl":"10.3389/jpps.2025.15553","url":null,"abstract":"<p><strong>Objective: </strong>Despite the antioxidant, anti-inflammatory, and anti-cellular-aging activities of urolithin A (UroA), a naturally occurring postbiotic, its high lipophilicity hampers its pharmaceutical application. To overcome this limitation improving its stability and bioavailability, submicron emulsions (S-EMs) were designed.</p><p><strong>Methods: </strong>Nineteen formulations (S-EM 1/S-EM 19) were prepared by two different methodologies. S-EMs were characterized evaluating macroscopical appearance and size distribution by photon correlation spectroscopy (PCS). One selected S-EM was loaded with UroA and characterized by PCS, transmission electron microscopy (TEM), small angle x-ray scattering (SAXS) and Fourier-transform infrared spectroscopy (FT-IR). Z potential, pH and syringeability were evaluated. UroA entrapment was studied efficiency by ultrafiltration and HPLC, while <i>in vitro</i> release by dialysis. Cytotoxicity was evaluated by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) (MTT) viability test on primary dermal human fibroblasts. The anti-inflammatory activity of S-EM-UroA was evaluated at 3, 6, and 24 h post-injection using the carrageenan-induced paw edema model in male C57BL/6 mice, and compared with UroA suspension and unloaded S-EM.</p><p><strong>Results: </strong>The preformulative study enabled to select method and composition for S-EM preparation. S-EM 18 was selected for UroA loading (SEM-UroA), due to mean diameter, zeta potential, pH and syringeability suitable for intraperitoneal administration. The loading of UroA (0.2 mg/mL) did not influence S-EM physicochemical features, while maintaining technological properties for 3 months. <i>In vitro</i> drug release showed a biphasic profile, 2.35-fold faster in the case of SEM-UroA compared to the drug suspension. <i>In vitro</i> studies revealed absence of cytotoxicity at concentrations up to 5 µM. <i>In vivo</i> studies, conducted as a first step in assessing the potential of S-EM-UroA, demonstrated a dose-dependent anti-inflammatory effect. Specifically, S-EM-UroA at 2 mg/kg reduced paw edema at 24 h (<i>p</i> < 00.5; One-Way ANOVA followed by Tukey's test), and at 4 mg/kg significantly reduced edema at all time points (<i>p</i> < 0.01), whereas the UroA suspension or S-EM had no effect on carrageenan-induced paw edema at any time point.</p><p><strong>Conclusion: </strong>These findings underscore the potential of UroA loaded S-EM as an effective delivery system, demonstrating its superiority over simple UroA suspensions in enhancing the systemic anti-inflammatory effects of the postbiotic.</p>","PeriodicalId":50090,"journal":{"name":"Journal of Pharmacy and Pharmaceutical Sciences","volume":"28 ","pages":"15553"},"PeriodicalIF":4.3,"publicationDate":"2025-11-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12634460/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145589873","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}

{"title":"Zaleplon nanospanlastics loaded transdermal patches: formulation, optimization, ex-vivo permeation, and in-vivo studies.","authors":"Ahmed A El-Shenawy, Reham A Abd Elkarim, Reda A Mahmoud, Abd El Hakim Ramadan, Ali H Alamri, Hamdy Abdelkader, Mohamed S Elafify, Essam A Mahmoud, Mohammed S Saddik, Mohamed S Mohamed","doi":"10.3389/jpps.2025.15406","DOIUrl":"10.3389/jpps.2025.15406","url":null,"abstract":"<p><p>Zaleplon (ZLP) is a commonly used sedative-hypnotic drug that has low oral bioavailability because of its poor water solubility and extensive hepatic metabolism. This study aimed to encapsulate ZLP into spanlastic nanovesicles to enhance its bioavailability via transdermal delivery. Using Span 60 and Tween 80, ZLP-loaded spanlastics were fabricated using thin film hydration technique according to 3² full factorial design. In the applied design, the influence of formulation variables on vesicle size, entrapment efficiency, and cumulative drug amount released over 24 h was investigated, leading to the identification of the optimal formulation. The optimized spanlastics were nanosized, spherical vesicles measuring 297.2 ± 8.17 nm, with an encapsulation efficiency of 65.75 ± 3.28% and a 24-hour drug release rate of 76.44 ± 5.66%. FT-IR studies revealed no significant chemical interactions between ZLP and the excipients used. HPMC K100M transdermal patches loaded with the optimized ZLP-spanlastics were formulated utilizing solvent casting technique. The patches were smooth and elastic with uniform drug content, ranging from 92.65 ± 2.54 to 96.12 ± 1.57%. The steady-state flux (Jss) of the spanlastic transdermal patch (ZLP-SP1) across rabbit skin was over 3.62 times higher than that of the control transdermal patch, indicating a significant enhancement in drug permeation. The investigated transdermal patches were stable under accelerated conditions with non-irritating properties. The <i>in-vivo</i> studies have shown that the pharmacokinetic parameters of ZLP oral suspension and ZLP-SP1 are significantly different, with the relative bioavailability of ZLP-SP1 being 2.681%. Therefore, these fabricated transdermal patches could be effectively used to treat insomnia.</p>","PeriodicalId":50090,"journal":{"name":"Journal of Pharmacy and Pharmaceutical Sciences","volume":"28 ","pages":"15406"},"PeriodicalIF":5.5,"publicationDate":"2025-11-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12626903/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145566063","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}