Pharmaceutical Development and Technology最新文献

HPMCAS-solidified supersaturated baicalin self-nanoemulsifying drug delivery systems: development and anti-colitis evaluation. hpmcas固化过饱和黄芩苷自纳米乳化给药系统：开发和抗结肠炎评价。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-06-13 DOI: 10.1080/10837450.2025.2518567

Jie Wang, Xuemei Gu, Zhiyang Lv, Jing Chen, Zihan Gao, Xinyun Hu, Wei Xiao

{"title":"HPMCAS-solidified supersaturated baicalin self-nanoemulsifying drug delivery systems: development and anti-colitis evaluation.","authors":"Jie Wang, Xuemei Gu, Zhiyang Lv, Jing Chen, Zihan Gao, Xinyun Hu, Wei Xiao","doi":"10.1080/10837450.2025.2518567","DOIUrl":"10.1080/10837450.2025.2518567","url":null,"abstract":"This study developed a hydroxypropyl methylcellulose acetate succinate (HPMCAS)-functionalized supersaturated self-nanoemulsifying drug delivery system (HPMCAS-SNEDDS@BA) to address the poor solubility and bioavailability of baicalin (BA), a flavonoid with anti-colitis efficacy. The formulation was systematically optimized through solubility screening, emulsification efficiency evaluation, and pseudo-ternary phase diagram analysis. Central composite design-response surface methodology (CCD-RSM) was employed to identify the optimal SNEDDS@BA composition, followed by HPMCAS ratio optimization based on supersaturation maintenance in biorelevant media. Comprehensive characterization included emulsification performance, droplet morphology, solid-state properties, in vitro release, and stability. The optimized formulation (mass ratio: HPMCAS-castor oil-RH40-PEG400-BA = 151.5:20:40:40:1) generated homogeneous, transparent nanoemulsions with spherical droplets, achieving an emulsification time of 48.30 ± 0.74 s, a mean particle size of 47.77 ± 2.32 nm, and a polydispersity index (PDI) of 0.259 ± 0.007. HPMCAS-SNEDDS@BA effectively prevented premature gastric emulsification while enhancing intestinal dissolution rates and sustaining BA supersaturation. Pharmacokinetic studies demonstrated a 5.84-fold improvement in BA bioavailability compared to unmodified formulations. In a dextran sulfate sodium (DSS)-induced colitis model, HPMCAS-SNEDDS@BA outperformed BA suspension and SNEDDS@BA, normalizing colon length, reducing inflammatory cytokines, and restoring mucosal architecture. These findings validate the dual functionality of HPMCAS as a pH-responsive polymer and crystallization inhibitor, enabling targeted intestinal delivery and optimized therapeutic outcomes for ulcerative colitis.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-16"},"PeriodicalIF":2.6,"publicationDate":"2025-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144267016","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

Formulation and characterization of novel oral pH-sensitive electrospun nanofibers for boosting dissolution and penetration of model class IV drug. 促进IV类药物溶出渗透的新型口服ph敏感静电纺丝纳米纤维的配方与表征。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-06-13 DOI: 10.1080/10837450.2025.2517709

Omar Y Mady, Safaa Khaled, Asmaa A Hedaya, Noorelhoda Abdine, Yusuf Haggag

{"title":"Formulation and characterization of novel oral pH-sensitive electrospun nanofibers for boosting dissolution and penetration of model class IV drug.","authors":"Omar Y Mady, Safaa Khaled, Asmaa A Hedaya, Noorelhoda Abdine, Yusuf Haggag","doi":"10.1080/10837450.2025.2517709","DOIUrl":"10.1080/10837450.2025.2517709","url":null,"abstract":"Sulpiride (a model class IV drug) is a central dopamine antagonist, that is commonly used in the treatment of various psychiatric and gastrointestinal conditions. However, its poor aqueous solubility and low oral bioavailability (20-30%) limit its therapeutic efficacy. Electrospun nanofibers offer a promising method to enhance the oral absorption of poorly water-soluble drugs. This study, for the first time, aimed to investigate the feasibility of electrospun Eudragit S100-loaded Sulpiride nanofibers as an enhanced oral delivery system, compared to drug-loaded solid dispersion. The physicochemical properties of the nanofibers were characterized. The drug's intestinal permeability was evaluated using an ex vivo non-everted sac technique. Sulpiride-loaded nanofibers exhibited uniform morphology with a very narrow nanosize range of (98.4-123.6 nm) and a high drug-loading efficiency of >98%. In vitro, dissolution demonstrated a significant enhancement in the Sulpiride's dissolution rates from the nanofiber formulations (>94% of the drug released within 4 h) compared to the solid dispersion formulation (˂77% of the drug released). The nanofiber formulations exhibited a 2-fold increase in the drug's intestinal permeability and a 4-fold increase in apparent permeability (Papp) compared to the free drug. The improved dissolution and intestinal permeability of Sulpiride-loaded nanofibers suggest their potential application for enhancing the oral delivery and therapeutic efficacy of class IV drugs.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-16"},"PeriodicalIF":2.6,"publicationDate":"2025-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144258693","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

Investigating the In Vivo Distribution Characteristics of Gel-in-Water Nanogel Emulsions and Demonstrating Their Efficacy in Treating C26 Tumor-Bearing Mice. 研究水凝胶纳米乳的体内分布特征及对C26荷瘤小鼠的治疗作用。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-06-13 DOI: 10.1080/10837450.2025.2518564

Yi Zhang, Jannatul Fardous, Ryota Doi, Yuuta Inoue, Yasuhiro Ikegami, Hiroyuki Ijima

{"title":"Investigating the In Vivo Distribution Characteristics of Gel-in-Water Nanogel Emulsions and Demonstrating Their Efficacy in Treating C26 Tumor-Bearing Mice.","authors":"Yi Zhang, Jannatul Fardous, Ryota Doi, Yuuta Inoue, Yasuhiro Ikegami, Hiroyuki Ijima","doi":"10.1080/10837450.2025.2518564","DOIUrl":"https://doi.org/10.1080/10837450.2025.2518564","url":null,"abstract":"Nanotechnology has been advancing drug delivery systems (DDSs) for decades. Nanoparticle DDSs, in which nanometric carriers deliver drugs to the target site, are highly valued for cancer treatment. In this study, based on nanoemulsion technology, gel-in-water (G/W) nanoemulsion was developed by using an organogel, i.e., 12-hydroxystearic acid and castor oil, followed by encapsulation of the model anticancer drug paclitaxel (PTX) within the nanogel droplets. The G/W was prepared using ultrasound and stabilized with a nonionic surfactant. The enhanced permeability and retention of G/W were investigated by encapsulating coumarin-6 and comparing it with an oil-in-water (O/W) nanoemulsion. Temporal changes in tissue distribution of both nanoemulsions were used to assess the effect of gelation on drug distribution. Regardless of the tissue type, the extraction efficiency of G/W was lower compared to O/W. The fluorescence intensity of coumarin-6 in G/W was higher compared to O/W. The size of G/W nanoparticles affects lung distribution and blood retention. PTX-loaded G/W (PTX-G/W) nanoparticles effectively treated colon cancer in vivo. They also exhibited antitumor activity against colon26 (C26) cells in vitro. The impact of particle size on the in vivo tissue distribution of G/W nanoemulsions suggests an improvement in drug delivery to the tumor site via nanoparticles.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-17"},"PeriodicalIF":2.6,"publicationDate":"2025-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144286042","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

Gum tragacanth-based hemostatic sponge for enhanced hemostasis in dental surgery. 牙龈黄芪止血海绵在牙科手术中的止血作用。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-06-12 DOI: 10.1080/10837450.2025.2516238

Mirmousa Mousavai, Ramin Khajavi, Mohammadreza Kalaee, Mohammad Karim Rahimi

{"title":"Gum tragacanth-based hemostatic sponge for enhanced hemostasis in dental surgery.","authors":"Mirmousa Mousavai, Ramin Khajavi, Mohammadreza Kalaee, Mohammad Karim Rahimi","doi":"10.1080/10837450.2025.2516238","DOIUrl":"10.1080/10837450.2025.2516238","url":null,"abstract":"Regulating hemorrhage is crucial during dental procedures, particularly surgical interventions where substantial blood loss may occur. Hemostatic sponges are effective instruments for controlling hemorrhage, facilitating hemostasis, preparing the surgical area, and enhancing the healing of injuries. This work aimed to present a novel hemostatic sponge created by integrating antihemorrhagic chemicals with the natural polysaccharide tragacanth. Gum tragacanth (GT) (derived from the species Astragalus gossypinus) was solubilized in water and combined with nanoclay (NC) and tranexamic acid (TXA) at varying doses. Subsequently, they were freeze-dried in cubic silicone molds. Scanning electron micrographs revealed that the incorporation of TXA and NC significantly increased the porosity of the sponges. No evidence of chemical bonding was present in our converted infrared spectra. Prothrombin time (PT), activated partial thromboplastin time (aPTT), and whole blood coagulation index showed improvement with the administration of hemostatics, with TXA demonstrating a more pronounced impact. The cytotoxicity assay of the hemostatic GT exhibited no notable difference from the control sample. The hemostatic GT has demonstrated significant potential for medical applications, particularly in dentistry, and applies to procedures such as endodontics and prosthesis placement.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-25"},"PeriodicalIF":2.6,"publicationDate":"2025-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144234784","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

Impact of medication swallowing lubricants on the in vitro dissolution of crushed and whole metformin tablets: dissolution kinetics study. 药物吞食润滑剂对二甲双胍碎片和整片体外溶出度的影响：溶出动力学研究。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-06-12 DOI: 10.1080/10837450.2025.2516234

Vivek Babu Nooney, Thilini Thrimawithana, Barbora de Courten, Albert Le, Filip Nikolovski, Noemi Cieleszky, Seerat Fatima, Ayman Allahham

{"title":"Impact of medication swallowing lubricants on the in vitro dissolution of crushed and whole metformin tablets: dissolution kinetics study.","authors":"Vivek Babu Nooney, Thilini Thrimawithana, Barbora de Courten, Albert Le, Filip Nikolovski, Noemi Cieleszky, Seerat Fatima, Ayman Allahham","doi":"10.1080/10837450.2025.2516234","DOIUrl":"10.1080/10837450.2025.2516234","url":null,"abstract":"Metformin is the most common drug used in patients with type 2 diabetes. Our aim is to assess if the in vitro dissolution of Metformin IR 500 mg tablets and its kinetics is altered in the presence of various medication swallowing lubricants used in vivo and to evaluate their rheological properties of tablet lubricant. The dissolution profile of metformin tablets (crushed and whole) mixed with selected medication swallowing lubricants was studied in a Distek® Dissolution apparatus at 6 different time points (n = 5). Samples were diluted and analysed using a UV-visible Spectrometer at a wavelength of 232 nm using a calibrated absorbance-concentration curve. Dissolution data will be modelled to understand the effect on its dissolution kinetics. Rheology studies were completed using an AR G2 System Rheometer. Gloup® Forte delayed the in vitro dissolution of metformin from crushed or whole tablets and produced lower peak concentrations, irrespective of the pH of the dissolution media (reduction up to 35% reduction in concentration in pH = 6.8). Gloup® Forte has changed the release to almost erosion-controlled in different media when mixed with crushed metformin tablets. Further studies evaluating the effects of commonly used thickened fluids on medication may be required to better inform clinical practice.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-14"},"PeriodicalIF":2.6,"publicationDate":"2025-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144234785","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

Development of molnupiravir and peramivir loaded liposome formulations for combined antiviral therapy. 用于联合抗病毒治疗的莫诺匹拉韦和帕拉米韦负载脂质体制剂的研制。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-06-09 DOI: 10.1080/10837450.2025.2516239

Hadiye Keskin, Tuba Reçber, Nazlıcan Filazi, Dilek Gelen-Gungor, Sukru Ozturk, Hakan Eroğlu, Emirhan Nemutlu, Aykut Özkul, Kezban Ulubayram, İpek Eroğlu

{"title":"Development of molnupiravir and peramivir loaded liposome formulations for combined antiviral therapy.","authors":"Hadiye Keskin, Tuba Reçber, Nazlıcan Filazi, Dilek Gelen-Gungor, Sukru Ozturk, Hakan Eroğlu, Emirhan Nemutlu, Aykut Özkul, Kezban Ulubayram, İpek Eroğlu","doi":"10.1080/10837450.2025.2516239","DOIUrl":"10.1080/10837450.2025.2516239","url":null,"abstract":"The pandemic caused by the SARS-CoV-2 virus has led scientists to intensify research on antiviral drugs and vaccines. As a result of these studies, it was observed that molnupiravir (MLP) and peramivir (PRV) could be used against pandemic. MLP affects SARS-CoV-2 replication, but it necessitates high doses, which can cause adverse effects in patients. PRV is a neuraminidase inhibitor, but the bioavailability of the drug after oral administration is very low. In this study, MLP-, PRV-loaded and combined liposome (COMB-Lipo) formulations were prepared via the thin film hydration method. Phospholipon 90 G-based formulations exhibited the most favorable characteristics, with a particle size of 111-145 nm, a polydispersity index (PDI) of less than 0.4, and a zeta potential (ZP) of 6-12 mV). Cell culture studies demonstrated that developed stable formulations are nontoxic to L929 and Vero E6 cells. Antiviral activity assessments against SARS-CoV-2 suggested the effectiveness of liposomes in inhibiting viral activity. These findings demonstrate that a possible synergistic effect of the newly developed sustained-release COMB-Lipo formulation is suggested with the complementary antiviral mechanisms of the combined agents. As a result, the therapeutic potential of co-delivery of anti-SARS-CoV-2 drugs for pulmonary application is considered a promising approach for long-acting treatment of COVID-19.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-21"},"PeriodicalIF":2.6,"publicationDate":"2025-06-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144226274","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

Cationic Nanocrystalline Suspensions: A Potential Approach for Nose to Brain Delivery of L-Dopa in Parkinson's Therapy. 阳离子纳米晶体悬浮液：在帕金森治疗中左旋多巴鼻到脑输送的一种潜在途径。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-06-05 DOI: 10.1080/10837450.2025.2516237

Chiedza Kakono, Bwalya A Witika, Pedzisai A Makoni, Roderick B Walker

{"title":"Cationic Nanocrystalline Suspensions: A Potential Approach for Nose to Brain Delivery of L-Dopa in Parkinson's Therapy.","authors":"Chiedza Kakono, Bwalya A Witika, Pedzisai A Makoni, Roderick B Walker","doi":"10.1080/10837450.2025.2516237","DOIUrl":"https://doi.org/10.1080/10837450.2025.2516237","url":null,"abstract":"Levodopa (L-dopa) is the most effective treatment for Parkinson's disease, but it exhibits low oral bioavailability. Intranasal L-dopa nanosuspensions were manufactured to improve bioavailability using the olfactory and trigeminal delivery routes for direct brain delivery and bypassing the blood-brain barrier. This study focuses on the formulation development and comprehensive in vitro characterization of L-dopa nanocrystals designed as a potential formulation for intranasal delivery. The nanosuspensions were optimized using Design of Experiments. The L-dopa nanosuspension was produced at 50 °C using sonoprecipitation and mechanical stirring, with water as the solvent and ethanol as the antisolvent phases, with Tween® 80 and cetyltrimethylammonium bromide used as stabilizing agents. The critical quality attributes monitored were particle/droplet size (PS), polydispersity index (PDI), Zeta potential (ZP), and percent yield (%). The pH and osmolarity of the optimized formulation were monitored, and scanning electron microscopy, powder X-ray diffraction, differential scanning calorimetry, Fourier-transform infrared spectroscopy, and in vitro release studies were used to characterize the optimized L-dopa nanosuspension further. Short-term stability testing of optimized L-dopa nanosuspensions was performed at 4 °C and 22 °C for 28 days. The mean PS, PDI, ZP, and % yield of the optimized nanosuspension were 161.4 ± 20.152 nm, 0.383 ± 0.090, +15.45 ± 1.664 mV, and 72.106 ± 0.023%, respectively. In conclusion, the optimized formulation exhibited the target CQA and may potentially enhance the bioavailability of L-dopa. These in vitro findings support the potential for intranasal L-dopa delivery, however, in vivo studies are necessary to confirm nose-to-brain transport and therapeutic effects.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-22"},"PeriodicalIF":2.6,"publicationDate":"2025-06-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144226273","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

Lycopene-carrier solid dispersion loaded lipid liquid crystal nanoparticle: in vitro evaluation and in vivo wound healing effects. 番茄红素载体固体分散脂质液晶纳米颗粒：体外评价和体内伤口愈合效果。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-05-27 DOI: 10.1080/10837450.2025.2504998

Farhad Shahverdi, Elham Khodaverdi, Jebrail Movaffagh, Soheil Tafazzoli Mehrjardi, Hossein Kamali, Ali Nokhodchi

{"title":"Lycopene-carrier solid dispersion loaded lipid liquid crystal nanoparticle: in vitro evaluation and in vivo wound healing effects.","authors":"Farhad Shahverdi, Elham Khodaverdi, Jebrail Movaffagh, Soheil Tafazzoli Mehrjardi, Hossein Kamali, Ali Nokhodchi","doi":"10.1080/10837450.2025.2504998","DOIUrl":"10.1080/10837450.2025.2504998","url":null,"abstract":"This study was conducted to develop a lycopene-carrier solid dispersion-loaded lipid liquid crystal nanoparticle (LLC) formulation aimed at enhancing aqueous solubility, bioavailability, and wound healing efficacy. Lycopene was extracted from tomato paste using the Soxhlet method and was formulated into solid dispersions with polyvinylpyrrolidone (PVP) and Poloxamer (Plx) to enhance the solubility of lycopene. The physicochemical properties of the solid dispersion products were characterized. Cytotoxicity on human fibroblast cells, cell migration, and wound healing treatment in the mice were also assessed. PVP demonstrated greater efficacy in enhancing the aqueous solubility of lycopene than Plx. The results indicated that the morphology of the LLC was cubosome, achieving a high encapsulation efficiency of 71.57 ± 2.1%. The LLC formulations demonstrated significantly enhanced release rates of 68.18 ± 1.78% and improved skin permeation compared to the lycopene solid dispersion solution. The results of the cell culture demonstrated the safety of the formulation, and the in vitro scratch test showed the migration of fibroblast cells in the presence of the lycopene-PVP solid dispersion loaded LLC compared to lycopene alone. Based on the obtained results, it can be concluded that the proposed formulation (lycopene-PVP solid dispersion loaded LLC) could be a suitable option for wound healing.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-18"},"PeriodicalIF":2.6,"publicationDate":"2025-05-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144023279","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

Solid supersaturated self-nanoemulsifying drug delivery system for abiraterone acetate: improved drug loading, dissolution, cellular uptake, and anticancer activity. 醋酸阿比特龙固体过饱和自纳米乳化给药系统：改善药物负载、溶出、细胞摄取和抗癌活性。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-05-23 DOI: 10.1080/10837450.2025.2505003

Ayush Nair, Mayur Aalhate, Srushti Mahajan, Ujala Gupta, Indrani Maji, Pankaj Kumar Singh

{"title":"Solid supersaturated self-nanoemulsifying drug delivery system for abiraterone acetate: improved drug loading, dissolution, cellular uptake, and anticancer activity.","authors":"Ayush Nair, Mayur Aalhate, Srushti Mahajan, Ujala Gupta, Indrani Maji, Pankaj Kumar Singh","doi":"10.1080/10837450.2025.2505003","DOIUrl":"10.1080/10837450.2025.2505003","url":null,"abstract":"Abiraterone acetate (ABT) is an androgen biosynthesis inhibitor approved for the treatment of prostate cancer. However, the treatment course of ABT is constrained by its high dose, poor solubility and permeability issues. A solid supersaturated self-nanoemulsifying drug delivery system (ssSNEDDS) is an excellent approach for improving drug loading. The aim was to increase the solubility and drug loading of ABT in SNEDDS via supersaturation by using a polymeric precipitation inhibitor (HPMC E5). Liquid SNEDDS were thoroughly optimized with a mixture design followed by solidification with Aerosil® 200 by the adsorption method. The developed ABT-ssSNEDDS showed a nano-ranged particle size of 106.23 ± 4.15 nm and PDI of 0.234 ± 0.0069. Furthermore, the powder showed an angle of repose of 34.86 ± 0.30° indicating good flow properties with smooth morphology under SEM analysis. DSC and PXRD studies revealed amorphization of ABT in the ABT-ssSNEDDS group. Furthermore, the dissolution study demonstrated significantly higher ABT release from ABT-ssSNEDDS in comparison to free ABT after 2 h in pH 1.2 and 6.8 pH buffer. In-vitro cell culture studies in the PC-3 cell line denoted significantly enhanced anticancer activity and cellular uptake. Thus, ABT-ssSNEDDS could be an encouraging approach for improved oral therapy and enhanced drug loading of ABT.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-17"},"PeriodicalIF":2.6,"publicationDate":"2025-05-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144015402","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

An insight into cell-penetrating peptides: perspectives on design, optimization, and targeting in drug delivery systems. 洞察细胞穿透肽：在药物输送系统的设计，优化和靶向的观点。

IF 2.6 4区医学

Pharmaceutical Development and Technology Pub Date : 2025-05-23 DOI: 10.1080/10837450.2025.2505000

Ali Asghar Khakshur, Elham Khodaverdi, Hossein Kamali, Ali Nokhodchi

{"title":"An insight into cell-penetrating peptides: perspectives on design, optimization, and targeting in drug delivery systems.","authors":"Ali Asghar Khakshur, Elham Khodaverdi, Hossein Kamali, Ali Nokhodchi","doi":"10.1080/10837450.2025.2505000","DOIUrl":"10.1080/10837450.2025.2505000","url":null,"abstract":"The authors carried out a comprehensive review of the application of peptides known as cell-penetrating peptides (CPPs) in various drug delivery systems (DDS), with the prospect of achieving novel solutions and ideas to overcome the challenges of DDS, by making them more able to penetrate cells and biological membranes. A conceptual search was conducted in relevant literature databases (Scopus, PubMed, Web of Science, and Google Scholar) up to 1 April 2025 using keywords such as drug delivery systems, cell-penetrating peptides, CPPs, complexes, conjugates, nanoparticles, dendrimers, exosomes, liquid crystalline, liposomes, micelles, nanospheres and lipid nanoparticles. The studies demonstrate that the antimicrobial effect of drugs, including curcumin, gentamicin, and antifungal drugs like imidazoacridinone derivatives, can be enhanced when they are conjugated or complexed with CPPs. CPPs possess positive charges, which make them suitable for gene therapy applications by facilitating the delivery of plasmids and siRNAs with negative charges in modern delivery systems. Medicinal formulations containing CPPs in combination with liquid crystals or nanostructured lipid carriers (NLCs) increase drugs penetration to the skin. Additionally, several investigations showed that CPPs could have a positive impact on the pharmacokinetic and pharmacodynamic of chemotherapy agents, reducing their side effects. CPPs have significant potential in enhancing penetration, bioavailability, targeting, and optimization of DDS. By using computer modeling and designing CPPs with more desirable features and conducting more clinical studies, new methods for treating diseases and better formulations can be achieved.","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-27"},"PeriodicalIF":2.6,"publicationDate":"2025-05-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"144015380","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