International Journal of Pharmaceutics: X最新文献

{"title":"QbD-guided phospholipid-tagged nanonized boswellic acid naturosomal delivery for effective rheumatoid arthritis treatment","authors":"Poonam Usapkar ,&nbsp;Suprit Saoji ,&nbsp;Pradnya Jagtap ,&nbsp;Muniappan Ayyanar ,&nbsp;Mohan Kalaskar ,&nbsp;Nilambari Gurav ,&nbsp;Sameer Nadaf ,&nbsp;Satyendra Prasad ,&nbsp;Damiki Laloo ,&nbsp;Mohd Shahnawaz Khan ,&nbsp;Rupesh Chikhale ,&nbsp;Shailendra Gurav","doi":"10.1016/j.ijpx.2024.100257","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100257","url":null,"abstract":"<div><p>Studies have reported the potential role of Boswellic acids (BAs), bioactive pentacyclic triterpenes from <em>Boswellia serrata</em> (BS), in treating rheumatoid arthritis (RA). However, poor water solubility and limited oral absorption are restricting factors for its better therapeutic efficacy. Based on these assumptions, the current study aimed to develop naturosomal delivery of BAs to boost their extremely low bioavailability, colloidal stability, and water solubility. Nanonized naturosomes were developed and subsequently analyzed to show their physicochemical and functional features employing the quality-by-design approach. The solubility analysis of Boswellic acid naturosomes revealed a 16 times improvement in aqueous solubility compared to BS extract (BSE). The zeta potential and dynamic light scattering findings of BSE naturosomes (BSENs) have demonstrated their colloidal stability with regulated nano-size particles. Additionally, compared to BSE (⁓31%), <em>in-vitro</em> dissolution experiments showed that &gt;99% of pentacyclic triterpenes were released from BSENs. Studies on <em>ex-vivo</em> permeation showed that BSENs' permeation (&gt;79%) significantly improved over BSE's (⁓20%). <em>In-vivo</em> efficacy studies using CFA-prompted arthritis in rodents showed a critical expansion in body wt and an undeniable reduction in paw thickness, paw volume, and TNF-α treated with BSEN compared to the arthritis control and BSE-treated group. These findings suggest that BSENs can help treat RA drugs by demonstrating their efficacy in further clinical research to validate the significant improvements.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100257"},"PeriodicalIF":4.7,"publicationDate":"2024-05-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S259015672400029X/pdfft?md5=c608a4a20a497fda980471a23e56bd44&pid=1-s2.0-S259015672400029X-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141078184","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"RP-HPLC-CAD method for the rapid analysis of lipids used in lipid nanoparticles derived from dual centrifugation","authors":"Valentin Bender,&nbsp;Leon Fuchs,&nbsp;Regine Süss","doi":"10.1016/j.ijpx.2024.100255","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100255","url":null,"abstract":"<div><p>The use of lipids as suitable excipients for drug carrier systems has been established for years. Liposomes or lipid nanoparticles (LNPs) in general have been shown capable of delivering both hydrophilic and hydrophobic drugs. The Covid-19 pandemic and the resulting vaccines have significantly increased interest in the potential for these lipid-based systems, which can carry different types of therapeutic RNAs. LNPs used for the transfection of RNA are usually a multi-component mixture of phospholipids and other lipids. Essential components are positively charged or ionizable lipids such as DOTAP or SM-102, but also uncharged helper lipids such as cholesterol, DOPE, DSPC, DMG-PEG₂₀₀₀ or DSPE-PEG₂₀₀₀. Due to the differences in charge, simultaneous detection is a challenge. Here, we present a reversed-phase high-performance liquid chromatography charged-aerosol-detector method (RP-HPLC-CAD method) using a C-18 column for the simultaneous determination of charged and uncharged lipids. Our method has been validated according to the ICH-Q2 (R2) guideline for accuracy, precision, specificity and working range, including the limit of detection (LOD) and quantification (LOQ), as well as the calibration range. We were able to show satisfactory results in both precision and accuracy. The working range also shows great potential with a calibration range from 9.375 to 1000 μg/ml, LODs &lt;1.85 μg/ml and LOQs &lt;6.16 μg/ml. This method represents a fast and reproducible procedure for quantifying the lipids mentioned. In combination with the novel approach for the production of LNPs using dual centrifugation (DC), it offers the possibility of extremely rapid production of RNA-loaded LNPs, and the immediate analysis for their lipid components.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100255"},"PeriodicalIF":4.7,"publicationDate":"2024-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000276/pdfft?md5=f7f09777fb062085e5bd0e1adbdcb8d5&pid=1-s2.0-S2590156724000276-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140894524","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Evaluation of gender differences in the pharmacokinetics of oral zileuton nanocrystalline formulation using a rat model","authors":"Chandra Mohan Reddy Muthumula ,&nbsp;Sangeeta Khare ,&nbsp;Rajan Jog ,&nbsp;Bhagya Wickramaratne ,&nbsp;Angela Lee ,&nbsp;Sushanta Chakder ,&nbsp;Diane J. Burgess ,&nbsp;Kuppan Gokulan","doi":"10.1016/j.ijpx.2024.100254","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100254","url":null,"abstract":"<div><p>Zileuton is a leukotriene inhibitor used to treat asthma. As a BCS class II drug it exhibits challenges with solubility which likely impact its absorption. As patient gender significantly impacts the pharmacokinetics of many drugs, this study aimed to investigate potential gender-based pharmacokinetic differences after oral zileuton administration in rats. Male and female Sprague Dawley rats received single oral gavage doses of pure zileuton as an active pharmaceutical ingredient (30 mg/kg body weight (bw)), physical mixture (PM; at 30 mg/kg bw of the formulation contains zileuton, kollidon VA64 fine, dowfax2A1 and trehalose), and nanocrystalline formulation of zileuton (NfZ; at 30 mg/kg bw of the formulation). Plasma, tissue, and urine concentrations were quantified using high performance liquid chromatography (HPLC). Noncompartmental pharmacokinetic analysis showed higher zileuton levels in the plasma of female versus male rats across all evaluated forms of zileuton (API, PM, and NfZ). Female rats demonstrated higher peak plasma concentrations (C_max) and increased area under the plasma concentration-time curve (AUC) relative to males, regardless of formulation. These findings reveal substantial gender disparities in the pharmacokinetics of zileuton in the rat model. This study emphasizes the critical need to evaluate gender differences during preclinical drug development to enable gender-based precision dosing strategies for equivalent efficacy/safety outcomes in male and female patients. Additional studies are warranted to investigate underlying mechanisms of such pharmacokinetic gender divergences.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100254"},"PeriodicalIF":4.7,"publicationDate":"2024-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000264/pdfft?md5=e86c6e00a910abd55197a0d13539b17f&pid=1-s2.0-S2590156724000264-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140901358","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Stimuli-sensitive biomimetic nanoparticles for the inhibition of breast cancer recurrence and pulmonary metastasis","authors":"Dongjie Yang ,&nbsp;Lan Zhang ,&nbsp;Jiang Ni ,&nbsp;Yang Ding ,&nbsp;Anam Razzaq ,&nbsp;Zaheer Ullah Khan ,&nbsp;Haroon Iqbal ,&nbsp;Yasmene Falah Alanazi ,&nbsp;Naveed Ullah Khan ,&nbsp;Rong Wang","doi":"10.1016/j.ijpx.2024.100252","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100252","url":null,"abstract":"<div><p>Biomimetic nanoparticles represent a promising avenue for mitigating rapid clearance by the reticuloendothelial system (RES); however, current challenges include insufficient tumour targeting, suboptimal adhesion, and inadequate localized drug release within tumour regions. These shortcomings contribute to persistent contests, such as recurrence and pulmonary metastasis, even with advanced breast cancer therapies. Stimuli-sensitive drug release can furbish the membrane coated nanoparticles for their efficiency against the stated problems. To enhance the efficacy of biomimetic nanoparticles in addressing these issues, we proposed a versatile, stimuli-responsive drug delivery system by encapsulating doxorubicin (Dox) and perfluorohexane (PFH) within poly (lactic-<em>co</em>-glycolic acid) (PLGA) nanoparticles, subsequently coated with macrophage-derived cell membranes. Within this framework, PFH serves as the mediator for ultrasonic (US)-irradiation-triggered drug release specifically within tumour microenvironment, while the macrophage-derived cell membrane coating enhances cell adhesion, enables immune evasion, and natural tumour-homing ability. The characterization assays and <em>in vitro</em> evaluations yielded encouraging results, indicating enhanced targeting and release efficiencies. <em>In vivo</em> studies demonstrated marked inhibitory effects on both breast cancer recurrence and pulmonary metastasis. The resulting data indicate that these engineered nanoparticles have notable potential for targeted delivery and controlled release upon US irradiation, thereby offering significant therapeutic efficacy against primary breast cancer, pulmonary metastasis, and recurrent malignancies. Our findings lay the groundwork for a novel clinical approach, representing an intriguing direction for ongoing investigation by oncologists.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100252"},"PeriodicalIF":4.7,"publicationDate":"2024-05-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000240/pdfft?md5=b0467013f8ea70f40e3bfe7488374cfb&pid=1-s2.0-S2590156724000240-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140893395","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Polycaprolactone – Vitamin E TPGS micelles for delivery of paclitaxel: In vitro and in vivo evaluation","authors":"Ziyad Binkhathlan ,&nbsp;Osman Yusuf ,&nbsp;Raisuddin Ali ,&nbsp;Abdullah H. Alomrani ,&nbsp;Aws Alshamsan ,&nbsp;Abdullah K. Alshememry ,&nbsp;Aliyah Almomen ,&nbsp;Musaed Alkholief ,&nbsp;Ibrahim A. Aljuffali ,&nbsp;Faleh Alqahtani ,&nbsp;Saad Alobid ,&nbsp;Essam A. Ali ,&nbsp;Afsaneh Lavasanifar","doi":"10.1016/j.ijpx.2024.100253","DOIUrl":"10.1016/j.ijpx.2024.100253","url":null,"abstract":"<div><p>This study aimed to present findings on a paclitaxel (PTX)-loaded polymeric micellar formulation based on polycaprolactone-vitamin E TPGS (PCL-TPGS) and evaluate its in vitro anticancer activity as well as its in vivo pharmacokinetic profile in healthy mice in comparison to a marketed formulation. Micelles were prepared by a co-solvent evaporation method. The micelle's average diameter and polydispersity were determined using dynamic light scattering (DLS) technique. Drug encapsulation efficiency was assessed using an HPLC assay. The in vitro cytotoxicity was performed on human breast cancer cells (MCF-7 and MDA-MB-231) using MTT assay. The in vivo pharmacokinetic profile was characterized following a single intravenous dose of 4 mg/kg to healthy mice. The mean diameters of the prepared micelles were ≤ 100 nm. Moreover, these micelles increased the aqueous solubility of PTX from ∼0.3 μg/mL to reach nearly 1 mg/mL. While the PTX-loaded micelles showed an in vitro cytotoxicity comparable to the marketed formulation (Ebetaxel), drug-free PCL-TPGS micelles did not show any cytotoxic effects on both types of breast cancer cells (∼100% viability). Pharmacokinetics of PTX as part of PCL-TPGS showed a significant increase in its volume of distribution compared to PTX conventional formulation, Ebetaxel, which is in line with what was reported for clinical nano formulations of PTX, i.e., Abraxane, Genexol-PM, or Apealea. The findings of our studies indicate a significant potential for PCL-TPGS micelles to act as an effective system for solubilization and delivery of PTX.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100253"},"PeriodicalIF":4.7,"publicationDate":"2024-05-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000252/pdfft?md5=2585d71757535ea96c12dfa95b6eeb05&pid=1-s2.0-S2590156724000252-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141037993","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Fine excipient materials in carrier-based dry powder inhalation formulations: The interplay of particle size and concentration effects","authors":"Mustafa M.A. Elsayed ,&nbsp;Iman M. Alfagih ,&nbsp;Katrina Brockbank ,&nbsp;Fawaz Alheibshy ,&nbsp;Alhassan H. Aodah ,&nbsp;Raisuddin Ali ,&nbsp;Khaled Almansour ,&nbsp;Ahmed O. Shalash","doi":"10.1016/j.ijpx.2024.100251","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100251","url":null,"abstract":"<div><p>The contributions of fine excipient materials to drug dispersibility from carrier-based dry powder inhalation (DPI) formulations are well recognized, although they are not completely understood. To improve the understanding of these contributions, we investigated the influences of the particle size of the fine excipient materials on characteristics of carrier-based DPI formulations. We studied two particle size grades of silica microspheres, with volume median diameters of 3.31 μm and 8.14 μm, as fine excipient materials. Inhalation formulations, each composed of a lactose carrier material, one of the fine excipient materials (2.5% or 15.0% <em>w</em>/<em>w</em>), and a drug (fluticasone propionate) material (1.5% <em>w</em>/<em>w</em>) were prepared. The physical microstructure, the rheological properties, the aerosolization pattern, and the aerodynamic performance of the formulations were studied. At low concentration, the large silica microspheres had a more beneficial influence on the drug dispersibility than the small silica microspheres. At high concentration, only the small silica microspheres had a beneficial influence on the drug dispersibility. The results reveal influences of fine excipient materials on mixing mechanics. At low concentration, the fine particles improved deaggregation and distribution of the drug particles over the surfaces of the carrier particles. The large silica microspheres were associated with a greater mixing energy and a greater improvement in the drug dispersibility than the small silica microspheres. At high concentration, the large silica microspheres kneaded the drug particles onto the surfaces of the carrier particles and thus impaired the drug dispersibility. As a critical attribute of fine excipient materials in carrier-based dry powder inhalation formulations, the particle size demands robust specification setting.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100251"},"PeriodicalIF":4.7,"publicationDate":"2024-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000239/pdfft?md5=62d18652a5012b5acacc30fc1fd8ae03&pid=1-s2.0-S2590156724000239-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140950844","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"β-Cyclodextrin metal-organic framework as a green carrier to improve the dissolution, bioavailability, and liver protective effect of luteolin","authors":"Dan Yang ,&nbsp;Min Zhao ,&nbsp;Yihe Huang ,&nbsp;Liwen Chen ,&nbsp;Jiqin Fang ,&nbsp;Jiaonan Liu ,&nbsp;Miao Wang ,&nbsp;Chunjie Zhao","doi":"10.1016/j.ijpx.2024.100250","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100250","url":null,"abstract":"<div><p>The incidence of acetaminophen-induced liver injury has increased, but effective prevention methods are limited. Although luteolin has hepatoprotective activity, its low solubility and bioavailability limit its applications. Cyclodextrin metal-organic frameworks (CD-MOFs) possess 3D-network structures and large inner cavities, which make them excellent carriers of poorly soluble drugs. In this study, we used CD-MOFs as carriers to improve the dissolution of luteolin and assessed their antioxidant activity, bioavailability, and hepatoprotective effects. Luteolin was loaded into β-CD-MOF, γ-CD-MOF, β-CD, and γ-CD, and characterized by powder X-ray diffractometry (PXRD) and thermogravimetric analysis (TGA). Our results showed that luteolin-β-CD-MOF was the most stable. The main driving forces were hydrogen bonds and van der Waals forces, as determined by molecular simulation. The loading capacity of luteolin-β-CD-MOF was 14.67 wt%. Compared to raw luteolin, luteolin-β-CD-MOF exhibited a 4.50-fold increase in dissolution and increased antioxidant activity <em>in vitro</em>. Luteolin-β-CD-MOF increased the bioavailability of luteolin by approximately 4.04- and 11.07-fold in healthy rats and liver injured rats induced by acetaminophen <em>in vivo</em>, respectively. As determined by biochemical analysis, luteolin-β-CD-MOF exhibited a better hepatoprotective effect than raw luteolin in rats with acetaminophen-induced liver injury. This study provides a new approach for preventing acetaminophen-mediated liver damage.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100250"},"PeriodicalIF":4.7,"publicationDate":"2024-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000227/pdfft?md5=c6f32db4696c4216d3e1851761876fe9&pid=1-s2.0-S2590156724000227-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140816043","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"A drug repurposing approach of Atorvastatin calcium for its antiproliferative activity for effective treatment of breast cancer: In vitro and in vivo assessment","authors":"Dina M. Gaber ,&nbsp;Sherihan S. Ibrahim ,&nbsp;Ashraf K. Awaad ,&nbsp;Yasmine M. Shahine ,&nbsp;Salma Elmallah ,&nbsp;Hebatallah S. Barakat ,&nbsp;Noha I. Khamis","doi":"10.1016/j.ijpx.2024.100249","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100249","url":null,"abstract":"<div><p>Breast cancer, the most common cancer among women, caused over 500,000 deaths in 2020. Conventional treatments are expensive and have severe side effects. Drug repurposing is a novel approach aiming to reposition clinically approved non-cancer drugs into newer cancer treatments. Atorvastatin calcium (ATR Ca) which is used for the treatment of hypercholesterolemia has potential to modulate cell growth and apoptosis. The study aimed at utilizing gelucire-based solid lipid nanoparticles (SLNs) and lactoferrin (Lf) as targeting ligand to enhance tumor targeting of atorvastatin calcium for effective management of breast cancer. Lf-decorated-ATR Ca-SLNs showed acceptable particle size and PDI values &lt;200 nm and 0.35 respectively, entrapment efficiency &gt;90% and sustained drug release profile with 78.97 ± 12.3% released after 24 h. <em>In vitro</em> cytotoxicity study on breast cancer cell lines (MCF-7) showed that Lf-decorated-ATR Ca-SLNs obviously improved anti-tumor activity by 2 to 2.5 folds compared to undecorated ATR Ca-SLNs and free drug. Further, <em>In vivo</em> study was also carried out using Ehrlich breast cancer model in mice. Caspase-3 apoptotic marker revealed superior antineoplastic and apoptosis-inducing activity in the groups treated with ATR Ca-SLNs either decorated/ undecorated with Lf in dosage 10 mg/kg/day <em>p &lt;</em> <em>0.001</em> with superior activity for lactoferrin-decorated formulation.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100249"},"PeriodicalIF":4.7,"publicationDate":"2024-04-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000215/pdfft?md5=f75da30078fb3cbd4ab1268e1bef84ed&pid=1-s2.0-S2590156724000215-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140632766","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Nanomedicine-based disulfiram and metal ion co-delivery strategies for cancer treatment","authors":"Xinyue Shen ,&nbsp;Huixiang Sheng ,&nbsp;Ying Zhang ,&nbsp;Xuan Dong ,&nbsp;Longfa Kou ,&nbsp;Qing Yao ,&nbsp;Xinyu Zhao","doi":"10.1016/j.ijpx.2024.100248","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100248","url":null,"abstract":"<div><p>Disulfiram (DSF) is a second-line drug for the clinical treatment of alcoholism and has long been proven to be safe for use in clinical practice. In recent years, researchers have discovered the cancer-killing activity of DSF, which is highly dependent on the presence of metal ions, particularly copper ions. Additionally, free DSF is highly unstable and easily degraded within few minutes in blood circulation. Therefore, an ideal DSF formulation should facilitate the co-delivery of metal ions and safeguard the DSF throughout its biological journey before reaching the targeted site. Extensive research have proved that nanotechnology based formulations can effectively realize this goal by strategic encapsulation therapeutic agents within nanoparticle. To be more specific, this is accomplished through precise delivery, coordinated release of metal ions at the tumor site, thereby amplifying its cytotoxic potential. Beyond traditional co-loading techniques, innovative approaches such as DSF-metal complex and metal nanomaterials, have also demonstrated promising results at the animal model stage. This review aims to elucidate the anticancer mechanism associated with DSF and its reliance on metal ions, as well as to provide a comprehensive overview of recent advances in the arena of nanomedicine based co-delivery strategies for DSF and metal ion in the context of cancer therapy.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100248"},"PeriodicalIF":4.7,"publicationDate":"2024-04-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000203/pdfft?md5=52779c429393da062e4f422c900ca257&pid=1-s2.0-S2590156724000203-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140638813","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Fabrication and application of targeted ciprofloxacin nanocarriers for the treatment of chronic bacterial prostatitis","authors":"Sahar I. Mohammad ,&nbsp;Basmah Nasser Aldosari ,&nbsp;Magda M. Mehanni ,&nbsp;Ahmed O. El-Gendy ,&nbsp;Walaa G. Hozayen ,&nbsp;Obaid Afzal ,&nbsp;Randa Mohammed Zaki ,&nbsp;Ossama M. Sayed","doi":"10.1016/j.ijpx.2024.100247","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100247","url":null,"abstract":"<div><p>Pathogenic bacteria cause chronic bacterial prostatitis (CBP). CPB is characterized by urinary tract infection and persistence of pathogenic bacteria in prostatic secretion. Owing to poor blood supply to the prostate gland and limited drug penetration, CBP treatment is difficult. Transferosomes are ultradeformable vesicles for nanocarrier applications, which have become an important area of nanomedicine. Such carriers are specifically targeted to the pathological area to provide maximum therapeutic efficacy. It consists of a lipid bilayer soybean lecithin phosphatidylcholine (PC), an edge activator Tween 80 with various ratios, and a chloroform/methanol core. Depending on the lipophilicity of the active substance, it can be encapsulated within the core or among the lipid bilayer. Due to their exceptional flexibility, which enables them to squeeze themselves through narrow pores that are significantly smaller than their size, they can be a solution. One formulation (Cipro5 PEG) was selected for further in vitro analysis and was composed of phosphatidylcholine (PC), Tween 80, and polyethylene glycol-6 stearate (PEG-6 stearate) in a ratio of 3:3:1 in a chloroform/methanol mixture (1:2 <em>v</em>/v). In vitro, the results showed that PEGylated transferosomes had faster drug release, higher permeation, and increased bioavailability. The transferosomes were quantified with a particle size of 202.59 nm, a zeta potential of-49.38 mV, and a drug entrapment efficiency of 80.05%. The aim of this study was to investigate drug targeting. Therefore, Monoclonal antibody IgG was coupled with Cipro5 PEG, which has specificity and selectivity for conjugated nanoparticles. In vivo, a total of twenty-five adult Wistar rats were obtained and randomly divided into 5 groups, each of 5 rats at random: the control group, blank group, positive control group, Cipro 5PEG group, and Cipro 5PEG coupled with IgG antibody group. The cytokines levels (IL-1β, IL-8, and TNF-α) in the serum were detected by analysis kits. Compared with the control group, treatment with Cipro 5PEG coupled with the IgG antibody could significantly inhibit cytokines, according to histological analysis. Cipro 5PEG, coupled with the IgG antibody group, reduced prostate tissue inflammation. Hence, our results show a promising approach to delivering antibiotics for the targeted therapy of CBP.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100247"},"PeriodicalIF":4.7,"publicationDate":"2024-04-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000197/pdfft?md5=2df5d3cf9672f87c7c6cb99c150ad6bb&pid=1-s2.0-S2590156724000197-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140647683","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}