International Journal of Pharmaceutics: X最新文献

{"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}

{"title":"Fabrication and in vitro/vivo evaluation of quercetin nanocrystals stabilized by glycyrrhizic acid for liver targeted drug delivery","authors":"Baode Shen ,&nbsp;Yuwen Zhu ,&nbsp;Fengxia Wang ,&nbsp;Xiang Deng ,&nbsp;Pengfei Yue ,&nbsp;Hailong Yuan ,&nbsp;Chenying Shen","doi":"10.1016/j.ijpx.2024.100246","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100246","url":null,"abstract":"<div><p>The purpose of this study was to design novel drug nanocrystals (NCs) stabilized by glycyrrhizic acid (GL) for achieving liver targeted drug delivery due to the presence of GL receptor in the hepatocytes. Quercetin (QT) exhibits good pharmacological activities for the treatment of liver diseases, including liver steatosis, fatty hepatitis, liver fibrosis, and liver cancer. It was selected as a model drug owing to its poor water solubility. QT NCs stabilized by GL (QT-NCs/GL) were fabricated by wet media milling technique and systemically evaluated. QT-NCs stabilized by poloxamer 188 (QT-NCs/P188) were prepared as a reference for comparison of in vitro and in vivo performance with QT-NCs/GL. QT-NCs/GL and QT-NCs/P188 with similar particle size around 130 nm were successfully fabricated by wet media milling technique. Both of QT-NCs/GL and QT-NCs/P188 showed irregular particles and short rods under SEM. XRPD revealed that QT-NCs/GL and QT-NCs/P188 remained in crystalline state with reduced crystallinity. QT-NCs/GL and QT-NCs/P188 exhibited significant solubility increase and drug release improvement of QT as compared to raw QT. No significant difference for the plasma concentration–time curves and pharmacokinetic parameters of QT were found following intravenous administration of QT-NCs/GL and QT-NCs/P188. However, a significantly higher liver distribution of QT following intravenous administration of QT-NCs/GL was observed in comparison to QT-NCs/P188, indicating QT-NCs stabilized by GL could achieve liver targeted delivery of QT. It could be concluded that GL used as stabilizer of QT NCs have a great potential for liver targeted drug delivery.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100246"},"PeriodicalIF":4.7,"publicationDate":"2024-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000185/pdfft?md5=97b6b11389ba07f9c16c6ab1f4ab2404&pid=1-s2.0-S2590156724000185-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140542484","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":"Formulation and evaluation of azithromycin-loaded silver nanoparticles for the treatment of infected wounds","authors":"Mohammed S. Saddik ,&nbsp;Mostafa F. Al-Hakkani ,&nbsp;Ahmed M. Abu-Dief ,&nbsp;Mohamed S. Mohamed ,&nbsp;Islam A. Al-Fattah ,&nbsp;Mahmoud Makki ,&nbsp;Mohamed A. El-Mokhtar ,&nbsp;Marwa A. Sabet ,&nbsp;M.S. Amin ,&nbsp;Hoda A. Ahmed ,&nbsp;Khalaf Al-Ghamdi ,&nbsp;Mostafa K. Mohammad ,&nbsp;Mohammad H.A. Hassan","doi":"10.1016/j.ijpx.2024.100245","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100245","url":null,"abstract":"<div><p>Infected wounds pose a significant challenge in healthcare, requiring innovative therapeutic strategies. Therefore, there is a critical need for innovative pharmaceutical materials to improve wound healing and combat bacterial growth. This study examined the efficacy of azithromycin-loaded silver nanoparticles (AZM-AgNPs) in treating infected wounds. AgNPs synthesized using a green method with <em>Quinoa</em> seed extract were loaded with AZM. Characterization techniques, including X-ray Powder Diffraction (XRD), scanning electron microscope (SEM), transmission electron microscope (TEM), and Uv-Vis analysis were utilized. The agar diffusion assay and determination of the MIC were used to assess the initial antibacterial impact of the formulations on both MRSA and <em>E. coli</em>. In addition, the antimicrobial, wound-healing effects and histological changes following treatment with the AZM-AgNPs were assessed using an infected rat model. The nanoparticles had size of 24.9 ± 15.2 nm for AgNPs and 34.7 ± 9.7 nm for AZM-AgNPs. The Langmuir model accurately characterized the adsorption of AZM onto the AgNP surface, indicating a maximum loading capacity of 162.73 mg/g. AZM-AgNPs exhibited superior antibacterial properties in vivo and in vitro compared to controls. Using the agar diffusion technique, AZM-AgNPs showed enhanced zones of inhibition against <em>E. coli</em> and MRSA, which was coupled with decreased MIC levels. In addition, in vivo studies showed that AZM-AgNP treated rats had the best outcome characterized by improved healing process, lower bacterial counts and superior epithelialization, compared to the control group. In conclusion, AZM-AgNPs can be synthesized using a green method with Quinoa seed with successful loading of azithromycin onto silver nanoparticles. In vitro and in vivo studies suggest the promising use of AZM-AgNPs as an effective therapeutic agent for infected wounds.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100245"},"PeriodicalIF":4.7,"publicationDate":"2024-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000173/pdfft?md5=878bdaea5d9707834044e9e7361d307b&pid=1-s2.0-S2590156724000173-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140545960","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":"Pectin nanoparticles loaded with nitric oxide donor drug: A potential approach for tissue regeneration","authors":"Noha I. Elsherif ,&nbsp;Abdulaziz M. Al-Mahallawi ,&nbsp;Iman Saad Ahmed ,&nbsp;Rehab N. Shamma","doi":"10.1016/j.ijpx.2024.100244","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100244","url":null,"abstract":"<div><p>The process of wound healing and tissue regeneration involves several key mechanisms to ensure the production of new tissues with similar cellular functions. This study investigates the impact of pectin, a natural polysaccharide, and nebivolol hydrochloride (NBV), a nitric oxide (NO) donor drug, on wound healing. Utilizing ionotropic gelation, NBV-loaded pectin nanoparticles were developed following a 2²3¹ full factorial design. The optimized formulation, determined using Design expert® software, exhibited an encapsulation efficiency percentage of 70.68%, zeta potential of −51.4 mV, and a particle size of 572 nm, characterized by a spherical, discrete morphology. An <em>in vivo</em> study was conducted to evaluate the effectiveness of the optimal formulation in wound healing compared to various controls. The results demonstrated the enhanced ability of the optimal formulation to accelerate wound healing. Moreover, histopathological examination further confirmed the formulation's benefits in tissue proliferation and collagen deposition at the wound site 15 days post-injury. This suggests that the developed formulation not only promotes faster healing but does so with minimal side effects, positioning it as a promising agent for effective wound healing and tissue regeneration.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100244"},"PeriodicalIF":4.7,"publicationDate":"2024-04-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000161/pdfft?md5=0f6a8ba3d90b739e7a06518972e60639&pid=1-s2.0-S2590156724000161-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140343930","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":"Feed factor profile prediction model for two-component mixed powder in the twin-screw feeder","authors":"Yuki Kobayashi ,&nbsp;Sanghong Kim ,&nbsp;Takuya Nagato ,&nbsp;Takuya Oishi ,&nbsp;Manabu Kano","doi":"10.1016/j.ijpx.2024.100242","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100242","url":null,"abstract":"<div><p>In continuous pharmaceutical manufacturing processes, it is crucial to control the powder flow rate. The feeding process is characterized by the amount of powder delivered per screw rotation, referred to as the feed factor. This study aims to develop models for predicting the feed factor profiles (FFPs) of two-component mixed powders with various formulations, while most previous studies have focused on single-component powders. It further aims to identify the suitable model type and to determine the significance of material properties in enhancing prediction accuracy by using several FFP prediction models with different input variables. Four datasets from the experiment were generated with different ranges of the mass fraction of active pharmaceutical ingredients (API) and the powder weight in the hopper. The candidates for the model inputs are (a) the mass fraction of API, (b) process parameters, and (c) material properties. It is desirable to construct a high-performance prediction model without the material properties because their measurement is laborious. The results show that using (c) as input variables did not improve the prediction accuracy as much, thus there is no need to use them.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100242"},"PeriodicalIF":4.7,"publicationDate":"2024-03-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000148/pdfft?md5=e39edc07e8ce19bfa70a064e4c6ae931&pid=1-s2.0-S2590156724000148-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140346680","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":"The interplay of poorly soluble drugs in dissolution from amorphous solid dispersions","authors":"Marcel Kokott,&nbsp;Jörg Breitkreutz,&nbsp;Raphael Wiedey","doi":"10.1016/j.ijpx.2024.100243","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100243","url":null,"abstract":"<div><p>In recent years, the application of fixed dose combinations of antiretroviral drugs in HIV therapy has been established. Despite numerous therapeutic benefits, this approach poses several challenges for the formulation development especially when poorly soluble drugs are considered. Amorphous solid dispersions (ASD) thereby have gained considerable interest in the pharmaceutical field, however, mainly including binary systems containing only one drug and a polymer. The <em>co</em>-formulation of two amorphous drugs can be accompanied by an immense increase in the complexity of the system as exemplarily reported for ritonavir and lopinavir embedded in a composite polymer matrix of PVPVA. The present study aims to present a new formulation approach to overcome the well-documented interaction during dissolution. Two different polymers, PVPVA and HPMCAS were used to produce ASDs for both drugs individually via hot-melt extrusion. The embedding of lopinavir in the slower dissolving polymer HPMCAS, while using PVPVA for ritonavir was found to significantly improve the overall dissolution performance compared to the individual use of PVPVA as well as to the commercial product Kaletra®. In addition, the use of different grades of HPMCAS demonstrated the possibility to further modify the dissolution profile. For a preliminary biorelevant assessment, the selected formulations were tested in a biphasic dissolution setup.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100243"},"PeriodicalIF":4.7,"publicationDate":"2024-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S259015672400015X/pdfft?md5=0aee7123035bce40c8fcfd17e816b6a3&pid=1-s2.0-S259015672400015X-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140343929","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":"Spanlastic-laden nanogel as a plausible platform for dermal delivery of bimatoprost with superior cutaneous deposition and hair regrowth efficiency in androgenic alopecia","authors":"Bjad K. Almutairy ,&nbsp;El-Sayed Khafagy ,&nbsp;Mohammed F. Aldawsari ,&nbsp;Abdullah Alshetaili ,&nbsp;Hadil Faris Alotaibi ,&nbsp;Amr Selim Abu Lila","doi":"10.1016/j.ijpx.2024.100240","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100240","url":null,"abstract":"<div><p>Bimatoprost (BIM) is a prostaglandin F2α analogs originally approved for the treatment of glaucoma and ocular hypertension. Recent studies have highlighted its potential to boost hair growth. The objective of this investigation is to challenge the potential of spanlastics (SLs) as a surfactant-based vesicular system for promoting the cutaneous delivery of BIM for the management of alopecia. BIM-loaded spanlastics (BIM-SLs), composed of Span as the main vesicle component and Tween as the edge activator, were fabricated by ethanol injection method. The formulated BIM-SLs were optimized by 2³ full factorial design. The optimized formula (F1) was characterized for entrapment efficiency, surface charge, vesicle size, and drug release after 12 h (Q_12h). The optimized formula (F1) exhibited high drug entrapment efficiency (83.1 ± 2.1%), appropriate zeta potential (−19.9 ± 2.1 mV), Q_12h of 71.3 ± 5.3%, and a vesicle size of 364.2 ± 15.8 nm, which favored their cutaneous accumulation. In addition, <em>ex-vivo</em> skin deposition studies revealed that entrapping BIM within spanlastic-based nanogel (BIM-SLG) augmented the dermal deposition of BIM, compared to naïve BIM gel. Furthermore, <em>in vivo</em> studies verified the efficacy of spanlastic vesicles to boost the cutaneous accumulation of BIM compared to naive BIM gel; the AUC_0-12h of BIM-SLG was 888.05 ± 72.31 μg/mL.h, which was twice as high as that of naïve BIM gel (AUC_0-12h 382.86 ± 41.12 μg/mL.h). Intriguingly, BIM-SLG outperforms both naïve BIM gel and commercial minoxidil formulations in stimulating hair regrowth in an androgenetic alopecia mouse model. Collectively, spanlastic vesicles might be a potential platform for promoting the dermal delivery of BIM in managing alopecia.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100240"},"PeriodicalIF":4.7,"publicationDate":"2024-03-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000124/pdfft?md5=31c97412f1f763f28d6a16d81b46b73d&pid=1-s2.0-S2590156724000124-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140321255","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":"Halofuginone-guided nano-local therapy: Nano-thermosensitive hydrogels for postoperative metastatic canine mammary carcinoma with scar removal","authors":"Runan Zuo ,&nbsp;Lingqing Kong ,&nbsp;Wanjun Pang ,&nbsp;Shanxiang Jiang","doi":"10.1016/j.ijpx.2024.100241","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100241","url":null,"abstract":"<div><p>In female dogs, the highest morbidity and mortality rates cancer are the result of mammary adenocarcinoma, which presents with metastases in the lung. Other than early surgical removal, however, no special methods are available to treat mammary adenocarcinoma. Because human breast cancer and canine mammary carcinoma share clinical characteristics and heterogeneity, the canine model is a suitable spontaneous tumor model for breast cancer in humans. In this study, the physical swelling method was used to prepare halofuginone-loaded D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) polymer micelles nano-thermosensitive hydrogels (HTPM-gel). Furthermore, HTPM-gel was investigated via characterization, morphology, properties such as swelling experiment and <em>in vitro</em> release with reflecting its splendid nature. Moreover, HTPM-gel was further examined its capability to anti-proliferation, anti-migration, and anti-invasion. Ultimately, HTPM-gel was investigated for its <em>in vivo</em> anticancer activity in the post-operative metastatic and angiogenic canine mammary carcinoma. HTPM-gel presented spherical under transmission electron microscope (TEM) and represented grid structure under scanning electron microscope (SEM), with hydrodynamic diameter (HD) of 20.25 ± 2.5 nm and <em>zeta</em> potential (ZP) of 15.10 ± 1.82 mV. Additionally, HTPM-gel own excellent properties comprised of pH-dependent swelling behavior, sustained release behavior. To impede the migration, invasion, and proliferation of CMT-U27 cells, we tested the efficacy of HTPM-gel. Evaluation of <em>in vivo</em> anti-tumor efficacy demonstrates HTPM-gel exhibit a splendid anti-metastasis and anti-angiogenic ability, with exhibiting ideal biocompatibility. Notably, HTPM-gel also inhibited the scar formation in the healing process after surgery. In summary, HTPM-gel exhibited anti-metastasis and anti-angiogenic and scar repair features. According to the results of this study, HTPM-gel has encouraging clinical potential to treat tumors with multifunctional hydrogel.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100241"},"PeriodicalIF":4.7,"publicationDate":"2024-03-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000136/pdfft?md5=9b24978aa3117713504a565872d6dea9&pid=1-s2.0-S2590156724000136-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140327644","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":"Non-invasive caffeinated-nanovesicles as adipocytes-targeted therapy for cellulite and localized fats","authors":"Lobna M. Khalil ,&nbsp;Wessam M. El-Refaie ,&nbsp;Yosra S.R. Elnaggar ,&nbsp;Hamdy Abdelkader ,&nbsp;Adel Al Fatease ,&nbsp;Ossama Y. Abdallah","doi":"10.1016/j.ijpx.2024.100236","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100236","url":null,"abstract":"<div><p>Caffeine (CAF) is a non-selective adenosine A1 receptor antagonist which predominates in fat cells. When CAF binds to adenosine receptors, it increases cyclic adenosine monophosphate; inhibiting adipogenesis and inducing fat lipolysis. Resveratrol (RSV) is an antioxidant polyphenol possessing different anti-obesity mechanisms. Topical application of both hydrophilic CAF and lipophilic RSV is limited.</p><p>This study aimed to develop novel caffeinated-resveratrol bilosomes (CRB) and caffeine-bilosomes (CB) that could non-invasively target and deposit in fat cells. RSV bilosomes (RB) were prepared as a non-targeted system for comparison. CRB showed nanosize (364.1 nm ±6.5 nm) and high entrapment for both active compounds. Rats treated topically with CRB revealed a significant decrease (<em>P</em> = 0.039) in body weight. Histological analysis of the excised skin demonstrated a reduction in the subcutaneous fatty layer thickness and a decrease in the size of connective tissue-imbedded fat cells. Kidney histological examination of RB-treated rats showed subcapsular tubular epithelial cells with cytoplasmic vacuolation. This reflects a systemic effect of RSV from the non-targeted RB compared to CRB, which had a targeting effect on the adipose tissue. In conclusion, CAF in CRB significantly enhanced RSV deposition in adipose tissue and assisted its local-acting effect for managing obesity and cellulite.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100236"},"PeriodicalIF":4.7,"publicationDate":"2024-03-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000082/pdfft?md5=965207ea439ea05c29d9d734c2f11dba&pid=1-s2.0-S2590156724000082-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140137908","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 network of regulatory innovations to improve FDA quality assessments of human drug applications","authors":"Russie Tran,&nbsp;Grace Fraser,&nbsp;Adam C. Fisher,&nbsp;Sau L. Lee,&nbsp;Ashley Boam,&nbsp;Stelios Tsinontides,&nbsp;Jennifer Maguire,&nbsp;Lawrence X. Yu,&nbsp;Susan Rosencrance,&nbsp;Steven Kozlowski,&nbsp;Don Henry","doi":"10.1016/j.ijpx.2024.100239","DOIUrl":"https://doi.org/10.1016/j.ijpx.2024.100239","url":null,"abstract":"<div><p>A network of regulatory innovations brings a holistic approach to improving the submission, assessment, and lifecycle management of pharmaceutical quality information in the U.S. This dedicated effort in the FDA’s Center for Drug Evaluation and Research (CDER) aims to enhance the quality assessment of submissions for new drugs, generic drugs, and biological products including biosimilars. These regulatory innovations include developing or contributing: (i) the Knowledge-Aided Assessment and Structured Application (KASA), (ii) a new common technical document for quality (ICH M4Q(R2)), (iii) structured data on Pharmaceutical Quality/Chemistry, Manufacturing and Controls (PQ/CMC), (iv) Integrated Quality Assessment (IQA), (v) the Quality Surveillance Dashboard (QSD), and (vi) the Established Conditions tool from the ICH Q12 guideline. The innovations collectively drive CDER toward a more coordinated, effective, and efficient quality assessment. Improvements are made possible by structured regulatory submissions, a systems approach to quality risk management, and data-driven decisions based on science, risk, and effective knowledge management. The intended result is better availability of quality medicines for U.S. patients.</p></div>","PeriodicalId":14280,"journal":{"name":"International Journal of Pharmaceutics: X","volume":"7 ","pages":"Article 100239"},"PeriodicalIF":4.7,"publicationDate":"2024-03-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S2590156724000112/pdfft?md5=e8c8fe5fc89a8ee9a2360ed20920c21a&pid=1-s2.0-S2590156724000112-main.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140160102","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}