International Journal of Drug Delivery Technology最新文献

{"title":"A Bird Eye View on Effervescent Drug Delivery System","authors":"Sanjali Jadhav, Avinash Gangurde","doi":"10.25258/ijddt.13.3.45","DOIUrl":"https://doi.org/10.25258/ijddt.13.3.45","url":null,"abstract":"Effervescent drug delivery systems (EDDS) have gained significant attention in the pharmaceutical industry due to their unique characteristics and potential advantages over conventional dosage forms. This comprehensive review aims to provide an in-depth understanding of EDDS, including their formulation strategies, underlying mechanisms, and diverse applications in drug delivery. EDDS are effervescent dosage forms that release drugs upon water dissolution, leading toward carbon dioxide gas generation. The effervescence, resulting from the reaction between an acid and a base, facilitates rapid drug dissolution and enhances drug bioavailability. The primary components of an EDDS include an active pharmaceutical ingredient (API), effervescent agents (e.g., organic acids and bases), binders, disintegrants, and other excipients. Effervescent tablets, granules, powders, and effervescent-coated dosage forms are commonly employed formulations. Several factors, such as pH, temperature, solubility, and particle size, influence the drug’s effervescence process and subsequent release kinetics. The drug release mechanisms from EDDS can be attributed to various phenomena, including effervescence-driven disintegration, gas evolution, and solubilization. The effervescence-induced carbon dioxide bubbles mechanically disrupt the dosage form, leading to enhanced drug dissolution and subsequent release. Additionally, the carbon dioxide gas acts as a propellant, providing rapid drug delivery and potentially improving patient compliance. EDDS find applications in diverse therapeutic areas, including analgesics, antacids, dietary supplements, and antiviral agents. They offer several advantages, such as improved drug stability, enhanced bioavailability, increased patient convenience, and ease of administration, particularly for populations with swallowing difficulties. Furthermore, EDDS can be tailored to achieve controlled release, targeted drug delivery, and taste masking through appropriate formulation modifications. However, challenges associated with EDDS include their sensitivity to environmental conditions, potential drug degradation during effervescence, and the need for specialized packaging to maintain stability. The selection of suitable effervescent agents, excipients, and manufacturing processes is crucial to overcome these limitations and ensure consistent product performance. In conclusion, effervescent drug delivery","PeriodicalId":13851,"journal":{"name":"International Journal of Drug Delivery Technology","volume":"33 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135866573","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Preparation and Evaluation of Primidone Solid Lipid Nanoparticle for Alleviating Seizure Activity in Wistar Rats","authors":"Pooja Agarwal, B. Vasudha","doi":"10.25258/ijddt.13.3.24","DOIUrl":"https://doi.org/10.25258/ijddt.13.3.24","url":null,"abstract":"Introduction: In order to increase primidone’s anticonvulsant action, the study set out to manufacture it in solid lipid nanoparticle form (PRI-SLN). Method: Microemulsification and ultrasonication procedures were used to create 17 PRI-SLN formulations. Results: The PRI-SLN displayed a high entrapment efficiency (46.37 ± 2.42% to 81.82 ± 1.21%), as well as small particle size (149.9 ± 6.72 to 188.8 ± 5.25 nm). According to the in-vitro release study, PRI from SLNs releases more slowly than PRI by itself. The thermal analysis showed the drug’s compatibility with other substances and its presence in the more soluble amorphous state. Following a lethal and chronic dosage of picrotoxin, the PRI-SLN exhibited a higher anticonvulsant efficacy, according to in-vivo research on rats (p< 0.05). Conclusion: SLN with stronger anticonvulsant action can be made from PRI.","PeriodicalId":13851,"journal":{"name":"International Journal of Drug Delivery Technology","volume":"53 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135866872","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Phenol Glucosides as Potential Inhibitors of SGLT1 for Enhanced Diabetes Mellitus Treatment in Patients with Declining Renal Function","authors":"Mahesh Nemade, Khushabu Patil, Anjali Bedse, Piyush Chandra, Rakesh Ranjan, Harshal Tare, Manish Bhise","doi":"10.25258/ijddt.13.3.28","DOIUrl":"https://doi.org/10.25258/ijddt.13.3.28","url":null,"abstract":"Diabetes mellitus poses a significant global health challenge, necessitating the continual search for innovative therapeutic strategies. While sodium-glucose cotransporter 2 (SGLT2) inhibitors have shown promise in diabetes management, their efficacy diminishes in patients with declining renal function. This study aims to evaluate the potential of phenol glucosides as inhibitors for the sodium-glucose transport protein 1 (SGLT1), a key player in glucose uptake. We identified phlorizin as a representative phenol glucoside for experimental validation. The SGLT1 protein structure (PDB ID 7wmv) was analyzed through Ramachandran plot, ERRAT score, and ProSAweb Z-score, confirming its high-quality 3D conformation. A ligand-based virtual screening approach yielded 400 compounds that matched well with our pharmacophore models, including 10 compounds from virtual libraries. Notably, two compounds stood out for their high matching scores. Molecular docking simulations revealed strong binding affinities with SGLT1, especially for the compound CHEMBL2303983 with a binding energy of -11.2 kcal/mol. ADMET analysis was conducted to evaluate the drug-likeness & safety profile of such high-affinity compounds. The compounds exhibited variable water solubility and moderate lipophilicity but were generally compliant with most drug-likeness rules. However, certain challenges such as low GI absorption and inability to cross the blood-brain barrier were identified. No PAINS or Brenk alerts were raised, suggesting a low likelihood of assay interference or toxicity. In conclusion, our in-silico approach has identified promising candidates among phenol glucosides for inhibition of SGLT1, albeit with challenges in solubility and pharmacokinetics that require further optimization. The study opens new avenues for the synthesis and experimental verification of novel SGLT1 inhibitors.","PeriodicalId":13851,"journal":{"name":"International Journal of Drug Delivery Technology","volume":"14 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135867467","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"In-silico Exploration for Novel CDK8 Inhibitors: A Virtual Study by Pharmacophore Screening","authors":"Khushabu Patil, Mahesh Nemade, Anjali Bedse, Piyush Chandra, Rakesh Ranjan, Harshal Tare, Samir Patil","doi":"10.25258/ijddt.13.3.21","DOIUrl":"https://doi.org/10.25258/ijddt.13.3.21","url":null,"abstract":"The primary goal of this research is to identify potent and safe CDK8 inhibitors from the ChEMBL (kinases) database. The study employs a multi-faceted computational approach to achieve its objectives. Structure-based pharmacophore modeling is used for the initial screening of potential CDK8 inhibitors. Subsequent molecular docking studies are conducted to assess the binding affinities of the screened molecules. Finally, toxicity profiling is carried out to ensure the safety of the potential inhibitors. A total of 150 molecules were identified that passed the initial pharmacophore screening. Among these, molecule CHEMBL404766 was found to have the highest binding affinity in molecular docking studies. Furthermore CHEMBL404766 was found to be the safest candidate, exhibiting a negligible toxic dose in toxicity profiling. The study suggests the potential use of computational approaches for the identification and design of potent and safe CDK8 inhibitors. These findings have significant implications for the development of targeted therapies in diseases where CDK8 plays a crucial role","PeriodicalId":13851,"journal":{"name":"International Journal of Drug Delivery Technology","volume":"77 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135867704","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Evaluation of Few Immunological Parameters in Patients with Chronic Renal Failure in Najaf","authors":"Buthaina Abd E. Naser, Zainab S Mahdi","doi":"10.25258/ijddt.13.3.51","DOIUrl":"https://doi.org/10.25258/ijddt.13.3.51","url":null,"abstract":"Kidney failure is a chronic disease currently spreading worldwide, and one of its most important complications. Many indicators can be used to detect kidney disease early, which, if not treated, will eventually lead to failure. Kidney disease often leads to death. The study aimed to find a relationship between chronic renal failure and some immunological parameters and its relationship to the mechanism of dialysis, if it was hemorrhagic or peritoneal This study was conducted at the Kidney Center in Al-Sadr Teaching Hospital, Al-Najaf, and lasted from September 2022 to May 2023, including 57 males with chronic renal failure and 33 males. Listening male subjects who were considered as a control group. It was divided into age groups from 20 to 70, the duration of infection from 1 to 4 years, 5 to 7 and 8 to 15 years, and the body mass index included normal, excess, and obesity for patients with hemodialysis, peritoneal dialysis, and patients who did not reach the stage hemodialysis. The study concluded significant differences in the immunological indicators MCP-1 NTN-1, IL-1, α-TNF in the renal failure serum compared with healthy subjects. There was a positive relationship in the MCP-1, NTNT-1,IL-1, α TNF level. The results showed that there are significant differences p < 0.05 in age groups and body mass index in patients with renal failure compared with healthy subjects. There are no significant differences p > 0.05 with the duration of infection in patients with chronic renal failure compared with healthy controls. The presence of significant differences predicted kidney failure, p < 0.05, in the MCP-1 immunological indicators NTN-1, IL-1, α-TNF –TNF, The approved ROC table in patients with renal failure showed that the highest area of the biomarker NTN-1 and the lowest area is the biomarker α- TNF and immunological indicators are considered as predictors of early diagnosis of chronic renal failure.","PeriodicalId":13851,"journal":{"name":"International Journal of Drug Delivery Technology","volume":"46 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-09-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135867833","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Factors Aff ecting Foam Stability of Clotrimazole Vaginal Foam","authors":"Jumana M Falhi, H. Kassab","doi":"10.25258/ijddt.13.1.43","DOIUrl":"https://doi.org/10.25258/ijddt.13.1.43","url":null,"abstract":"Clotrimazole (CLT) is a broad-spectrum antifungal, synthetic imidazole derivative, used for Candida albicans the major cause of vaginitis. Vulvovaginal candidiasis (VVC) symptoms can cause discomfort and lower a women’s quality of life. Foams are used to apply formulation without the use of fi ngertips, the more stable the foam the better for coverage of larger surface area. CLT 2% vaginal foam were prepared as an O/W emulsion using Tween 20 and Span 20, Lemon oil, PEG 400, SLS, cetyl alcohol, and the formulas were evaluated for foamability and foam stability, foam density, cycles of freezing and thawing, heating, and cooling, and the impact of the chosen formula on Candida culture are all taken into consideration. The results showed that the CLT prepared successfully as vaginal foam, and the selected formula (F24) considered as the best formula which has good miscibility, texture and acceptable homogeneity, pH (4.8), drug content (97.5%), acceptable foamability and foam stability; foam expansion FE (70%), foam liquid stability (FLS) (40%), foam volume stability FVS (23.5%), gas fraction (GF) (35 mL), acceptable foam density (0.90), good stability at temperature changes, freeze–thaw cycle (pass), heating–cooling cycle (pass) with no phase separation, fast complete drug release (100% in about 40 min), no interaction between the solid components of the formula and acceptable inhibition zone against Candida strains. Finally, we can conclude that formulation of CLT as vaginal foam is an optimum method to improve patients’ compliance and cure the disease with low recurrence possibility due to fast release and long contact time with the aff ected area.","PeriodicalId":13851,"journal":{"name":"International Journal of Drug Delivery Technology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49168349","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Development of Size Optimized Bromelain Loaded Nanocarriers by Box- Behnken Design","authors":"Anit J George, Fels Saju, B. Mishra","doi":"10.25258/ijddt.13.1.02","DOIUrl":"https://doi.org/10.25258/ijddt.13.1.02","url":null,"abstract":"Bromelain (BRN) is an extensive product of investigation, regarded as eff ective naturally produced anticancer agents. Heterogeneity of tumors amongst patients and within disease, generates a necessity of personalization of nanomedicine. The size of nanoparticle is found to be a signifi cant target in enhancing precision therapeutics, by fondly accumulate it within the tumor microenvironment. The objective of the study is to achieve an optimum size of 50 to 100 nm BRN loaded nano carriers, to intensify the EPR eff ect and thereby overcome heterogeneity. Optimization of the nanoparticles commenced with the interrogation of eff ect by various formulation variables. The development of nanoparticles carried out by the nanoprecipitation method, where three independent variables, such as the amount of PLGA, Tween 80 and BRN are chosen after an overall screening and employed in Design Expert Software. The selected Box-Behnken design provides a total of 17 confi rmatory runs at varied levels of independent variables and detected its infl uence on responses. The runs resulted in an optimized formula with the desired particle size of 78.64 ± 2.14 nm and a maximum entrapment effi ciency of 89.14% at 24th hour. Then the selected formula characterized for polydispersity index, zeta potential, sanning electron m icroscopy, determination of drug content, study of in-vitro drug release etc.","PeriodicalId":13851,"journal":{"name":"International Journal of Drug Delivery Technology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49386117","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Bacterial Inhibition by Nanoparticles Treated Eucalyptus Extract Rana S. Hasan1, Maha E. Irzoqy2, Jalal M. Z. Jalal1, Safaa M. Sultan1","authors":"Rana S. Hasan, Maha E. Irzoqy, Jalal M Z Jalal, Safaa M. Sultan","doi":"10.25258/ijddt.13.1.54","DOIUrl":"https://doi.org/10.25258/ijddt.13.1.54","url":null,"abstract":"This study aimed to test the effi ciency of eucalyptus extracts (aqueous and alcoholic) supplemented with zinc nanoparticles in inhibiting gram-negative and gram-positive bacteria isolated in patients and their identifi cation. The results showed the identifi cation of two gram-negative bacteria: Salmonella and Entamoeba coli. Three types of gram-positive bacteria are Staphylococcus aureus, Staphylococcus albus, Staphylococcus epidermidis The eff ect of the aqueous extract of eucalyptus on the aforementioned species was tested, as it proved highly eff ective in infl uencing the growth of gram-positive bacteria than it is with gram-negative bacteria. While the eff ect of the alcoholic extract on the growth of negative bacteria was greater than its eff ect on the gram-positive bacteria and it proved highly eff ective on E. coli compared to Salmonella. The results of the synergistic action of the above-mentioned extracts when mixed with nano-zinc, showed a signifi cant increase in the inhibition of the growth of bacterial species. Whereas the turbulent eff ect of the alcoholic extract with nano-zinc showed a signifi cant eff ect on the growth of dye-negative bacteria compared to the eff ect of the aqueous extract supplemented with nano-zinc, which gave the highest eff ect in inhibiting the growth of gram-positive bacteria.","PeriodicalId":13851,"journal":{"name":"International Journal of Drug Delivery Technology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43096565","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Electrochemistry Study of Few Ru(II) and Zn(II)-Thione and Selone Complexes","authors":"Mohammed A. A. Abbas, Drew Reynolds, Julia L. Brumaghim","doi":"10.25258/ijddt.13.1.40","DOIUrl":"https://doi.org/10.25258/ijddt.13.1.40","url":null,"abstract":"Hydrogen peroxide, as a byproduct of cellular respiration through incomplete reduction of oxygen yields deleterious free radicals through the Fenton reaction with iron (II/III) and Cu(I/II). Metals, such as ruthenium and zinc, are also capable of like- Fenton reaction and the production of the hydroxide radical responsible for oxidative DNA damage. This damage manifests itself through single-strand breaks in the DNA backbone corresponding to mutation and apoptosis of cells. Thus, recent research has focused on preventing this reaction through organometallic antioxidative methods. Sulfur and selenium antioxidant compounds like dmit, dmise, and methimazole coordinate to iron and other Fenton-like metal centers. Based on the electrochemistry study, the result of cyclic voltammetry can predict whether or not these metals compounds generate hydroxyl radicals when they meet hydrogen peroxide in body by fi guring out their redox potentials. In this study, the electrochemical eff ects of these thione/selone ligands are determined through cyclic voltammetry with diff ering metal centers. Zinc complex redox activity was found to vary negligibly in changing solvent as well as scan speeds. In addition, ruthenium complexes from solvato complex precursors, their electrochemical peaks analyzed to prepare for reaction with hydrogen peroxide.","PeriodicalId":13851,"journal":{"name":"International Journal of Drug Delivery Technology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48820282","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Preparation and Evaluation of PVA, Chitosan Polymeric Matrixes and In-vitro Study for their Controlled Release of Enzalutamide","authors":"O. Hatem, Z. Alebady","doi":"10.25258/ijddt.13.1.44","DOIUrl":"https://doi.org/10.25258/ijddt.13.1.44","url":null,"abstract":"Enzalutamide is an eff ective androgen signaling receptor inhibitor that aff ects the androgen pathway in various ways. Enzalutamide can reduce the competitive binding of testosterone to the androgen receptor. It also inhibits the translocation of the activated androgen receptor for the cytoplasm to the nucleus, and its binding to DNA and cofactors recruitment to the binding site. This study evaluated polyvinyl alcohol/chitosan hydrogels as a pH-sensitive matrix drug delivery system for enzalutamide. The release of enzalutamide from PVA/CS hydrogel were determined at the simulated gastric and intestinal fl uid (SGF and SIF, respectively). Various kinetic models were employed to evaluate the drug release’s kinetic mechanism. The drug release was infl uenced by the concentration of polymers, the pH of the release medium, and the amount of cross-linking agent. Hydrogels containing (60:40) PVA to chitosan showed a higher release percentage of about 98% at SIF. The kinetic models showed that the release process follows the Higuchi model in SGF with a regression coeffi cient of 0.925. In contrast, SIF follows the fi rstorder model with a regression coeffi cient value of 0.994. The results confi rmed that the new formed PVA/CS hydrogels are potential systems for enzalutamide-controlled drug delivery","PeriodicalId":13851,"journal":{"name":"International Journal of Drug Delivery Technology","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-03-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49036388","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}