المؤلفون: Zhao Y, Xu X, Dai A, Jia Y, Wang W

المصدر: International Journal of Nanomedicine, Vol Volume 19, Pp 5721-5737 (2024)

مصطلحات موضوعية: hot melt extrusion technology, curcumin, nanocrystals, dissolution, absorption in vivo, Medicine (General), R5-920

الوصف: Yujie Zhao,1 Xiaoyin Xu,1 Anyin Dai,2 Yunxiang Jia,1 Wenxi Wang1 1College of Pharmacy, Zhejiang University of Technology, Hangzhou, People’s Republic of China; 2Department of Pharmacy, The 903rd Hospital of People’s Liberation Army, Hangzhou, People’s Republic of ChinaCorrespondence: Wenxi Wang, College of Pharmacy, Zhejiang University of Technology, 18# Chaowang Road, Hangzhou, Zhejiang, 310014, People’s Republic of China, Tel +86 571 8832 0772, Fax +86 571 8832 0320, Email yjw@zjut.edu.cnPurpose: Curcumin nanocrystals (Cur-NCs) were prepared by hot melt extrusion (HME) technology to improve the dissolution and bioavailability of curcumin (Cur).Methods: Cur-NCs with different drug-carrier ratios were prepared by one-step extrusion process with Eudragit® EPO (EEP) as the carrier. The dispersed size and solid state of Cur in extruded samples were characterized by dynamic light scattering (DLS), scanning electron microscope (SEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD). The thermal stability of Cur was analyzed by thermogravimetric analysis (TGA) and high performance liquid chromatography (HPLC). Dissolution and pharmacokinetics were studied to evaluate the improvement of dissolution and absorption of Cur by nano-preparation.Results: Cur-NCs with particle sizes in the range of 50~150 nm were successfully prepared by using drug-carrier ratios of 1:1, 2:1 and 4:1, and the crystal form of Cur was Form 1 both before and after HME. The extrudate powders showed very efficient dissolution with the cumulative dissolution percentage of 80% in less than 2 min, and the intrinsic dissolution rates of them were 13.68 ± 1.20 mg/min/cm2, 11.78 ± 0.57 mg/min/cm2 and 4.35 ± 0.20 mg/min/cm2, respectively, whereas that of pure Cur was only 0.04 ± 0.00 mg/min/cm2. The TGA data demonstrated that the degradation temperature of Cur was about 250 °C, while the HPLC results showed Cur was degraded when extruded at the temperature over 150 °C. Pharmacokinetic experiment showed a significant improvement in the absorption of Cur. The Cmax of Cur in the Cur-NC group was 1.68 times that of pure Cur group, and the Cmax and area under the curve (AUC0-∞) of metabolites were 2.79 and 4.07 times compared with pure Cur group.Conclusion: Cur-NCs can be prepared by HME technology in one step, which significantly improves the dissolution and bioavailability of Cur. Such a novel method for preparing insoluble drug nanocrystals has broad application prospects. Keywords: hot melt extrusion technology, curcumin, nanocrystals, dissolution, absorption in vivo

وصف الملف: electronic resource

العلاقة: https://www.dovepress.com/enhanced-dissolution-and-bioavailability-of-curcumin-nanocrystals-prep-peer-reviewed-fulltext-article-IJNTest; https://doaj.org/toc/1178-2013Test

الوصول الحر: https://doaj.org/article/e5c636aa7f704649ba75753fc5ec103eTest

المؤلفون: Ju Ri Ye, Ha Yeon Lee, Yea-Jin Park, Yong Kwon Chae, Hyo-Jin An, Jong-Suep Baek, Ok Hyung Nam

المصدر: Medicina, Vol 59, Iss 12, p 2066 (2023)

مصطلحات موضوعية: wound healing, natural product, hot melt extrusion technology, biocompatible materials, Medicine (General), R5-920

الوصف: Background and Objectives: In spite of the oral environment being healing-prone, its dynamic changes may affect wound healing. The purpose of this study was to assess the oral wound healing effect of Angelica gigas Nakai (AG) prepared by hot-melt extrusion. Materials and Methods: Human gingival fibroblast (HGF) cells were treated with AG or AG via hot-melt extrusion (AGH) for 24 h to determine the optimal concentration. For evaluating the anti-inflammatory effect of AG and AGH, a nitric oxide assay was performed under lipopolysaccharide (LPS) stimulation. The wound-healing effects of AG and AGH were evaluated using cell proliferation/migration assays and wound-healing marker expression through qRT-PCR. Results: Both AG and AGH showed no cytotoxicity on HGH cells. Regarding nitric oxide production, AGH significantly decreased LPS-induced nitric oxide production (p < 0.05). AGH showed a significantly positive result in the cell proliferation/cell migration assay compared with that in AG and the control. Regarding wound healing marker expression, AGH showed significantly greater VEGF and COL1α1 expression levels than those in the others (p < 0.05), whereas α-SMA expression was significantly different among the groups. Conclusions: Within the limits of this study, AGH accelerated oral wound healing in vitro.

وصف الملف: electronic resource

العلاقة: https://www.mdpi.com/1648-9144/59/12/2066Test; https://doaj.org/toc/1010-660XTest; https://doaj.org/toc/1648-9144Test

الوصول الحر: https://doaj.org/article/68cc56fb285e4376a41aa7697e770939Test

المؤلفون: Chen, Lingwu, Hu, Enshi, Shen, Peiya, Qian, Shuai, Heng, Weili, Zhang, Jianjun, Gao, Yuan, Wei, Yuanfeng

المصدر: Pharm Res ; ISSN:1573-904X ; Volume:41 ; Issue:6

مصطلحات موضوعية: amorphous solid dispersion, drug release plateau, hot melt extrusion technology, polymer composite matrix, sustained-release regulation

الوصف: This study was designed to develop ibuprofen (IBU) sustained-release amorphous solid dispersion (ASD) using polymer composites matrix with drug release plateaus for stable release and to further reveal intrinsic links between polymer' matrix ratios and drug release behaviors.

العلاقة: https://doi.org/10.1007/s11095-024-03709-yTest; https://pubmed.ncbi.nlm.nih.gov/38744732Test

الإتاحة: https://doi.org/10.1007/s11095-024-03709-yTest
https://pubmed.ncbi.nlm.nih.gov/38744732Test

المؤلفون: Moro, Franco Henrique, Carvalho, Renata Aquino de, Barud, Hernane da Silva, Amaral, André Capaldo, Silva, Eraldo Jannone da

المصدر: Research, Society and Development; Vol. 11 No. 6; e58111629472 ; Research, Society and Development; Vol. 11 Núm. 6; e58111629472 ; Research, Society and Development; v. 11 n. 6; e58111629472 ; 2525-3409

مصطلحات موضوعية: Tecnologia de extrusão por fusão a quente, Tecidos suporte, Medicina regenerativa, Engenharia tecidual, Impressão tridimensional, Hot melt extrusion technology, Tissue scaffolds, Regenerative medicine, Tissue engineering, Printing, three-dimensional, Tecnología de extrusión de fusión en caliente, Andamios del tejido, Ingeniería de tejidos, Impresión tridimensional

الوصف: Use biological or synthetic scaffolds to conduct cellular events of the regenerative process constitute one of the major strategies in regenerative medicine area. Customized scaffolds built by additive manufacturing prove to be a great solution to this problem. Two desired features that aid in scaffold’s biocompatibility are the surface roughness and the geometric characteristic of the topography, usually achieved by a chemical procedure performed after printing. This research presented a modification on a 3D printer nozzle for directly generating an external topography in the extruded filaments, eliminating the need for an additional post-processing step. Cell morphology and viability on supports printed by the proposed and conventional method were evaluated in in vitro experiments and the new nozzle proved to be efficient in generating printed filaments with a degree of cytocompatibility superior to those obtained by conventional filaments. ; El uso de soportes biológicos o sintéticos para conducir eventos celulares del proceso regenerativo es una de las principales estrategias en el campo de la medicina regenerativa. Los soportes personalizados producidos por fabricación aditiva demuestran ser una gran solución a este problema. Dos características deseadas que ayudan en la biocompatibilidad de los soportes son la rugosidad de la superficie y la característica geométrica de su topografía, generalmente logradas por un procesamiento químico realizado después de la impresión. Esta investigación presenta la propuesta para obtener una boquilla de impresora 3D capaz de generar directamente una topografía externa sobre los filamentos extruidos, eliminando la necesidad de un paso adicional de postprocesado. La morfología celular y la viabilidad sobre soportes impresos por el método propuesto y convencional fueron evaluadas en experimentos in vitro y la nueva boquilla demostró ser eficiente en la generación de filamentos impresos con un grado de citocompatibilidad superior a los obtenidos por filamentos convencionales. ...

وصف الملف: application/pdf

العلاقة: https://rsdjournal.org/index.php/rsd/article/view/29472/25527Test; https://rsdjournal.org/index.php/rsd/article/view/29472Test

الإتاحة: https://doi.org/10.33448/rsd-v11i6.29472Test
https://rsdjournal.org/index.php/rsd/article/view/29472Test

المؤلفون: Sagar, Salave, Kedar, Prayag, Dhwani, Rana, Prakash, Amate, Rupali, Pardhe, Ajinkya, Jadhav, Anil B, Jindal, Derajram, Benival

المصدر: Recent Advances in Drug Delivery and Formulation. 16:170-191

مصطلحات موضوعية: Hot Temperature, Polymers, Delayed-Action Preparations, Hot Melt Extrusion Technology, Biomedical Engineering, Technology, Pharmaceutical, Pharmaceutical Science

الوصف: Background: The Hot Melt Extrusion (HME) technique has shown tremendous potential in transforming highly hydrophobic crystalline drug substances into amorphous solids without using solvents. This review explores in detail the general considerations involved in the process of HME, its applications and advances. Objective: The present review examines the physicochemical properties of polymers pertinent to the HME process. Theoretical approaches for the screening of polymers are highlighted as a part of successful HME processed drug products. The critical quality attributes associated with the process of HME are also discussed in this review. HME plays a significant role in the dosage form design, and the same has been mentioned with suitable examples. The role of HME in developing several sustained release formulations, films, and implants is described along with the research carried out in a similar domain. Methods: The method includes the collection of data from different search engines like PubMed, ScienceDirect, and SciFinder to get coverage of relevant literature for accumulating appropriate information regarding HME, its importance in pharmaceutical product development, and advanced applications. Results: HME is known to have advanced pharmaceutical applications in the domains related to 3D printing, nanotechnology, and PAT technology. HME-based technologies explored using Design-of- Experiments also lead to the systematic development of pharmaceutical formulations. Conclusion: HME remains an adaptable and differentiated technique for overall formulation development.

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3ae2f4e0d0eb68e704d02fec1c22b589Test
https://doi.org/10.2174/2667387816666220819124605Test

المؤلفون: Sung-Min Choi, Sung-Hoon Lee, Chin-Yang Kang, Jun-Bom Park

المصدر: Pharmaceutics; Volume 12; Issue 8; Pages: 757

مصطلحات موضوعية: hot-melt extrusion technology, cilostazol, dissolution rate and permeability, PBPK simulation, parameter-sensitive analysis

الوصف: The aim of this study was to control the dissolution rate and permeability of cilostazol. To enhance the dissolution rate of the active pharmaceutical ingredient (API), hot-melt extrusion (HME) technology was applied to prepare a solid dispersion (SD). To control permeability in the gastrointestinal tract regardless of food intake, the HME process was optimized based on physiologically based pharmacokinetic (PBPK) simulation. The extrudates were produced using a laboratory-scale twin-screw hot-melt extruder with co-rotatory screws and a constant feeding rate. Next, for PBPK simulation, parameter-sensitive analysis (PSA) was conducted to determine the optimization approach direction. As demonstrated by the dissolution test, the solubility of extrudate was enhanced comparing cilostazol alone. Based on the PSA analysis, the surfactant induction was a crucial factor in cilostazol absorption; thus, an extrudate with an even distribution of lipids was produced using hot-melt extrusion technology, for inducing the bile salts in the gastrointestinal tract. In vivo experiments with rats demonstrated that the optimized hot-melt extruded formulation was absorbed more rapidly with lower deviation and regardless of the meal consumed when compared to marketed cilostazol formulations.

وصف الملف: application/pdf

العلاقة: Pharmaceutical Technology, Manufacturing and Devices; https://dx.doi.org/10.3390/pharmaceutics12080757Test

الإتاحة: https://doi.org/10.3390/pharmaceutics12080757Test

المؤلفون: Suresh Bandari, Karthik Yadav Janga, Sandeep Sarabu, Narendar Dudhipala, Feng Zhang, Venkata Raman Kallakunta, Michael A. Repka

المصدر: Eur J Pharm Biopharm

مصطلحات موضوعية: Materials science, Nifedipine, Polymers, Scanning electron microscope, Chemistry, Pharmaceutical, Drug Compounding, Pharmaceutical Science, Article, Excipients, Differential scanning calorimetry, Drug Stability, Multi unit, Solubility, chemistry.chemical_classification, Drug Carriers, Hot Melt Extrusion Technology, Temperature, Humidity, General Medicine, Polymer, Amorphous solid, Drug Liberation, chemistry, Chemical engineering, Delayed-Action Preparations, Extrusion, Dispersion (chemistry), Biotechnology

الوصف: The current study is aimed at the development of chrono modulated multiple unit particulate systems (MUPS) of nifedipine (ND) by a continuous double extrusion process. ND, a poorly soluble drug was formulated into an amorphous solid dispersion (ASD) to improve its solubility. Further, the ASD was converted into MUPS to control the drug release through a combination of pulsatile and sustained release portions. In the preparation of the ASD, the polymer HPMCAS LG was employed at different concentrations. MUPS were formulated by using Eudragit® FS100, Eudragit® RSPO, Klucel™ HF and lipids Precirol® ATO 5, Geleol™, Compritol® ATO5. The differential scanning calorimetry and powder X-ray diffraction studies of MUPS revealed the amorphous nature of ND. Scanning electron microscopy (SEM) studies depicted the surface morphology of the ASD and the gradual change in the surface of the coated MUPS during in-vitro release studies. The in-vitro drug release profiles of ASD indicated significant improvement (p 0.05) of solubility of ND and MUPS demonstrated a combination of pulsatile and zero-order controlled release up to 12 h. Accelerated stability studies for MUPS at 40 °C/75% RH revealed the formulations were stable. These findings suggest hot melt double extrusion as a potential alternative for conventional techniques to produce MUPS.

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b002f18a97f33f64c94ddd08d2ad8127Test
https://doi.org/10.1016/j.ejpb.2021.08.014Test

المؤلفون: Deck Khong Tan, Ali Nokhodchi, Mohammed Maniruzzaman, Niko Munzenrieder

المصدر: Current Drug Delivery. 18:700-711

مصطلحات موضوعية: chemistry.chemical_classification, Materials science, Plastics extrusion, Hot Melt Extrusion Technology, Pharmaceutical Science, Biocompatible Materials, Polymer, Polyethylene glycol, Miscibility, chemistry.chemical_compound, chemistry, Chemical engineering, Polylactic acid, Printing, Three-Dimensional, PEG ratio, Drug delivery, Technology, Pharmaceutical, Extrusion, Tablets

الوصف: Background:: Fused Deposition Modelling (FDM) 3D printing has received much interest as a fabrication method in the medical and pharmaceutical industry due to its accessibility and cost-effectiveness. A low-cost method to produce biocompatible and biodegradable filaments can improve the usability of FDM 3D printing for biomedical applications. Objectives:: The feasibility of producing low-cost filaments suitable for FDM 3D printing via single screw and twin-screw hot melt extrusion was explored. Methods:: A single-screw extruder and a twin-screw extruder were used to produce biocompatible filaments composed of varying concentrations of polyethylene glycol (PEG) at 10%, 20%, 30% w/w and polylactic acid (PLA) 90%, 80% and 70% w/w, respectively. DSC, TGA and FTIR were employed to investigate the effect of PEG on the PLA filaments. Results:: The presence of PEG lowered the processing temperature of the formulation compositions via melt-extrusion, making it suitable for pharmaceutical applications. The use of PEG can lower the melting point of the PLA polymer to 170°C, hence lowering the printing temperature. PEG can also improve the plasticity of the filaments, as the rupture strain of twin-screw extruded filaments increased up to 10-fold as compared to the commercial filaments. Advanced application of FTIR analysis confirmed the compatibility and miscibility of PEG with PLA. Conclusion:: Twin-screw extrusion is more effective in producing a polymeric mixture of filaments as the mixing is more homogenous. The PEG/PLA filament is suitable to be used in 3D printing of medical or pharmaceutical applications such as medical implants, drug delivery systems, or personalised tablets.

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1dcc1a5d2582f7b585b68f93a2d174b8Test
https://doi.org/10.2174/1567201817999201103195456Test

المؤلفون: Ahmad B. Albadarin, Javed Iqbal, Samuel Solomon

المصدر: European Journal of Pharmaceutics and Biopharmaceutics. 165:244-258

مصطلحات موضوعية: Materials science, Chemistry, Pharmaceutical, Drug Compounding, Pharmaceutical Science, 02 engineering and technology, 030226 pharmacology & pharmacy, Excipients, 03 medical and health sciences, 0302 clinical medicine, Drug Stability, medicine, Molecule, Solubility, Felodipine, Hot Melt Extrusion Technology, General Medicine, Mesoporous silica, Silicon Dioxide, 021001 nanoscience & nanotechnology, Amorphous solid, Drug Liberation, Chemical engineering, Solvents, Extrusion, 0210 nano-technology, Dispersion (chemistry), Ternary operation, Porosity, Biotechnology, medicine.drug

الوصف: In this work, the application of various mesoporous silica grades in the preparation of stabilized ternary amorphous solid dispersions of Felodipine using hot melt extrusion was explored. We have demonstrated the effectiveness of mesoporous silica in these dispersions without the need for any organic solvents i.e., no pre-loading or immersion steps required. The physical and chemical properties, release profiles of the prepared formulations and the surface concentrations of the various molecular species were investigated in detail. Formulations containing 25 wt% and 50 wt% of Felodipine demonstrated enhanced stability and solubility of the drug substance compared to its crystalline counterpart. Based on the Higuchi model, ternary formulations exhibited a 2-step or 3-step release pattern which can be ascribed to the release of drug molecules from the organic polymer matrix and the external silica surface, followed by a release from the silica pore structure. According to the Korsmeyer-Peppas model, the release rate and release mechanism are governed by a complex quasi-Fickian release mechanism, in which multiple release mechanisms are occurring concurrently and consequently. Stability studies indicated that after 6 months storage of all formulation at 30% RH and 20 oC, Felodipine in all formulations remained stable in its amorphous state except for the formulation comprised of 40 wt% Syloid AL-1FP with a 50 wt% drug load.

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8257bcdc5a29168b459509c0b841fb93Test
https://doi.org/10.1016/j.ejpb.2021.04.017Test

المؤلفون: Arvind, Bagde, Emmanual, Kouagou, Mandip, Singh

المصدر: AAPS PharmSciTech

مصطلحات موضوعية: Drug Carriers, Ecology, Anti-Inflammatory Agents, Hot Melt Extrusion Technology, Pharmaceutical Science, General Medicine, Aquatic Science, Article, Rats, Flurbiprofen, Liposomes, Drug Discovery, Animals, Nanoparticles, Gels, Agronomy and Crop Science, Ecology, Evolution, Behavior and Systematics

الوصف: Hot melt extrusion (HME) has been used for the formulation of topical solid lipid nanoparticle (SLN) gel without using any other size reduction technique including high pressure homogenization or sonication. SLN formulation solely using HME has not been applied to other drugs except IBU. Therefore, the purpose of the present study was to formulate FLB SLN solely using HME technique and evaluate the SLN formulation in inflammation animal model. Stable 0.5% w/v FLB SLN gel with particle size < 250 nm, PI < 0.3 and EE of > 98% was prepared. Differential scanning calorimetry (DSC) thermogram showed that the drug was converted to amorphous form in the HME process. Additionally, rheological studies demonstrated that FLB SLN gel and marketed FLB gel showed shear thinning property. FLB SLN formulation showed significantly (p < 0.05) higher peak force required to spread the formulation as compared to marketed FLB formulation. Stability studies showed that FLB SLN gel was stable for a month at room temperature and 2–4°C. Moreover, in vitro permeation test (IVPT) and ex vivo skin deposition study results revealed that FLB SLN gel showed significant (p < 0.05) increase in drug deposition in dermal layer and drug permeation as compared to control marketed formulation. Further, in vivo anti-inflammatory study showed equivalent inhibition of rat paw edema using 0.5% w/v FLB SLN gel which has 10 times less strength compared to control formulation. Overall, FLB SLN formulation was successfully manufactured solely using HME technique which resulted in enhanced the skin permeation of FLB and superior anti-inflammatory activity.

الوصول الحر: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c9b1e347ac493af4c2e23a583059914aTest
https://doi.org/10.1208/s12249-022-02410-wTest