scholarly journals Encapsulation of Flurbiprofen by Chitosan Using a Spray-Drying Method with In Vitro Drug Releasing and Molecular Docking

2017 ◽  
Vol 14 (1) ◽  
pp. 34-39 ◽  
Author(s):  
Lalehan AKYÜZ ◽  
Fatih DUMAN ◽  
Murat KAYA
Keyword(s):  
Molecular Docking ◽  
Spray Drying ◽  
Drying Method

scholarly journals In vitro and in vivo evaluation of sustained release ketoprofen-loaded nanoparticles

2013 ◽  
Vol 16 (1) ◽  
pp. 15-25
Author(s):  
Tuyen Thi Phuong Dao ◽  
Nhan Ngoc Thanh Le ◽  
Anh Tuan Nguyen ◽  
Khai Tan Tran ◽  
Dam Duy Le ◽  
...  
Keyword(s):  
Spray Drying ◽  
In Vitro Dissolution ◽  
Drying Method ◽  
In Vivo Evaluation ◽  
The Matrix ◽  
Nanoparticle Formulation ◽  
Electron Microscopes ◽  
Size And Morphology

The purpose of this study is to i) fabricate a biodegradable nanoparticle formulation of Ketoprofen, ii) evaluate its characteristics, iii) investigate its in vitro dissolution and in vivo pharmaceutical property. The nanoparticle formulation was prepared by spray drying method using Eudragit L100 as the matrix polymer. Size and morphology of drug-loaded nanoparticles were characterized with the electron microscopes (TEM, SEM). These successfully prepared nanoparticles by spray drying method are spherical in shape and quite homologous with diameter size of 100 – 200 nm. The in vitro dissolution studies were conducted at pH 1.2 and 7.4. The results indicated that there is a significant increase in Keto concentration at pH 7.4 compared to pH 1.2. For the in vivo assessment, our Keto-loaded nanoparticles and referential Profenid were administered by oral gavages to rabbits. The results implied that Keto-loadednanoparticles remarkably increased AUC compared to Profenid.

scholarly journals CURCUMIN MICROENCAPSULATION USING CHITOSAN–ETHYL CELLULOSE–GMS MIXTURE FOR PRESERVATION OF MUCOADHESIVE PROPERTIES AND CONTROLLED RELEASE KINETIC

2022 ◽  
pp. 288-294
Author(s):  
DENI RAHMAT ◽  
YUNAHARA FARIDA ◽  
NOVI YANTIH ◽  
GITA SEPTYANA DEWI ◽  
SARAH ANGELA PURNAMA
Keyword(s):  
Particle Size ◽  
Water Content ◽  
Spray Drying ◽  
Spherical Shape ◽  
Release Kinetic ◽  
Drying Method ◽  
Solid Dosage Forms ◽  
Solid Dosage ◽  
Better Than

Objective: This research aimed to prepare curcumin microcapsules by the spray drying method and to evaluate their characteristics. Methods: The microcapsules were prepared by the spray drying method. The generated microcapsules were evaluated for organoleptic, morphology, particle size, the percentage of curcumin and water content. Furthermore, the release of curcumin from the microcapsules was tested in vitro and compared to uncoated curcumin powder. In addition, the mucoadhesive properties of uncoated curcumin powder and curcumin microcapsules were also evaluated. Results: The results showed that the microcapsules had spherical shape with particle size in the range of 100–1009 µm and water content of 9.34% (w/w) (FIII) and 8.09% (w/w) (FVI). The release of curcumin from its uncoated powder and the microcapsules FVI within 8 h were 8.87% and 26.32% (w/w), respectively. It was found that the mucoadhesive properties of microcapsules FVI were better than those of FIII and uncoated curcumin powder. Microcapsules FVI rendered the cumulative amount of curcumin remaining on the intestinal mucosa of 55% (w/w) within 3 h. Conclusion: Accordingly, curcumin microcapsules generated by spray drying could be further formulated into various solid dosage forms for a better therapeutic effect.

scholarly journals Preparation and in Vitro Bioactivity of Micron-sized Bioactive Glass Particles Using Spray Drying Method

2018 ◽  
Vol 9 (1) ◽  
pp. 19 ◽  
Author(s):  
Yu-Jen Chou ◽  
Chih-Wei Hsiao ◽  
Nien-Ti Tsou ◽  
Meng-Huang Wu ◽  
Shao-Ju Shih
Keyword(s):  
Spray Drying ◽  
Glass Melting ◽  
Sol Gel ◽  
Synthetic Methods ◽  
Biological Applications ◽  
Drying Method ◽  
In Vitro Bioactivity ◽  
Bioactive Glasses ◽  
Spray Dried

In recent years, bioactive glasses (BGs) have attracted enormous attention with their superior bioactivity, non-toxicity and degradability. Owing to their properties, they have been applied in various biological applications. In the present work, we demonstrated that micron-sized BGs can be prepared with a spray drying method. This technique offers the advantages of low contamination and the ability of mass production, in contrast to the two major synthetic methods, conventional glass-melting and sol-gel, previously used for preparation of BGs. Characterizations of phase composition, morphology and specific surface area of spray dried BG powders were carried out and bioactivity was examined in vitro with respect to the ability to form a hydroxyapatite layer on the surface of the particles after they were immersed in simulated body fluid.

scholarly journals Influence of Sodium Alginate on Hypoglycemic Activity of Metformin Hydrochloride in the Microspheres Obtained by the Spray Drying

2016 ◽  
Vol 2016 ◽  
pp. 1-12 ◽  
Author(s):  
Marta Szekalska ◽  
Magdalena Wróblewska ◽  
Katarzyna Sosnowska ◽  
Katarzyna Winnicka
Keyword(s):  
Sodium Alginate ◽  
Spray Drying ◽  
Drug Loading ◽  
Release Profile ◽  
Hypoglycemic Activity ◽  
Metformin Hydrochloride ◽  
Drying Method ◽  
Alginate Concentration ◽  
Polymer Ratio

Alginate microspheres with metformin hydrochloride were prepared by the spray drying method in order to improve residence time of drug in the stomach. Nine formulations (F1–F9) with various drug : polymer ratio (1 : 2, 1 : 1, and 2 : 1) and different sodium alginate concentration (1%, 2%, and 3%) were evaluated for size, morphology, drug loading, Zeta potential, and swelling degree.In vitrodrug release, mathematical release profile, and physical state of microspheres were also evaluated. Optimal formulation characterized by the highest drug loading was formulation F6 (drug : polymer ratio 2 : 1 and 2% alginate solution). Based on glucose uptake inSaccharomyces cerevisiaecells andα-amylase inhibition tests, it could be concluded that alginate microspheres enhance hypoglycemic activity of metformin hydrochloride evaluatedin vitro. Designed microspheres are promising as alternative, multicompartment dosage form for metformin hydrochloride delivery.

Molecular Docking Approaches to Suggest the Anti-Mycobacterial Targets of Natural Products

2020 ◽  
Author(s):  
Rafael Baptista ◽  
Sumana Bhowmick ◽  
Shen Jianying ◽  
Luis Mur
Keyword(s):  
Natural Products ◽  
Molecular Docking ◽  
Free Energies ◽  
Antibiotic Resistant ◽  
Drug Lead ◽  
Bisbenzylisoquinoline Alkaloids ◽  
Docking Approach ◽  
Global Threat ◽  
Physicochemical And Structural Properties

Tuberculosis (TB) is a major global threat mostly due to the development of antibiotic resistant forms of Mycobacterium tuberculosis, the causal agent of the disease. Driven by the pressing need for new anti-mycobacterial agents, several natural products (NPs) have been shown to have in vitro activities against M. tuberculosis. The utility of any NP as a drug lead is augmented when the anti-mycobacterial target(s) is unknown. To suggest these, we used a molecular docking approach to predict the interactions of 53 selected anti-mycobacterial NPs against known ‘druggable’ mycobacterial targets ClpP1P2, DprE1, InhA, KasA, PanK, PknB and Pks13. The docking scores / binding free energies were predicted and calculated using AutoDock Vina along with physicochemical and structural properties of the NPs, using PaDEL descriptors. These were compared to the established inhibitor (control) drugs for each mycobacterial target. The specific interactions of the bisbenzylisoquinoline alkaloids 2-nortiliacorinine, tiliacorine and 13’-bromotiliacorinine against the targets PknB and DprE1 (-11.4, -10.9 and -9.8 kcal.mol-1 ; -12.7, -10.9 and -10.3 kcal.mol-1 , respectively) and the lignan αcubebin and Pks13 (-11.0 kcal.mol-1 ) had significantly superior docking scores compared to controls. Our approach can be used to suggest predicted targets for the NP to be validated experimentally but these in silico steps are likely to facilitate drug optimisation.

Moxifloxacin Hydrochloride-Loaded Eudragit® RL 100 and Kollidon® SR Based Nanoparticles: Formulation, In vitro Characterization and Cytotoxicity.

2020 ◽  
Vol 23 ◽  
Author(s):  
Gülsel Yurtdaş Kırımlıoğlu ◽  
Sinan Özer ◽  
Gülay Büyükköroğlu ◽  
Yasemin Yazan
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Spray Drying ◽  
Prolonged Release ◽  
Ocular Delivery ◽  
Corneal Permeability ◽  
Release Pattern ◽  
In Vitro Characterization ◽  
Ocular Bioavailability

Background: Considering the low ocular bioavailability of conventional formulations used for ocular bacterial infection treatment, there’s a need for designing efficient novel drug delivery systems that may enhance of precorneal retention time and corneal permeability. Aim and Objective: The current research focuses on developing nanosized and non-toxic Eudragit® RL 100 and Kollidon® SR nanoparticles loaded with moxifloxacin hydrochloride (MOX) for its prolonged release to be promising for effective ocular delivery. Methods: In this study, MOX was incorporation was carried out by spray drying method aiming ocular delivery. In vitro characteristics were evaluated in detail with different methods. Results: MOX was successfully incorporated into Eudragit® RL 100 and Kollidon® SR polymeric nanoparticles by spray-drying process. Particle size, zeta potential, entrapment efficiency, particle morphology, thermal, FTIR, XRD and NMR analyses and MOX quantification using HPLC method were carried out to evaluate the nanoparticles prepared. MOX loaded nanoparticles demonstrated nanosized and spherical shape while in vitro release studies demonstrated modified release pattern which followed Korsmeyer-Peppas kinetic model. Following successful incorporation of MOX into the nanoparticles, the formulation (MOX: Eudragit® RL 100, 1:5) (ERL-MOX 2) was selected for further studies by the reason of its better characteristics like cationic zeta potential, smaller particle size, narrow size distribution and more uniform prolonged release pattern. Moreover, ERL-MOX 2 formulation remained stable for 3 months and demonstrated higher cell viability values for MOX. Conclusion: In vitro characterization analyses showed that non-toxic, nano-sized and cationic ERLMOX 2 formulation has the potential of enhancing ocular bioavailability.

The Antiviral and Antimalarial Drug Repurposing in Quest of Chemotherapeutics to Combat COVID-19 Utilizing Structure-Based Molecular Docking

2020 ◽  
Vol 23 ◽  
Author(s):  
Sisir Nandi ◽  
Mohit Kumar ◽  
Mridula Saxena ◽  
Anil Kumar Saxena
Keyword(s):  
Molecular Docking ◽  
In Silico ◽  
Drug Repurposing ◽  
Clinical Settings ◽  
The Novel ◽  
In Silico Docking ◽  
Biochemical Mechanisms ◽  
Novel Coronavirus ◽  
In Silico Molecular Docking

Background: The novel coronavirus disease (COVID-19) is caused by a new strain (SARS-CoV-2) erupted in 2019. Nowadays, it is a great threat that claims uncountable lives worldwide. There is no specific chemotherapeutics developed yet to combat COVID-19. Therefore, scientists have been devoted in the quest of the medicine that can cure COVID- 19. Objective: Existing antivirals such as ASC09/ritonavir, lopinavir/ritonavir with or without umifenovir in combination with antimalarial chloroquine or hydroxychloroquine have been repurposed to fight the current coronavirus epidemic. But exact biochemical mechanisms of these drugs towards COVID-19 have not been discovered to date. Method: In-silico molecular docking can predict the mode of binding to sort out the existing chemotherapeutics having a potential affinity towards inhibition of the COVID-19 target. An attempt has been made in the present work to carry out docking analyses of 34 drugs including antivirals and antimalarials to explain explicitly the mode of interactions of these ligands towards the COVID-19protease target. Results: 13 compounds having good binding affinity have been predicted towards protease binding inhibition of COVID-19. Conclusion: Our in silico docking results have been confirmed by current reports from clinical settings through the citation of suitable experimental in vitro data available in the published literature.

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