scholarly journals Supercritical Carbon Dioxide as a Green Alternative to Achieve Drug Complexation with Cyclodextrins

2021 ◽  
Vol 14 (6) ◽  
pp. 562
Author(s):  
Mauro Banchero
Keyword(s):  
Release Kinetics ◽  
Drug Bioavailability ◽  
Residual Content ◽  
Supercritical Solvent ◽  
Cyclodextrin Complexation ◽  
Supercritical Fluid Technology ◽  
Conventional Drug ◽  
Size And Morphology ◽  
Solvent Residue ◽  
Complexation Mechanism

Cyclodextrins are widely used in pharmaceutics to enhance the bioavailability of many drugs. Conventional drug/cyclodextrin complexation techniques suffer from many drawbacks, such as a high residual content of toxic solvents in the formulations, the degradation of heat labile drugs and the difficulty in controlling the size and morphology of the product particles. These can be overcome by supercritical fluid technology thanks to the outstanding properties of supercritical CO2 (scCO2) such as its mild critical point, its tunable solvent power, and the absence of solvent residue after depressurization. In this work the use of scCO2 as an unconventional medium to achieve the complexation with native and substituted cyclodextrins of over 50 drugs, which belong to different classes, are reviewed. This can be achieved with different approaches such as the “supercritical solvent impregnation” and “particle-formation” techniques. The different techniques are discussed to point out how they affect the complexation mechanism and efficiency, the physical state of the drug as well as the particle size distribution and morphology, which finally condition the release kinetics and drug bioavailability. When applicable, the results obtained for the same drug with various cyclodextrins, or different complexation techniques are compared with those obtained with conventional approaches.

scholarly journals Synthesis and Characterization of a Fe3O4@PNIPAM-Chitosan Nanocomposite and Its Potential Application in Vincristine Delivery

Polymers ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1704
Author(s):  
Cynthia N. Hernández-Téllez ◽  
Ana G. Luque-Alcaraz ◽  
Maribel Plascencia-Jatomea ◽  
Hiram J. Higuera-Valenzuela ◽  
Mabeth Burgos-Hernández ◽  
...  
Keyword(s):  
Fe3o4 Nanoparticles ◽  
Release Kinetics ◽  
Magnetic Core ◽  
Systematic Evaluation ◽  
Solution Temperature ◽  
Core Shell ◽  
Particle Size And Morphology ◽  
Size And Morphology ◽  
Thermomagnetic Properties ◽  
Release Model

In this research, we conducted a systematic evaluation of the synthesis parameters of a multi-responsive core-shell nanocomposite (Fe3O4 nanoparticles coated by poly(N-isopropylacrylamide) (PNIPAM) in the presence of chitosan (CS) (Fe3O4@PNIPAM-CS). Scanning electron microscopy (SEM) was used to follow the size and morphology of the nanocomposite. The functionalization and the coating of Fe3O4 nanoparticles (Nps) were evaluated by the ζ-potential evolution and Fourier Transform infrared spectroscopy (FTIR). The nanocomposite exhibited a collapsed structure when the temperature was driven above the lower critical solution temperature (LCST), determined by dynamic light scattering (DLS). The LCST was successfully shifted from 33 to 39 °C, which opens the possibility of using it in physiological systems. A magnetometry test was performed to confirm the superparamagnetic behavior at room temperature. The obtained systems allow the possibility to control specific properties, such as particle size and morphology. Finally, we performed vincristine sulfate loading and release tests. Mathematical analysis reveals a two-stage structural-relaxation release model beyond the LCST. In contrast, a temperature of 25 °C promotes the diffusional release model. As a result, a more in-depth comprehension of the release kinetics was achieved. The synthesis and study of a magnetic core-shell nanoplatform offer a smart material as an alternative targeted release therapy due to its thermomagnetic properties.

scholarly journals Application of Supercritical Solvent Impregnation for Production of Zeolite Modified Starch-Chitosan Polymers with Antibacterial Properties

Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4717 ◽  
Author(s):  
Jelena Pajnik ◽  
Ivana Lukić ◽  
Jelena Dikić ◽  
Jelena Asanin ◽  
Milan Gordic ◽  
...  
Keyword(s):  
Release Kinetics ◽  
Antibacterial Properties ◽  
Water Vapor Permeability ◽  
Weibull Model ◽  
Vapor Permeability ◽  
E Coli ◽  
Supercritical Solvent ◽  
Composite Polymers ◽  
Before And After ◽  
Impregnation Time

In the present study, supercritical solvent impregnation (SSI) has been applied to incorporate thymol into bio-composite polymers as a potential active packaging material. Thymol, a natural component with a proven antimicrobial activity, was successfully impregnated into starch-chitosan (SC) and starch-chitosan-zeolite (SCZ) films using supercritical carbon dioxide (scCO2) as a solvent. Experiments were performed at 35 °C, pressures of 15.5 and 30 MPa, and an impregnation time in the range of 4–24 h. The highest impregnation yields of SC films with starch to chitosan mass ratios of 1:1 and 1:2 were 10.80% and 6.48%, respectively. The addition of natural zeolite (15–60%) significantly increased the loading capacity of films enabling thymol incorporation in a quantity of 16.7–27.3%. FTIR and SEM analyses were applied for the characterization of the films. Mechanical properties and water vapor permeability of films before and after the impregnation were tested as well. Thymol release kinetics in deionized water was followed and modeled by the Korsmeyer-Peppas and Weibull model. SCZ films with thymol loading of approximately 24% exhibited strong antibacterial activity against E. coli and methicillin-resistant Staphylococcus (S.) aureus (MRSA).

scholarly journals Targeted Drug Delivery Systems for the Treatment of Glaucoma: Most Advanced Systems Review

Polymers ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 1742 ◽  
Author(s):  
Olga Cegielska ◽  
Paweł Sajkiewicz
Keyword(s):  
Drug Delivery ◽  
Side Effects ◽  
Targeted Delivery ◽  
Drug Targets ◽  
Drug Delivery Systems ◽  
Release Kinetics ◽  
Controlled Drug Release ◽  
Drug Carriers ◽  
Delivery Systems ◽  
Drug Bioavailability

Each year, new glaucoma drug delivery systems are developed. Due to the chronic nature of the disease, it requires the inconvenient daily administration of medications. As a result of their elution from the eye surface and penetration to the bloodstream through undesired permeation routes, the bioavailability of active compounds is low, and systemic side effects occur. Despite numerous publications on glaucoma drug carriers of controlled drug release kinetics, only part of them consider drug permeation routes and, thus, carriers’ location, as an important factor affecting drug delivery. In this paper, we try to demonstrate the importance of the delivery proximal to glaucoma drug targets. The targeted delivery can significantly improve drug bioavailability, reduce side effects, and increase patients’ compliance compared to both commercial and scientifically developed formulations that can spread over the eye surface or stay in contact with conjunctival sac. We present a selection of glaucoma drug carriers intended to be placed on cornea or injected into the aqueous humor and that have been made by advanced materials using hi-tech forming methods, allowing for effective and convenient sustained antiglaucoma drug delivery.

scholarly journals Hydroxyl Ethyl Cellulose HHX and Polymethyl Methacrylate Based Site Specific Floating Delivery of Prochlorperazine Maleate

2016 ◽  
Vol 3 (1) ◽  
pp. 149-163
Author(s):  
Swati C. Jagdale ◽  
Aleesha B. Randhave
Keyword(s):  
Polymethyl Methacrylate ◽  
Release Kinetics ◽  
Hydroxyethyl Cellulose ◽  
Absolute Bioavailability ◽  
Drug Bioavailability ◽  
Compression Technique ◽  
Site Specific ◽  
Floating Drug Delivery

Background:Prochlorperazine maleate is a phenothiazine antipsychotic used principally in the treatment of nausea, vomiting and vertigo. Biological half- life of the drug is about 6 to 8 hrs and oral dose is 5 or 10 mg thrice or four times a day. The mean absolute bioavailability for drug is 12.5%. Due to the solubility of drug in acidic pH, it is mainly absorbed from stomach.Objective:Site specific oral floating delivery of prochlorperazine maleate will prolong the gastric retention time, increases the drug bioavailability, reduces frequency of administration and can result in better patient compliance.Method:The tablets were prepared by direct compression technique. Floating drug delivery was developed using gas forming agent and release retarding agenti.e.hydroxyethyl cellulose HHX (Natrosol HHX) and polymethyl methacrylate (PMMA). 32full factorial design was used for optimization. Prepared tablets were evaluated for pre and post compression parameters.Results:From the factorial batches it was observed that formulation containing 68.5% of hydroxyethyl cellulose HHX and 15% of polymethyl methacrylate had shown a drug release of 91.56 ± 2.7% with floating upto 10 hrs following Korsmeyer Peppas release kinetics.Conclusion:In- vivoplacebo X-ray study for optimized batch F6 had shown good gastroretention ability for 6 ± 0.5 hrs.In- vitroandin- vivostudy confirmed the site specific floating delivery for drug.

Modulation of Shape and Size-Dependent Characteristics of Nanoparticles

2019 ◽  
Vol 9 (3) ◽  
pp. 210-215
Author(s):  
Rashmi Sharma ◽  
Pramod K. Sharma ◽  
Rishabha Malviya
Keyword(s):  
Cellular Uptake ◽  
Half Life ◽  
Release Kinetics ◽  
Spherical Shape ◽  
Oral Drug ◽  
Cubic Phase ◽  
Drug Bioavailability ◽  
Size And Shape ◽  
Shape And Size

Background: Nanoparticles have considerably been studied for biomedical applications which include biosensing, bioimaging diagnostics, etc. but the effect of shape and size on the nanoparticles has received little attention. The execution of nanoparticles is affected by various factors such as size, shape, surface charge, etc. Objective: In this manuscript, the effects of nanoparticles size and shape on cellular uptake, biodistribution, and half-life of nanoparticles are discussed. The shape of nanoparticles affects the biodistribution, cellular uptake, adhesion strength, half-life circulation, and drug release kinetics and drug clearance. Methods and Results: The shape of the particles enhances the distribution ratio. Particles with a different shape such as spherical shape particles, improve oral drug bioavailability. Rod-like structure of particles showed more specific uptake and less nonspecific uptake in cells related to sphere particles. The size of the particles also affects the binding properties to the receptor and the enthalpic and entropic properties to control the adhesive strength in nanoparticles. Maximum in vitro cellular uptake showed a 10-60nm size range. Nanoparticles that are more than 100nm in size have the ability to penetrate through leaky vasculature into tumors. The size of the nanoparticles affects the biological fate and the large size particles are accumulated in the liver and spleen. Conclusion: The present manuscript specifically deals with the nanocarrier formulation such as cubosomes and hexasomes. The nanoparticles shape has an impact on hydrodynamics significantly and interfaces of vascular targeting. Due to the small particle size of the cubosomes nanoparticles, the cubic phase is more appropriate for the controlled release drug delivery system. It can be concluded from the findings of the literature survey that the size and shape of nanocarriers have a significant effect on pharmaceutical and biomedical adaptation.

scholarly journals A REVIEW ON NANOSPONGES A REVIEW ON NANOSPONGES: A BOON TO TARGETED DRUG DELIVERY FOR ANTICANCER DRUG

2019 ◽  
pp. 1-7
Author(s):  
NIKITA SEHGAL ◽  
VISHAL GUPTA N ◽  
SANDEEP KANNA
Keyword(s):  
Drug Delivery ◽  
Health Care ◽  
Cancer Treatment ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Delivery Systems ◽  
New Drugs ◽  
Stimuli Responsive ◽  
Drug Bioavailability ◽  
Conventional Drug

In recent decades, the rise in the investigation of new drugs had made health-care system expensive compared to conventional drug delivery systems and techniques. The present drug delivery systems have become highly productive and are growing fast. Majority of the anticancer agent has low water solubility resulting in multistep synthetic routes that require higher selectivity and specificity that can cause difficulty in the development of the formulation. Nanosponges (NSs) are branched cyclodextrin (CD) polymeric systems which have proven to be a boon in the pharmaceutical and biomedical fields. Different kinds of NSs based on different types of CDs and crosslinkers are used for developing of new drug formulations from the past few years for various applications in health care. Nanotechnology has overcome the issues regarding the drug solubility, stability, and other parameters and has attained success in achieving of sustained release, increased activity, improved permeability, delivery of nucleoprotein, the stimuli-responsive release of the drug, and improved drug bioavailability. There is a huge eruption of research on NSs for cancer treatment. Multiple anticancer moieties have been developed, taking into account the pharmacological and physicochemical perspective of the drug to develop a NS formulation. Our target in this review is to catch an efficient and far-reaching NSs for malignancy cancer treatment announced until now. This survey will give a perfect stage for providing details for researchers taking a shot at using new polymers for improving the treatment of the disease using nanotechnology. The present article provides details regarding antineoplastic molecules and provides ideas on CD-based NSs specifically using curcumin, tamoxifen, resveratrol, quercetin, oxygen-NSs, temozolomide, doxorubicin, and 5-fluorouracil (5-FU), and erlotinib (ETB) glutathione.

scholarly journals FORMULATION, CHARACTERIZATION AND IN VITRO EVALUATION OF FLOATING MICROSPHERES OF MEBENDAZOLE AS A GASTRO RETENTIVE DOSAGE FORM

2018 ◽  
Vol 8 (5-s) ◽  
pp. 311-314
Author(s):  
Lokesh Parmar ◽  
Mansi Gupta ◽  
Geeta Parkhe
Keyword(s):  
Ethyl Cellulose ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Entrapment Efficiency ◽  
Drug Bioavailability ◽  
Evaporation Method ◽  
Solvent Diffusion ◽  
Model Drug

The present study involves preparation and evaluation of floating microspheres using Mebendazole (MBZ) as a model drug for improving the drug bioavailability by prolongation of gastric retention time.  Ethyl cellulose, hydroxyl propyl methyl cellulose microspheres loaded with mebendazole were prepared by solvent diffusion evaporation method. The microspheres had smooth surfaces, with free-flowing and good-packing properties. The yield of the microspheres was up to 85.65±0.14% and ethyl cellulose microspheres entrapped the maximum amount of the drug. Scanning electron microscopy confirmed their hollow structures with sizes in the range 215.1 to 251.80 nm. The prepared microspheres exhibited prolonged drug release and Percentage buoyancy was found to70.25±0.15. The formulated batches were evaluated for percentage yield, particle size measurement, flow properties, percent entrapment efficiency, swelling studies. The formulations were subjected to Stability studies and In-vitro release and Release kinetics data was subjected to different dissolution models. Keywords: solvent diffusion evaporation method, Mebendazole, Ethyl cellulose, Hydroxyl propyl methyl cellulose

Physicochemical investigation and molecular modeling of cyclodextrin complexation mechanism with eugenol

2009 ◽  
Vol 42 (8) ◽  
pp. 1178-1185 ◽  
Author(s):  
Onanong Nuchuchua ◽  
Somsak Saesoo ◽  
Issara Sramala ◽  
Satit Puttipipatkhachorn ◽  
Apinan Soottitantawat ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Cyclodextrin Complexation ◽  
Physicochemical Investigation ◽  
Complexation Mechanism

Supercritical Solvent Impregnation in Controlled-Release Drugs

2010 ◽  
Vol 152-153 ◽  
pp. 1462-1465
Author(s):  
Zhen Tian ◽  
Nai Ci Bing ◽  
Ye Zhang ◽  
Ling Ling Wang ◽  
Wei Qiao
Keyword(s):  
Controlled Release ◽  
Organic Solvents ◽  
Supercritical Fluid ◽  
Supercritical Fluids ◽  
Elevated Temperatures ◽  
Amorphous Polymers ◽  
Bioactive Molecules ◽  
Supercritical Solvent ◽  
Supercritical Fluid Technology ◽  
Toxic Organic Solvents

In the field of pharmaceutical industry, the controlled-release drugs have received considerable attention in the last years. Impregnation using supercritical fluid technology has already proven its feasibility in the preparation of controlled release systems. The use of supercritical fluids such as supercritical CO2 has provided a ‘clean’ and effective alternative to traditional methods of drug releasing and polymer processes. In particular, scCO2 has a number of unique properties that make it possible to process both bioactive molecules and amorphous polymers without using toxic organic solvents or elevated temperatures. A high purity product, free of residual solvents is obtained, since no organic solvents are involved in the impregnation process. Here, we review the advantages of supercritical fluid and the preparation of controlled-release drugs by supercritical solvent impregnation.

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