scholarly journals Cyclodextrin-based nanosponges as drug carriers

2012 ◽  
Vol 8 ◽  
pp. 2091-2099 ◽  
Author(s):  
Francesco Trotta ◽  
Marco Zanetti ◽  
Roberta Cavalli
Keyword(s):  
Release Kinetics ◽  
Three Dimensional ◽  
Spherical Shape ◽  
Aqueous Solubility ◽  
Drug Carriers ◽  
Amorphous Structure ◽  
Water Soluble ◽  
Prolonged Release ◽  
Innovative Drug ◽  
Swelling Properties

Cyclodextrin-based nanosponges, which are proposed as a new nanosized delivery system, are innovative cross-linked cyclodextrin polymers nanostructured within a three-dimensional network. This type of cyclodextrin polymer can form porous insoluble nanoparticles with a crystalline or amorphous structure and spherical shape or swelling properties. The polarity and dimension of the polymer mesh can be easily tuned by varying the type of cross-linker and degree of cross-linking. Nanosponge functionalisation for site-specific targeting can be achieved by conjugating various ligands on their surface. They are a safe and biodegradable material with negligible toxicity on cell cultures and are well-tolerated after injection in mice. Cyclodextrin-based nanosponges can form complexes with different types of lipophilic or hydrophilic molecules. The release of the entrapped molecules can be varied by modifying the structure to achieve prolonged release kinetics or a faster release. The nanosponges could be used to improve the aqueous solubility of poorly water-soluble molecules, protect degradable substances, obtain sustained delivery systems or design innovative drug carriers for nanomedicine.

scholarly journals Supercritical carbon dioxide design strategies: from drug carriers to soft killers

2015 ◽  
Vol 373 (2057) ◽  
pp. 20150009 ◽  
Author(s):  
Ana Aguiar-Ricardo ◽  
Vasco D. B. Bonifácio ◽  
Teresa Casimiro ◽  
Vanessa G. Correia
Keyword(s):  
Carbon Dioxide ◽  
Supercritical Carbon Dioxide ◽  
Three Dimensional ◽  
Polymeric Materials ◽  
Drug Carriers ◽  
Water Soluble ◽  
Materials Processing ◽  
Design Strategies ◽  
Simple Economic ◽  
Supercritical Carbon

The integrated use of supercritical carbon dioxide (scCO 2 ) and micro- and nanotechnologies has enabled new sustainable strategies for the manufacturing of new medications. ‘Green’ scCO 2 -based methodologies are well suited to improve either the synthesis or materials processing leading to the assembly of three-dimensional multifunctional constructs. By using scCO 2 either as C1 feedstock or as solvent, simple, economic, efficient and clean routes can be designed to synthesize materials with unique properties such as polyurea dendrimers and oxazoline-based polymers/oligomers. These new biocompatible, biodegradable and water-soluble polymeric materials can be engineered into multifunctional constructs with antimicrobial activity, targeting moieties, labelling units and/or efficiently loaded with therapeutics. This mini-review highlights the particular features exhibited by these materials resulting directly from the followed supercritical routes.

scholarly journals Improved Dissolution of Albendazole from High Drug Loaded Ternary Solid Dispersion: Formulation and Characterization

2021 ◽  
Vol 20 (2) ◽  
pp. 149-158
Author(s):  
Shimul Halder ◽  
MAK Azad ◽  
Hrishik Iqbal ◽  
Madhabi Lata Shuma ◽  
Eva Rahman Kabir
Keyword(s):  
Solid Dispersion ◽  
Drug Loading ◽  
Aqueous Solubility ◽  
Drug Carriers ◽  
Physicochemical Characteristics ◽  
Water Soluble ◽  
Dissolution Behavior ◽  
Scanning Calorimetry ◽  
High Drug ◽  
Enhanced Solubility

Bioavailability of a poorly water-soluble drug, e.g., widely used anthelmintic drug Albendazole (ABZ), is very low and thus, to obtain an optimized therapeutic efficacy, the aqueous solubility of such drugs needs to be enhanced. The objective of this study was to develop an effective high drug-loaded solid dispersion (SD) of ABZ with two biocompatible drug carriers, namely Soluplus® and Ludiflash® to improve its physicochemical characteristics. Equilibrium solubility study was performed to choose the optimum polymer ratio among the formulations and it showed up to 50-fold enhanced solubility compared to crystalline ABZ in water. X-Ray Powder Diffraction (XRPD) and Differential Scanning Calorimetry (DSC) studies of SD-ABZ showed reduced crystallinity of ABZ in the SD. The polymeric carriers, notably Soluplus®, are thought to play a key role in the reduction of crystallinity and molecular polydispersity of ABZ. The dissolution studies in water showed improved dissolution of SD-ABZ compared to crystalline ABZ, with a quick onset of drug release followed by gradual dissolution. However, due to high drug-loading and retention of crystalline ABZ in the sample, the dissolution behavior was not as expected, and may require further studies to optimize the SD-ABZ formulation. Dhaka Univ. J. Pharm. Sci. 20(2): 149-158, 2021 (December)

scholarly journals Acid-Treated Water-Soluble Chitosan Suitable for Microneedle-Assisted Intracutaneous Drug Delivery

Pharmaceutics ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 209 ◽  
Author(s):  
Ajeesh Chandrasekharan ◽  
Young Jun Hwang ◽  
Keum-Yong Seong ◽  
Samdae Park ◽  
Sodam Kim ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Transdermal Drug Delivery ◽  
Release Kinetics ◽  
Water Soluble ◽  
Prolonged Release ◽  
Molding Process ◽  
Diverse Range ◽  
Neutral Ph ◽  
Drug Delivery Carrier ◽  
Bioactive Agents

Chitosan has been widely used as a nature-derived polymeric biomaterial due to its high biocompatibility and abundance. However, poor solubility in aqueous solutions of neutral pH and multiple fabrication steps for the molding process limit its application to microneedle technology as a drug delivery carrier. Here, we present a facile method to prepare water-soluble chitosan and its application for sustained transdermal drug delivery. The water-soluble chitosan was prepared by acid hydrolysis using trifluoroacetic acid followed by dialysis in 0.1 M NaCl solutions. We successfully fabricated bullet-shaped microneedle (MN) arrays by the single molding process with neutral aqueous chitosan solutions (pH 6.0). The chitosan MN showed sufficient mechanical properties for skin insertion and, interestingly, exhibited slow dissolving behavior in wet conditions, possibly resulting from a physical crosslinking of chitosan chains. Chitosan MN patches loading rhodamine B, a model hydrophilic drug, showed prolonged release kinetics in the course of the dissolving process for more than 72 h and they were found to be biocompatible to use. Since the water-soluble chitosan can be used for MN fabrication in the mild conditions (neutral pH and 25 °C) required for the loading of bioactive agents such as proteins and achieve a prolonged release, this biocompatible chitosan MN would be suitable for sustained transdermal drug delivery of a diverse range of drugs.

scholarly journals Antimicrobial Formulations of Absorbable Bone Substitute Materials as Drug Carriers Based on Calcium Sulfate

2016 ◽  
Vol 60 (7) ◽  
pp. 3897-3905 ◽  
Author(s):  
D. Pförringer ◽  
A. Obermeier ◽  
M. Kiokekli ◽  
H. Büchner ◽  
S. Vogt ◽  
...  
Keyword(s):  
Bone Substitute ◽  
Ex Vivo ◽  
Release Kinetics ◽  
Drug Carriers ◽  
Prolonged Release ◽  
Clinical Parameters ◽  
Bone Substitute Materials ◽  
Substitute Materials

ABSTRACTSubstitution of bones is a well-established, necessary procedure to treat bone defects in trauma and orthopedic surgeries. For prevention or treatment of perioperative infection, the implantation of resorbable bone substitute materials carrying antibiotics is a necessary treatment. In this study, we investigated the newly formulated calcium-based resorbable bone substitute materials containing either gentamicin (CaSO4-G [Herafill-G]), vancomycin (CaSO4-V), or tobramycin (Osteoset). We characterized the released antibiotic concentration per unit. Bone substitute materials were implanted in bones of rabbits via a standardized surgical procedure. Clinical parameters and levels of the antibiotic-releasing materials in serum were determined. Local concentrations of antibiotics were measured using antimicrobial tests of bone tissue. Aminoglycoside release kineticsin vitroper square millimeter of bead surface showed the most prolonged release for gentamicin, followed by vancomycin and, with the fastest release, tobramycin.In vivolevel in serum detected over 28 days was highest for gentamicin at 0.42 μg/ml, followed by vancomycin at 0.11 μg/ml and tobramycin at 0.04 μg/ml. The clinical parameters indicated high biocompatibility for materials used. None of the rabbits subjected to the procedure showed any adverse reaction. The highest availability of antibiotics at 14.8 μg/g on day 1 in the cortical tibiaex vivowas demonstrated for gentamicin, decreasing within 14 days. In the medulla, vancomycin showed a high level at 444 μg/g on day 1, decreasing continuously over 14 days, whereas gentamicin decreased faster within the initial 3 days. The compared antibiotic formulations varied significantly in release kinetics in serum as well as locally in medulla and cortex.

scholarly journals Novel Starch-PVA Polymer for Microparticle Preparation and Optimization Using Factorial Design Study

2015 ◽  
Vol 2015 ◽  
pp. 1-8
Author(s):  
Helen Chattopadhyay ◽  
Amit Kumar De ◽  
Sriparna Datta
Keyword(s):  
Polyvinyl Alcohol ◽  
Factorial Design ◽  
Microscopic Study ◽  
Targeted Delivery ◽  
Release Kinetics ◽  
Three Dimensional ◽  
Control Release ◽  
Spherical Shape ◽  
Drug Release Profile ◽  
Electron Microscopic

The aim of our present work was to optimize the ratio of a very novel polymer, starch-polyvinyl alcohol (PVA), for controlled delivery of Ornidazole. Polymer-coated drug microparticles were prepared by emulsion method. Microscopic study, scanning electron microscopic study, and atomic force microscopic study revealed that the microparticles were within 10 micrometers of size with smooth spherical shape. The Fourier transform infrared spectroscopy showed absence of drug polymer interaction. A statistical 32 full factorial design was used to study the effect of different concentration of starch and PVA on the drug release profile. The three-dimensional plots gave us an idea about the contribution of each factor on the release kinetics. Hence this novel polymer of starch and polyvinyl alcohol can be utilized for control release of the drug from a targeted delivery device.

scholarly journals Designing Functionalized Polyelectrolyte Microcapsules for Cancer Treatment

Nanomaterials ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 3055
Author(s):  
Daria Kalenichenko ◽  
Galina Nifontova ◽  
Alexander Karaulov ◽  
Alyona Sukhanova ◽  
Igor Nabiev
Keyword(s):  
Fluorescent Dyes ◽  
Malignant Tumors ◽  
Release Kinetics ◽  
Semiconductor Nanocrystals ◽  
Water Soluble ◽  
Particle Analysis ◽  
Prolonged Release ◽  
Polyelectrolyte Microcapsules ◽  
Tumor Tissues ◽  
Therapy And Diagnosis

The engineering of delivery systems for drugs and contrasting labels ensuring the simultaneous imaging and treatment of malignant tumors is an important hurdle in developing new tools for cancer therapy and diagnosis. Polyelectrolyte microcapsules (MCs), formed by nanosized interpolymer complexes, represent a promising platform for the designing of multipurpose agents, functionalized with various components, including high- and low-molecular-weight substances, metal nanoparticles, and organic fluorescent dyes. Here, we have developed size-homogenous MCs with different structures (core/shell and shell types) and microbeads containing doxorubicin (DOX) as a model anticancer drug, and fluorescent semiconductor nanocrystals (quantum dots, QDs) as fluorescent nanolabels. In this study, we suggest approaches to the encapsulation of DOX at different stages of the MC synthesis and describe the optimal conditions for the optical encoding of MCs with water-soluble QDs. The results of primary characterization of the designed microcarriers, including particle analysis, the efficacy of DOX and QDs encapsulation, and the drug release kinetics are reported. The polyelectrolyte MCs developed here ensure a modified (prolonged) release of DOX, under conditions close to normal and tumor tissues; they possess a bright fluorescence that paves the way to their exploitation for the delivery of antitumor drugs and fluorescence imaging.

scholarly journals Drug Carriers: Classification, Administration, Release Profiles, and Industrial Approach

Processes ◽  
2021 ◽  
Vol 9 (3) ◽  
pp. 470
Author(s):  
Paolo Trucillo
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Drug Carrier ◽  
Drug Carriers ◽  
Therapeutic Window ◽  
Innovative Drug ◽  
Administration Routes ◽  
Industrial Companies ◽  
Innovative Techniques ◽  
Carrier Systems

This work is aimed at providing a description of the complex world of drug carriers, starting from the description of this particular market in terms of revenue. Then, a brief overview of several types of conventional and innovative drug carrier systems has been included. The types of administration routes were also analyzed, with a critical and qualitative comment on drug release kinetics and drug profile shapes. Carriers were classified according to their ability to provide a prolonged and targeted release. The concept of the therapeutic window has been presented, providing advantages of having pulsed drug release to avoid side effects to target tissues. A critical comment on the use of conventional and innovative techniques for the production of drug carriers by large industrial companies has been proposed. As a final attempt for this work, an overall unique schematization of a drug carrier production process has been added, highlighting the necessity to create a strong double link among world-requested versatility of drug carriers for human applications and the newly developed industrial processes.

scholarly journals Fullerenols as a New Therapeutic Approach in Nanomedicine

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Jacek Grebowski ◽  
Paulina Kazmierska ◽  
Anita Krokosz
Keyword(s):  
Oxidative Stress ◽  
Free Radicals ◽  
Neurodegenerative Diseases ◽  
Spherical Shape ◽  
Drug Carriers ◽  
Water Soluble ◽  
Alternative Methods ◽  
Negative Effects ◽  
Anthracycline Antibiotics ◽  
Systemic Oxidative Stress

Recently, much attention has been paid to the bioactive properties of water-soluble fullerene derivatives: fullerenols, with emphasis on their pro- and antioxidative properties. Due to their hydrophilic properties and the ability to scavenge free radicals, fullerenols may, in the future, provide a serious alternative to the currently used pharmacological methods in chemotherapy, treatment of neurodegenerative diseases, and radiobiology. Some of the most widely used drugs in chemotherapy are anthracycline antibiotics. Anthracycline therapy, in spite of its effective antitumor activity, induces systemic oxidative stress, which interferes with the effectiveness of the treatment and results in serious side effects. Fullerenols may counteract the harmful effects of anthracyclines by scavenging free radicals and thereby improve the effects of chemotherapy. Additionally, due to the hollow spherical shape, fullerenols may be used as drug carriers. Moreover, because of the existence of the currently ineffective ways for neurodegenerative diseases treatment, alternative compounds, which could prevent the negative effects of oxidative stress in the brain, are still sought. In the search of alternative methods of treatment and diagnosis, today’s science is increasingly reaching for tools in the field of nanomedicine, for example, fullerenes and their water-soluble derivatives, which is addressed in the present paper.

A Free Energy Perturbation Approach to Estimate the Intrinsic Solubilities of Drug-like Small Molecules

2019 ◽  
Author(s):  
Sayan Mondal ◽  
Gary Tresadern ◽  
Jeremy Greenwood ◽  
Byungchan Kim ◽  
Joe Kaus ◽  
...  
Keyword(s):  
Solid State ◽  
Small Molecules ◽  
Three Dimensional ◽  
Aqueous Solubility ◽  
Computational Approach ◽  
Free Energy Perturbation ◽  
Perturbation Approach ◽  
Energy Perturbation ◽  
State Form ◽  
Good Agreement

<p>Optimizing the solubility of small molecules is important in a wide variety of contexts, including in drug discovery where the optimization of aqueous solubility is often crucial to achieve oral bioavailability. In such a context, solubility optimization cannot be successfully pursued by indiscriminate increases in polarity, which would likely reduce permeability and potency. Moreover, increasing polarity may not even improve solubility itself in many cases, if it stabilizes the solid-state form. Here we present a novel physics-based approach to predict the solubility of small molecules, that takes into account three-dimensional solid-state characteristics in addition to polarity. The calculated solubilities are in good agreement with experimental solubilities taken both from the literature as well as from several active pharmaceutical discovery projects. This computational approach enables strategies to optimize solubility by disrupting the three-dimensional solid-state packing of novel chemical matter, illustrated here for an active medicinal chemistry campaign.</p>

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

Sign in / Sign up

Export Citation Format

Share Document