scholarly journals Electrospun 4th-Generation Solid Dispersions of Poorly Water-Soluble Drug Utilizing Two Different Processes

2018 ◽  
Vol 2018 ◽  
pp. 1-10 ◽  
Author(s):  
Zhu Zhang ◽  
Wenbing Li ◽  
Guanghua Wang ◽  
Yang-Lu Qu ◽  
Deng-Guang Yu
Keyword(s):  
Sustained Release ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Drug Sustained Release ◽  
Water Soluble Drugs ◽  
Effective Delivery ◽  
Polyethylene Glycol 1000 ◽  
Poorly Water Soluble

Different from traditional solid dispersion (SD) for improving the dissolution rates of poorly water-soluble drugs, the upgraded 4th SD was developed to furnish a drug sustained-release profile. In this work, two different kinds of 4th SDs were fabricated using two electrospinning processes. One is a ternary SD (nanofibers F2) that consisted of ethyl cellulose (EC), polyethylene glycol 1000 (PEG), and tamoxifen citrate (TAM) from a modified coaxial process, and the other is a binary SD (nanofibers F1) which is comprised of EC and TAM from a single-fluid blending process. Scanning electronic microscopic observations demonstrated that F2 (330±50 nm) showed a better quality than F1 (870±230 nm) in terms of size and size distribution although both of them had a smooth surface morphology and a cross section. X-ray diffraction patterns verified that both SDs were amorphous nanocomposites owing to the favorable secondary interactions among these components, as suggested from the results of FTIR. In vitro dissolution experiments indicated that F2 could furnish an improved drug sustained-release characteristics compared to F1, exhausting all the contained TAM and having weaker leveling-off late release. The molecular behaviors of drug sustained-release from the binary 4th SD were suggested. The protocols reported here paved an alternative way for developing novel functional nanomaterials for effective delivery of poorly water-soluble drugs.

scholarly journals Solubility enhancement of carvedilol using drug–drug cocrystallization with hydrochlorothiazide

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Shivarani Eesam ◽  
Jaswanth S. Bhandaru ◽  
Chandana Naliganti ◽  
Ravi Kumar Bobbala ◽  
Raghuram Rao Akkinepally
Keyword(s):  
Aqueous Solubility ◽  
Sem Analysis ◽  
Water Soluble ◽  
High Permeability ◽  
Poorly Water Soluble Drugs ◽  
Drug Discovery And Development ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Dissolution In Vitro

Abstract Background Increasing hydrophilicity of poorly water-soluble drugs is a major challenge in drug discovery and development. Cocrystallization is one of the techniques to enhance the hydrophilicity of such drugs. Carvedilol (CAR), a nonselective beta/alpha1 blocker, used in the treatment of mild to moderate congestive heart failure and hypertension, is classified under BCS class II with poor aqueous solubility and high permeability. Present work is an attempt to improve the solubility of CAR by preparing cocrystals using hydrochlorothiazide (HCT), a diuretic drug, as coformer. CAR-HCT (2:0.5) cocrystals were prepared by slurry conversion method and were characterized by DSC, PXRD, FTIR, Raman, and SEM analysis. The solubility, stability, and dissolution (in vitro) studies were conducted for the cocrystals. Results The formation of CAR-HCT cocrystals was confirmed based on melting point, DSC thermograms, PXRD data, FTIR and Raman spectra, and finally by SEM micrographs. The solubility of the prepared cocrystals was significantly enhanced (7.3 times), and the dissolution (in vitro) was improved by 2.7 times as compared to pure drug CAR. Further, these cocrystals were also found to be stable for 3 months (90 days). Conclusion It may be inferred that the drug–drug (CAR-HCT) cocrystallization enhances the solubility and dissolution rate of carvedilol significantly. Further, by combining HCT as coformer could well be beneficial pharmacologically too.

scholarly journals SOLID DISPERSIONS: RESUSCITATING ORAL DELIVERY OF HYDROPHOBIC DRUGS

2019 ◽  
pp. 213-217
Author(s):  
RUCHI AGRAWAL ◽  
ABID RAZA ◽  
OM PRAKASH PATEL
Keyword(s):  
Oral Delivery ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Future Trends ◽  
Hydrophobic Drugs ◽  
Poorly Water Soluble Drugs ◽  
Advantages And Disadvantages ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Viable Method

Objective: This review article explores solid dispersions (SDs) as one of the suitable approaches to formulate poorly water-soluble drugs. The objective of this review on SD techniques is to explore their utility as a feasible, simple, and economically viable method for augmentation of dissolution of hydrophobic drugs. Methods: Various types of SDs are classified and compared. Use of surfactants to stabilize the SDs and their potential advantages and disadvantages has been discussed. Different techniques for preparing and evaluating SDs are appraised along with discussions on scalability and industrial production. Review of the current research on SD along with future trends is also offered. Results: Based on the various researches, SDs offer an efficient means of improving bioavailability while concurrently contributing to lower toxicity and dose-reduction. Conclusion: Solid-dispersions have been and continue to be one of the key technologies for solving the issue of poor solubility for newer hydrophobic molecules which are being discovered. This would give a new lease of life for such drugs enabling them to be delivered in an effective way.

scholarly journals Insoluble Polymers in Solid Dispersions for Improving Bioavailability of Poorly Water-Soluble Drugs

Polymers ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 1679
Author(s):  
Thao T.D. Tran ◽  
Phuong H.L. Tran
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Insoluble Polymers

In recent decades, solid dispersions have been demonstrated as an effective approach for improving the bioavailability of poorly water-soluble drugs, as have solid dispersion techniques that include the application of nanotechnology. Many studies have reported on the ability to change drug crystallinity and molecular interactions to enhance the dissolution rate of solid dispersions using hydrophilic carriers. However, numerous studies have indicated that insoluble carriers are also promising excipients in solid dispersions. In this report, an overview of solid dispersion strategies involving insoluble carriers has been provided. In addition to the role of solubility and dissolution enhancement, the perspectives of the use of these polymers in controlled release solid dispersions have been classified and discussed. Moreover, the compatibility between methods and carriers and between drug and carrier is mentioned. In general, this report on solid dispersions using insoluble carriers could provide a specific approach and/or a selection of these polymers for further formulation development and clinical applications.

Solubilisation of poorly water-soluble drugs during in vitro lipolysis of medium- and long-chain triacylglycerols

2004 ◽  
Vol 23 (3) ◽  
pp. 287-296 ◽  
Author(s):  
Janne Ørskov Christensen ◽  
Kirsten Schultz ◽  
Birgitte Mollgaard ◽  
Henning Gjelstrup Kristensen ◽  
Anette Mullertz
Keyword(s):  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
In Vitro Lipolysis ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Long Chain

scholarly journals NOVEL APPLICATION OF MIXED HYDROTROPIC SOLUBILIZATION TECHNIQUE IN THE FORMULATION AND EVALUATION OF SOLID DISPERSION OF FLUPIRTINE MALEATE

2018 ◽  
Vol 8 (5) ◽  
pp. 481-488
Author(s):  
Nisha Kumari Yadav ◽  
Tripti Shukla ◽  
Neeraj Upmanyu ◽  
Sharad Prakash Pandey ◽  
Mohammad Azaz Khan
Keyword(s):  
Particle Size ◽  
Solid Dispersion ◽  
Sodium Benzoate ◽  
Oral Bioavailability ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Evaporation Technique ◽  
Poorly Water Soluble

Flupirtine is an amino pyridine derivative that functions as a centrally acting non-opioid, non-steroidal analgesic. It is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties. Its muscle relaxant properties make it popular for back pain and other orthopedics uses. In the present investigation, recently developed mixed hydrotropic solid dispersion technology precludes the use of organic solvent and also decreases the individual concentration of hydrotropic agents, simultaneously decreasing their toxic potential. Mixed-hydrotropic solubilisation technique is the experience to increase the solubility of poorly water soluble drugs in the aqueous solution containing blends of hydrotropic agents, which may give synergistic enhancement effect on solubility of poorly water-soluble drugs and to reduce concentrations of each individual hydrotropic agent to minimize their toxic effects due to high concentration of hydrotropic agents. The Flupirtine loaded solid dispersion was prepared by a solvent evaporation technique using sodium benzoate and a niacinamide hydrotropic mixture. The prepared solid dispersions were valuated regarding their solubility, mean particle size, in-vitro drug release. The prepared solid dispersions were found very stable (chemically). The superior dissolution rate due to its reduced particle size may have contributed to the increased oral bioavailability. This study demonstrated that mixed-solvency may be an alternative approach for poorly soluble drugs to improve their solubility and oral bioavailability. Keywords: Flupirtine, Solid dispersion, Mixed-hydrotropic solubilisation, Solvent evaporation technique, Sodium benzoate, Niacinamide

scholarly journals A Review on Solid Dispersion and Carriers Used Therein for Solubility Enhancement of Poorly Water Soluble Drugs

2020 ◽  
Vol 10 (3) ◽  
pp. 359-369
Author(s):  
Avinash Ramrao Tekade ◽  
Jyoti Narayan Yadav
Keyword(s):  
Recent Trend ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Immediate Release ◽  
Water Soluble ◽  
Amorphous Solid Dispersions ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Enhanced Properties

A large number of hydrophilic and hydrophobic carriers in pharmaceutical excipients are available today which are used for formulation of solid dispersions. Depending on nature of carriers the immediate release solid dispersions and/or controlled release solid dispersions can be formulated. Initially crystalline carriers were used which are transformed into amorphous solid dispersions with enhanced properties. The carriers used previously were mostly synthetic one. Recent trend towards the use of natural carriers have replaced the use of synthetic carriers. This review is the overview of various synthetic, natural, semisynthetic, modified natural hydrophilic carriers used for formulation of solid dispersions.

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