scholarly journals Cyclodextrin Inclusion Complexes: Novel Techniques to Improve Solubility of Poorly Soluble Drugs: A Review

2016 ◽  
Vol I (I) ◽  
pp. 29-34
Author(s):  
Sobia Noreen ◽  
Irsah Maqbool ◽  
Muhammad Ijaz ◽  
Sairah Tanveer
Keyword(s):  
Inclusion Complexes ◽  
Aqueous Solubility ◽  
Complexing Agents ◽  
Dissolution Profile ◽  
Drug Candidates ◽  
Insoluble Drugs ◽  
Poorly Soluble ◽  
Poorly Soluble Drug ◽  
Technological Strategies ◽  
Crucial Test

For a formulation scientist, the dilemma of solubility is a crucial test during the product development phase that can be resolved by opting various technological strategies. Some of the strategies that are usually applied for enhancing solubility of drugs with low aqueous solubility include micronization, solvent deposition and solid dispersion. With these approaches, some advantages as well as drawbacks, are affiliated. The strategy of complexation amid all techniques, has been applied more accurately for the improvement of dissolution profile, aqueous solubility, and bioavailability of poorly soluble drug candidates. Cyclodextrin are unique cyclic carbohydrates that have been exploited as successful complexing agents having capability of forming inclusion complexes with insoluble drugs. Numerous strategies have been considered to analyze the methods for preparation of inclusion complexes. In this review, we have pursued the discussion on different complexation techniques and in a nutshell, emphasized the applications and economical/technical limitations related to these techniques.

scholarly journals Solubility EnhancementTechniques forPoorly Soluble Pharmaceuticals: A Review

2019 ◽  
Vol 7 (02) ◽  
pp. 09-16
Author(s):  
Jyoti Gupta ◽  
Anjana Devi
Keyword(s):  
Aqueous Solubility ◽  
Systemic Circulation ◽  
Peptic Ulcers ◽  
Drug Solubility ◽  
Formulation Development ◽  
Drug Candidates ◽  
Poorly Soluble ◽  
Poorly Soluble Drug ◽  
New Formulation ◽  
Rate Limiting

Among newly discovered chemical entities about 40% drugs are hydrophobic which are failed to reach market due to their low aqueous solubility. For orally administered drugs solubility is one of the rate limiting parameter to achieve their desired concentration in systemic circulation for pharmacological response.Drug efficacy can be limited due to poor aqueous solubility and some drugs also show side effects like gastric irritation, peptic ulcers,due to their poor solubility. Because of solubility problem of many drugs the bioavailability of them gets affected and hence solubility enhancement becomes challenging. The present review is devoted to various traditional and novel techniques for enhancing drug solubility to reduce the percentage of poorly soluble drug candidates eliminated from the new formulation development.

Studies on the Preparation, Characterization and Solubility of -Cyclodextrin-Roxythromycin Inclusion Complexes

2009 ◽  
Vol 2 (2) ◽  
pp. 523-530
Author(s):  
D. Nagasamy Venkatesh ◽  
S. Karthick ◽  
M. Umesh ◽  
G. Vivek ◽  
R.M. Valliappan ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Phase Solubility ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Ir Studies ◽  
Poorly Soluble ◽  
Poorly Soluble Drug

Roxythromycin/ β-cyclodextrin (Roxy/ β-CD) dispersions were prepared with a view to study the influence of β-CD on the solubility and dissolution rate of this poorly soluble drug. Phase-solubility profile indicated that the solubility of roxythromycin was significantly increased in the presence of β-cyclodextrin and was classified as AL-type, indicating the 1:1 stoichiometric inclusion complexes. Physical characterization of the prepared systems was carried out by differential scanning calorimetry (DSC), X-ray diffraction studies (XRD) and IR studies. Solid state characterization of the drug β-CD binary system using XRD, FTIR and DSC revealed distinct loss of drug crystallinity in the formulation, ostensibly accounting for enhancement of dissolution rate.

scholarly journals Physicochemical characterization and in vitro dissolution behaviour of celecoxib-β-cyclodextrin inclusion complexes

2007 ◽  
Vol 57 (1) ◽  
pp. 47-60 ◽  
Author(s):  
Vivek Sinha ◽  
R. Anitha ◽  
Soma Ghosh ◽  
Rachana Kumria ◽  
Jayant Bhinge ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Physicochemical Characterization ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Cyclodextrin Inclusion Complexes ◽  
Cyclodextrin Inclusion ◽  
Dissolution Behaviour ◽  
Poorly Soluble

Physicochemical characterization and in vitro dissolution behaviour of celecoxib-β-cyclodextrin inclusion complexes In this study, attempts were made to investigate the effects of β-cyclodextrin (β-CD) on the aqueous solubility and dissolution rate of celecoxib. Inclusion complexes were prepared by the kneading method and characterized by SEM, NMR, IR, DSC, and X-ray powder diffraction. Dissolution rate of the complexes was significantly greater than that of the corresponding physical mixtures and pure drug, indicating that the formation of inclusion complex increased the solubility of the poorly soluble drug celecoxib.

Prediction of blood–brain barrier penetration of poorly soluble drug candidates using surface activity profiling

2010 ◽  
Vol 75 (3) ◽  
pp. 405-410 ◽  
Author(s):  
Anna Christine Petereit ◽  
Kelly Swinney ◽  
Jurgen Mensch ◽  
Claire Mackie ◽  
Sigrid Stokbroekx ◽  
...  
Keyword(s):  
Blood Brain Barrier ◽  
Surface Activity ◽  
Brain Barrier ◽  
Drug Candidates ◽  
Activity Profiling ◽  
Blood Brain ◽  
Barrier Penetration ◽  
Poorly Soluble ◽  
Poorly Soluble Drug

scholarly journals Impairment of the in vitro Release of Carbamazepine from Tablets

2010 ◽  
Vol 10 (3) ◽  
pp. 234-238 ◽  
Author(s):  
Alija Uzunović ◽  
Edina Vranić ◽  
Šeherzada Hadžidedić
Keyword(s):  
Dissolution Rate ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Immediate Release ◽  
Point Of View ◽  
Dissolution Profile ◽  
Poorly Soluble ◽  
Per Oral ◽  
Vitro Release

Carbamazepine belongs to the class II biopharmaceutical classification system (BCS) which is characterized by a high per-oral dose, a low aqueous solubility and a high membrane permeability. The bioavailability of such a drug is limited by the dissolution rate. The present study deals with the formulations of immediate release tablets of poorly soluble carbamazepine. As model tablets for this investigation, two formulations (named “A” and “B” formulations) of carbamazepine tablets labeled to contain 200 mg were evaluated. The aim of this study was to establish possible differences in dissolution profile of these two formulations purchased from the local market.The increased crystallinity together with enlarged particle size, enhanced aggregation and decreased wettability of the drug, resulted in insufficient dissolution rate for formulation “B’.’ From the dissolution point of view, this formulation was inferior to the formulation “A, due to the solubilization effect.

scholarly journals LIQUISOLID COMPACTS: AN INNOVATIVE APPROACH FOR DISSOLUTION ENHANCEMENT

2018 ◽  
Vol 10 (6) ◽  
pp. 11
Author(s):  
Anjana Anil ◽  
Litha Thomas ◽  
Preethi Sudheer
Keyword(s):  
Aqueous Solubility ◽  
Pharmaceutical Products ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Drug Candidates ◽  
Water Soluble Drug ◽  
Water Soluble Drugs ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
Coating Agents

The challenge faced by the majority of the pharmaceutical products is the poor solubility of the drug candidates which leads to low bioavailability. Liquisolid compact is one of the emerging techniques that enhances the dissolution of poorly water soluble drugs. Liquisolid system mentions to the formulation made by the transforming the liquid drug, either in the form of suspension or solution in non volatile solvents into a dry, non-sticky, free-flowing and compactable powder mixtures. This is achieved by mixing the suspension or solution of the drug with appropriate carriers and coating agents. The technology has the ability to increase aqueous solubility, rate of dissolution and absorption of poorly soluble drug by keeping it in molecularly dispersed form leading to its improved bioavailability when compared to conventional tablets. Liquisolid technology is the impending approach for enhancing the solubility of poorly water-soluble drug by adopting simple manufacturing process and low production cost.

scholarly journals Cheminformatics-driven discovery of polymeric micelle formulations for poorly soluble drugs

2019 ◽  
Vol 5 (6) ◽  
pp. eaav9784 ◽  
Author(s):  
Vinicius M. Alves ◽  
Duhyeong Hwang ◽  
Eugene Muratov ◽  
Marina Sokolsky-Papkov ◽  
Ekaterina Varlamova ◽  
...  
Keyword(s):  
Prediction Accuracy ◽  
Drug Loading ◽  
Aqueous Solubility ◽  
Polymeric Micelle ◽  
Loading Capacity ◽  
Poorly Soluble Drugs ◽  
Polymer Complexes ◽  
Drug Candidates ◽  
Therapeutic Development ◽  
Poorly Soluble

Many drug candidates fail therapeutic development because of poor aqueous solubility. We have conceived a computer-aided strategy to enable polymeric micelle-based delivery of poorly soluble drugs. We built models predicting both drug loading efficiency (LE) and loading capacity (LC) using novel descriptors of drug-polymer complexes. These models were employed for virtual screening of drug libraries, and eight drugs predicted to have either high LE and high LC or low LE and low LC were selected. Three putative positives, as well as three putative negative hits, were confirmed experimentally (implying 75% prediction accuracy). Fortuitously, simvastatin, a putative negative hit, was found to have the desired micelle solubility. Podophyllotoxin and simvastatin (LE of 95% and 87% and LC of 43% and 41%, respectively) were among the top five polymeric micelle-soluble compounds ever studied experimentally. The success of the strategy described herein suggests its broad utility for designing drug delivery systems.

A Technical Approach of Solubility Enhancement of Poorly Soluble Drugs: Liquisolid Technique

2020 ◽  
Vol 17 (8) ◽  
pp. 638-650
Author(s):  
Nandini Chaudhary ◽  
Devika Tripathi ◽  
Awani K. Rai
Keyword(s):  
Systemic Circulation ◽  
Solubility Enhancement ◽  
Advanced Technology ◽  
Poorly Soluble Drugs ◽  
Technical Approach ◽  
Liquid Medication ◽  
Insoluble Drugs ◽  
Poorly Soluble ◽  
Poorly Soluble Drug ◽  
The Stability

Background: Solubility is one of the significant pre-formulation properties which regulate the desired concentration of drug in the systemic circulation. Most of the newly discovered chemical entities show poor solubility which consequently leads to poor bioavailability. To enhance the bioavailability of such type of drugs is a big challenge for pharmaceutical scientists. Liquisolid technology is a new and advanced technology used to transform the liquid medication into dry, free-flowing and easily compressible dosage form incorporation with the carrier and coating material. Objectives: This review represents the technical perspective of Liquisolid technologies that overcome the demerits of classic formulation strategies and amend the bioavailability of the poorly soluble drug. This technique is also approaches the stability, hygroscopicity and agglomeration issue which are mainly occurring in other techniques for solubility enhancement. Conclusion: Several technologies have been utilized to minimize the solubility problem but due to the complicated and expensive machinery fails to achieve the desired bioavailability of the poorly soluble drugs. Therefore, Liquisolid technology has been introduced as an innovative and promising technique that recovers the demerits of classic formulation strategies and also improves the bioavailability of the poorly soluble drug. This article exhibits the technical approach of the liquisolid system by improving the solubility as well as bioavailability of water-insoluble drugs.

APPLICATION OF LIQUISOLID TECHNIQUE FOR ENHANCEMENT OF DISSOLUTION OF WATER INSOLUBLE DRUG CHOLECALCIFEROL

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (01) ◽  
pp. 64-72
Author(s):  
Preha Handa ◽  
◽  
Nagoji Shinde ◽  
Bhagvati Sivabalan ◽  
Akhilesh Varma ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Dissolution Enhancement ◽  
Maximum Solubility ◽  
Drug Candidates ◽  
Poorly Soluble ◽  
Burman Design ◽  
Poorly Soluble Drug ◽  
Plackett Burman Design ◽  
Low Solubility ◽  
Better Than

The issue of low solubility and bioavailability poses a significant challenge for most of the drug candidates for oral delivery. Liquisolid, a recently evolved technique for dissolution enhancement, can dodge these barriers. The purpose of this research was to increase the solubility of poorly soluble drug cholecalciferol by liquisolid technique. The cholecalciferol’s solubility studies were performed in a mixture of Polysorbate 80 and PEG 400 in different ratios (1:1, 1:2, 2:1, 1:3, and 3:1). Maximum solubility was observed in a 1:2 ratio. There were changes in the X-ray diffractogram and shifting of the endothermic peak in DSC from 85oC to 146oC, which indicated the drug’s conversion into an amorphous form. The liquisolid form was adsorbed on the carrier material and compressed. The optimization was done by using Plackett Burman Design with Design-Expert software. It was observed that the drugs release profile of the optimized formulation was better than the generic product and was comparable to Divisun tablets 2000 I.U (Innovator).

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