scholarly journals Hydrotropic Solubilization: An Emerging Approach

2021 ◽  
Vol 11 (1-s) ◽  
pp. 200-206
Author(s):  
Ashwin Bhanudas Kuchekar ◽  
Ashwini Gawade ◽  
Sanjay Boldhane
Keyword(s):  
Patient Safety ◽  
Aqueous Solubility ◽  
Oral Route ◽  
Poorly Soluble Drugs ◽  
Gastrointestinal Mucosa ◽  
Optimal Drug ◽  
Insoluble Drugs ◽  
Poorly Soluble ◽  
Poor Absorption ◽  
Low Solubility

Drug development plays an important role in patient safety and effectiveness. The therapeutic suitability of a new drug depends on the solubility. The solubility of the sparingly soluble drug remains a problem in identifying new active compounds. Solubility plays an important role in achieving optimal drug concentration. Low solubility is not only a concern for the production of formulations, but also an obstacle from the outset when identifying active chemicals for therapeutic purposes. Due to its simplicity in terms of ease of administration and economy, the oral route is the preferred route of drug administration over other routes. Effective aqueous solubility is the first prerequisite for oral medication, since low solubility has poor absorption and bioavailability and unpredictable toxicity of the gastrointestinal mucosa. To avoid these crises, different methodologies are used to improve the solubility and bioavailability of poorly soluble drugs, and hydrotropic solubilization is one of them. Hydrotropic agents have the potential to improve the solubility of water-insoluble drugs. In this review, we try to address hydrotropic solubilization methodologies. Keywords: Hydrotropy, Micelles, Solubility, Formulation.

Improved Oral Delivery of Drugs Using Nanoemulsion

2022 ◽  
pp. 93-117
Author(s):  
Subramanian Natesan ◽  
Victor Hmingthansanga ◽  
Nidhi Singh ◽  
Pallab Datta ◽  
Sivakumar Manickam ◽  
...  
Keyword(s):  
Oral Administration ◽  
Oral Delivery ◽  
Oral Route ◽  
Poorly Soluble Drugs ◽  
Site Specific ◽  
Anatomy And Physiology ◽  
Oral Application ◽  
Biological Fate ◽  
Poorly Soluble ◽  
Low Solubility

Administration of drugs through the oral route is considered the simplest and most convenient way to offer greater patient compliance than other routes. Most active drugs discovered in the past and those being discovered in recent times are inadequate because of their inherent limitations in physicochemical properties such as low solubility and permeability, resulting in poor bioavailability, especially after oral administration in the form of tablet or capsule. Pharmaceutical nanoemulsion is the most promising, safer, and multimodal technique for delivering poorly soluble drugs and gaining more attention due to its characteristics such as higher solubilisation capacity, smaller size, surface charge, and site-specific drug targeting. This chapter focuses on the biological fate of nanoemulsion after oral administration and a few case studies related to the oral application of nanoemulsion in delivering poorly soluble drugs. In addition, the anatomy and physiology of the GI tract, components of nanoemulsion, and methods of preparation are addressed.

Solubility Enhancement of Poorly Soluble Drug Simvastatin by Solid Dispersion Technique

2016 ◽  
Vol 2 (2) ◽  
pp. 91-95
Author(s):  
Neelima Rani T ◽  
Pavani A ◽  
Sobhita Rani P ◽  
Srilakshmi N
Keyword(s):  
Dissolution Rate ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Onset Of Action ◽  
Kneading Method ◽  
Wetting Property ◽  
Poorly Soluble ◽  
Dispersion Technique ◽  
Low Solubility

This study aims to formulate solid dispersions (SDs) of Simvastatin (SIM) to improve the aqueous solubility, dissolution rate and to facilitate faster onset of action. Simvastatin is a BCS class II drug having low solubility & therefore low oral bioavailability. In the present study, SDs of simvastatin different drug-carrier ratios were prepared by kneading method. The results showed that simvastatin solubility & dissolution rate enhanced with polymer SSG in the ratio 1:7 due to increase in wetting property or possibly may be due to change in crystallinity of the drug.

Self-microemulsion Technology for Water-insoluble Drug Delivery

2019 ◽  
Vol 15 (6) ◽  
pp. 576-588 ◽  
Author(s):  
Beibei Yan ◽  
Yu Gu ◽  
Juan Zhao ◽  
Yangyang Liu ◽  
Lulu Wang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Aqueous Solubility ◽  
Delivery Systems ◽  
Poorly Soluble Drugs ◽  
New Chemical Entities ◽  
Poorly Soluble ◽  
Water Insoluble Drug ◽  
Semi Solid ◽  
Solidification Technology

: According to the drug discovery, approximately 40% of the new chemical entities show poor bioavailability due to their low aqueous solubility. In order to increase the solubility of the drugs, self-micro emulsifying drug delivery systems (SMEDDS) are considered as an ideal technology for enhancing the permeability of poorly soluble drugs in GI membranes. The SMEDDS are also generally used to enhance the oral bioavailability of the hydrophobic drugs. At present, most of the self-microemulsion drugs are liquid dosage forms, which could cause some disadvantages, such as the low bioavailability of the traditional liquid SMEDDS. Therefore, solid self-micro emulsifying drug delivery systems (S-SMEDDS) have emerged widely in recent years, which were prepared by solidifying a semi-solid or liquid self-emulsifying (SE) ingredient into a powder in order to improve stability, treatment and patient compliance. The article gives a comprehensive introduction of the study of SMEDDS which could effectively tackle the problem of the water-insoluble drug, especially the development of solidification technology of SMEDDS. Finally, the present challenges and the prospects in this field were also discussed.

scholarly journals Solubility Enhancement of Poorly soluble Drugs by using Novel Techniques : A Comprehensive Review

2020 ◽  
Vol 13 (2) ◽  
pp. 80-93 ◽  
Author(s):  
Abikesh P.K. Mahapatra ◽  
Vinod Patil ◽  
Ravindra Patil
Keyword(s):  
Dissolution Rate ◽  
Class Ii ◽  
Systemic Circulation ◽  
Poorly Soluble Drugs ◽  
Formulation Development ◽  
Solid Dosage ◽  
Bcs Class Ii ◽  
Pharmacological Response ◽  
Poorly Soluble ◽  
Low Solubility

The primary aim of this review was to improve the solubility and Bioavailability of BCS Class-II drugs because of their low solubility and dissolution rate. Solubility is one of the imp parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. Hence the class- II drugs require enhancement in solubility and dissolution rate in there formulation development particularly in solid dosage form such as in tablet and capsule. So because of this there are several methods and newer emerging technologies have been developed for increasing the solubility as well as Bioavailability of class –II drugs. In this article review on literature on newer techniques or methods as well as recent research on formulation development of class- II drugs was done.

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.

Polymeric Nanomicelles of Soluplus® as a Strategy for Enhancing the Solubility, Bioavailability and Efficacy of Poorly Soluble Active Compounds

2019 ◽  
Vol 9 (3) ◽  
pp. 184-197 ◽  
Author(s):  
Rosario Pignatello ◽  
Roberta Corsaro
Keyword(s):  
Polyvinyl Acetate ◽  
Solid Dispersions ◽  
Aqueous Media ◽  
Physical Stability ◽  
Small Diameter ◽  
Amorphous Solid ◽  
Poorly Soluble Drugs ◽  
Insoluble Drugs ◽  
Poorly Soluble

: Soluplus® is a commercially available graft amphipathic copolymer consisting of polyvinyl caprolactam, polyvinyl acetate, and polyethyleneglycol (13% PEG 6000/57% vinyl caprolactam/30% vinyl acetate). Among the various applications of this solubilizer excipient, produced by BASF, such as the production of amorphous solid dispersions of insoluble drugs, Soluplus® has shown to be able to form nano-sized micelles in water or other aqueous solutions, characterized by a very small diameter and an exceptionally narrow size distribution. These formulations allow to improve the solubility and physical stability in aqueous media of poorly soluble drugs. This review summarizes the recent data from literature on the methods of production and characterization of drugloaded nanomicelles based on Soluplus®, highlighting the potential fields of therapeutic application.

scholarly journals Novel Approaches to Enhance Oral Bioavailability of Poorly Soluble Drugs

2020 ◽  
Vol 2 (1) ◽  
pp. 12-16
Author(s):  
Buduru Gowthami ◽  
S.V. Gopala Krishna ◽  
D. Subba Rao
Keyword(s):  
Oral Administration ◽  
Metabolic Activity ◽  
Poorly Soluble Drugs ◽  
Drug Molecules ◽  
The Poor ◽  
Insoluble Drugs ◽  
Poorly Soluble ◽  
Convenient Route ◽  
Novel Approaches ◽  
Approved Drugs

Oral administration is considered as major, convenient route among all other routes of delivery, owing to several benefits. But, the poor solubility or enzymatic/metabolic activity are the major concerns in developing a successful formulation. About 40% of approved drugs which are in the current market and 90% of new drug molecules in the developmental pipeline are hydrophobic in nature. The challenge to formulate insoluble drugs has met with various approaches to overcome the problems related to solubility, application of nanotechnology is one amongst them. The present review deals with various nanocarriers and technologies that are proven to be effective in enhancing the bioavilability of poorly soluble drugs.

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.

Recent Advances in Self-Emulsifying Drug Delivery Systems

2015 ◽  
Vol 8 (1) ◽  
pp. 2693-2697
Author(s):  
Amol S Deshmukh
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Aqueous Solubility ◽  
Oral Route ◽  
Delivery Systems ◽  
Novel Technologies ◽  
Oral Formulations ◽  
Modern Drug ◽  
New Chemical Entities ◽  
Poorly Soluble

Oral route has always been preferred route for formulators and has dominated over other routes of administrations. But major problem encountered in oral formulations (as estimated more than 50 % of oral formulations are found to be poorly aqueous soluble), is low bioavailability, giving rise to further problems like, high inter and intra subject variability, lack of dose uniformity and finally leading to therapeutic failure. Approximately 40% of new chemical entities exhibit poor aqueous solubility and present a major challenge to modern drug delivery system, because of their low bioavailability. Particularly for BCS class II substances, the bioavailability may be enhanced by increasing the solubility and dissolution rate of the drug in the gastro-intestinal fluids. The newer and novel technologies developed in recent year for troubleshooting such above problems. This review describes an overview of SEDDS as a capable approach to effectively capture the problem of poorly soluble molecules and give the novel approaches for evaluation of the SEDDS. Self-emulsifying drug delivery systems (SEDDS) are isotropic mixtures of drug, lipids and surfactants, usually with one or more hydrophilic co-solvents or co-emulsifiers.  

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