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.

Drug Nanocrystals: A Comprehensive Review with Current Regulatory Guidelines

2020 ◽  
Vol 17 (6) ◽  
pp. 470-482
Author(s):  
Mori Dhaval ◽  
Jalpa Makwana ◽  
Ekta Sakariya ◽  
Kiran Dudhat
Keyword(s):  
Dissolution Rate ◽  
Dosage Form ◽  
Poorly Soluble Drugs ◽  
Comprehensive Review ◽  
Drug Molecules ◽  
Regulatory Guidelines ◽  
Poorly Soluble ◽  
Form Design ◽  
Capsule Suspension ◽  
Final Dosage Form

Drug nanocrystals offer an attractive approach for improving the solubility and dissolution rate of poorly soluble drugs which accounts for nearly 40 % newly discovered drug molecules. Both methods for manufacturing drug nanocrystals have high industrial acceptability for being simple and easy to scale which is evident from the number of approved products available in the market. Ability to modify multiple aspects of dosage form like bioavailability, release pattern and dosage form requirement along with flexibility in choosing final dosage form starting from the tablet, capsule, suspension to parenteral one, have made nanocrystal technology one of the very promising and adaptable technology for dosage form design.

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.

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.

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.

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.

Technological Advancements in Oral Films

2019 ◽  
Vol 9 (01) ◽  
pp. 15-20
Author(s):  
B Pandey ◽  
A B Khan
Keyword(s):  
3D Printing ◽  
Historical Background ◽  
Poorly Soluble Drugs ◽  
Modern Approach ◽  
Poorly Soluble ◽  
Critical Process Parameters ◽  
Biopharmaceutical Properties ◽  
Oral Films ◽  
Hot Melt ◽  
Modern Technologies

The aim of the review was to explore the necessity, advantages and different techniques of oral films for enhancing solubility of poorly soluble drugs with an emphasis on the newer, state-of the art technologies, such as 3D printing and hot-melt extrusion (HME). The historical background of oral films is presented along with the regularly used techniques. The modern approach of quality-by-design (QbD) is unravelled, identifying appropriate critical process parameters (CPP) and applied to oral films. A section is devoted modern technologies such as 3D printing and HME of oral films. Oral films are innovative formulations by which poorly soluble drugs have been founds to give positive results in enhancing their solubility and dissolution characteristics. With modern sophisticated techniques, precise mass production of oral films has been given a thrust. Oral films have better patient compliance, improved biopharmaceutical properties, improved efficacy, and better safety. By applying QbD and implementation of modern technologies the newer generation of oral films are yielding promising results

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