Drug Solubilization by Surfactants: Experimental Methods and Theoretical Perspectives

Author(s):  
Nisar Ahmad Malik

: This mini review will give an insight into the need and usefulness of investigating the solubilization of poorly soluble drugs. Commonly used experimental and theoretical models are outlined to study the efficacy of the carrier or excipient for the poorly soluble drugs. Furthermore, the use of surface active agents for drug solubilization is discussed in correlation with the mathematical models suggested from time to time. A few experimental techniques are also discussed which would be very helpful in elucidating the interactions prevailing in the mixed systems of poorly soluble drugs and surface active agents.

Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 134 ◽  
Author(s):  
Maria Gigliobianco ◽  
Cristina Casadidio ◽  
Roberta Censi ◽  
Piera Di Martino

Many approaches have been developed over time to overcome the bioavailability limitations of poorly soluble drugs. With the advances in nanotechnology in recent decades, science and industry have been approaching this issue through the formulation of drugs as nanocrystals, which consist of “pure drugs and a minimum of surface active agents required for stabilization”. They are defined as “carrier-free submicron colloidal drug delivery systems with a mean particle size in the nanometer range, typically between 10–800 nm”. The primary importance of these nanoparticles was the reduction of particle size to nanoscale dimensions, with an increase in the particle surface area in contact with the dissolution medium, and thus in bioavailability. This approach has been proven successful, as demonstrated by the number of such drug products on the market. Nonetheless, despite the definition that indicates nanocrystals as a “carrier-free” system, surface active agents are necessary to prevent colloidal particles aggregation and thus improve stability. In addition, in more recent years, nanocrystal properties and technologies have attracted the interest of researchers as a means to obtain colloidal particles with modified biological properties, and thus their interest is now also addressed to modify the drug delivery and targeting. The present work provides an overview of the achievements in improving the bioavailability of poorly soluble drugs according to their administration route, describes the methods developed to overcome physicochemical and stability-related problems, and in particular reviews different stabilizers and surface agents that are able to modify the drug delivery and targeting.


Author(s):  
Maria Rosa Gigliobianco ◽  
Cristina Casadidio ◽  
Roberta Censi ◽  
Piera Di Martino

Many approaches have been developed over time to counter the bioavailability limitations of poorly soluble drugs. With advances in nanotechnology in recent decades, science and industry have been approaching this issue through the formulation of drugs as nanocrystals, which consist of pure drugs and a minimum of surface active agents required for stabilization. They are carrier-free submicron colloidal drug delivery systems with a mean particle size in the nanometer range, typically between 10 and 800 nm. By reducing particle size to nanoscale, the particle surface area available for the molecule dissolution in the direction of dissolution medium is increased, and thus bioavailability is enhanced. This approach has proven successful, as demonstrated by the number of such drug products on the market. R&D and industry have offered many technological solutions to reduce the particle size to nanoscale, and also devised solutions for the handling of particle of nanodimensions, such as methods to accurately measure nanoparticle size and techniques to prevent physicochemical and stability related problems, such as aggregation. The present work provides an overview of the more recent achievements in improving the bioavailability of poorly soluble drugs according to their administration route, and describes the methods developed to overcome physicochemical and stability related problems.


Author(s):  
Ganesh R Godge ◽  
Mahesh A Garje ◽  
Aniket B Dode ◽  
Kailas N Tarkase

Now a days, many drug candidates are water insoluble hence they show a limited drug release and poor bioavailability. It is difficult to formulate these drugs by conventional dosage form. Nanosuspension technology is a promising approach to solve the problems of poorly soluble and less bioavailable drugs. Nanosuspension is a very finely colloidal, biphasic, and uniformly dispersed solid drug particles in a suitable aqueous vehicle, having a particle size below 1 μm stabilized by suitable surface active agents and polymers. Nanosuspensions are prepared by various suitable techniques for drug delivery applications. Due to reduced particle size at the nano scale, surface area, saturation solubility, dissolution velocity and bioavailability of BCS class II and class IV drugs are increased sufficiently. Nanosuspension is suitable to administration via various routes such as oral, intravenous, topical, pulmonary and ocular delivery systems. Nanosuspension can be also used for targeting purpose in various diseases such as cancer, HIV and production of sustained and extended release products by choosing suitable polymers. Production and manufacturing are not complicated, easy to scale up. Top down and bottom technologies are used for the preparation of nanosuspensions. It includes methods such as high-pressure homogenization, by milling media method, precipitation method, probe sonication, dry-co-grinding, supercritical fluid method, and lipid emulsion method. Formulation consists of stabilizers, surfactant, and solvents. Nanosuspension can be stored in the form of dry powder using spray drying, freeze drying techniques. This review describes the advantages, various methods of preparation, formulation consideration and characterization of nanosuspension.  


1986 ◽  
Vol 51 (2) ◽  
pp. 302-313 ◽  
Author(s):  
Zdeněk Brož ◽  
Mirko Endršt

Experimental data have been used on absorption of poorly soluble gases, helium, carbon dioxide, and propane, to study the mechanism of interfacial mass transfer in vertical gravitational film flow down the surface of the expanded metal sheet. It has been found that upon addition of surface active agents into water, the original almost freely moving liquid-gas interfacial surface behaves similarly as a liquid-solid surface. Two adjustable hydrodynamic parameters have been evaluated on the basis of the film penetration theory with the physical meaning of the dimensionless thickness of an unmixed region near the interface ϑ+ = 0.4 and the characteristic length < scale of the disturbance λ+ = 26.4.


Author(s):  
Chinthaginjala Haranath ◽  
Reddy Hindustan Abdul Ahad Pushpalatha Gutty ◽  
Kodi Kalpana ◽  
Manchikanti Sai Priyanka ◽  
Pasam Devika

In the last decade, nanosuspensions have gained considerable interest as a method for formulating poorly soluble drugs. Because of their cost-effectiveness and technological simplicity compared to liposomes and other colloidal drug carriers, nanoscale systems have recently received a lot of attention as a way of solving problems of solubility. Nanosuspensions are biphasic systems comprising of pure drug particles dispersed in an aqueous vehicle, stabilized by surface active agents. Fabrication of nanosuspension is simple and more advantageous than other approaches. Nanosuspension is a very finely single solid drug particle in an aqueous vessel, stabilized by surfactants for either oral or topical use or for parenteral and pulmonary administration, it can also be used for targeted drug delivery when incorporated in the ocular inserts and mucoadhesive hydrogels, with reduced particle size resulting in increased dissolution rate. This article covers the preparation of nanosuspension by bottom up technology, top down technology, melt emulsification, emulsification- solvent evaporation and supercritical fluid with their advantages and disadvantages, aspects of structure, classification and their drug delivery applications. Nanosuspension can be processed for the drugs which are of hydrophobic in nature quite easily employing stability enhancers, solvents that are of organic and additional ingredients including buffering agents, salts, PEG, osmotic agents and anti-freeze compounds.


2019 ◽  
Vol 9 (01) ◽  
pp. 15-20
Author(s):  
B Pandey ◽  
A B Khan

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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