The impact of polymeric excipients on the particle size of poorly soluble drugs after pH-induced precipitation

2016 ◽  
Vol 95 ◽  
pp. 138-144 ◽  
Author(s):  
Kateřina Punčochová ◽  
Marie Prajzlerová ◽  
Josef Beránek ◽  
František Štěpánek
Keyword(s):  
Particle Size ◽  
Poorly Soluble Drugs ◽  
Poorly Soluble ◽  
The Impact

scholarly journals Nanocrystals of Poorly Soluble Drugs: Drug Bioavailability and Physicochemical Stability

Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 134 ◽  
Author(s):  
Maria Gigliobianco ◽  
Cristina Casadidio ◽  
Roberta Censi ◽  
Piera Di Martino
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Colloidal Particles ◽  
Poorly Soluble Drugs ◽  
Drug Bioavailability ◽  
Free System ◽  
Surface Active Agents ◽  
Carrier Free ◽  
Poorly Soluble ◽  
Surface Active

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.

scholarly journals Formulation and In-Vitro evaluation of Nanocrystal formulation of poorly soluble drugs

2020 ◽  
Vol 9 (4-s) ◽  
pp. 1183-1190
Author(s):  
Arvind Sharma ◽  
Alok Pal Jain ◽  
Sandeep Arora
Keyword(s):  
Particle Size ◽  
In Vitro Study ◽  
Physicochemical Characteristics ◽  
Precipitation Method ◽  
Drug Candidate ◽  
Poorly Soluble Drugs ◽  
Drug Release Profile ◽  
Scanning Calorimetry ◽  
Poorly Soluble

Introduction:-Poor solubility of drug compounds which accounts for 40% of new molecules investigated at present is an issue of great concern in pharmaceutical industry and reducing particle size (i,e to reduce below 1000 nm )of drug candidate to be investigated is one of the simplest and efficient ways to overcome this challenge. Drug nanocrystals, solid nanosized drug particles are defined as formulation having 100% drug, which are covered by a stabilizer layer. In this study attempt was made to formulate and evaluate nanocrystals of poorly soluble drugs having low oral bioavailability. Material and method:- Nanocrystals were prepared successfully by varying concentration of different stabilizers by anti-solvent precipitation method. The formulated nanocrystals were evaluated by determining physicochemical characteristics such as physical appearance, Differential Scanning Calorimetry (DSC), scanning electron microscopy (SEM), X-ray powder diffractometry, solubility studies, particle size distribution, zeta potential, and in vitro drug release profile studies. Results:- An in-vitro study was performed on the successful formulation in comparison to drug powder using dissolution apparatus The particle size of RVT and PSNC-3 was found to be 1975.3 nm and 790.1 nm respectively. Conclusion: Precipitated Nanocrystals formulated with different stablizer’s method resultedin formation of small and uniform RVT nanocrystals with an improved saturation solubility, dissolution rate. Keywords: Nanocrystal, poorly soluble drugs

scholarly journals Nanocrystals of Poorly Soluble Drugs: Drug Bioavailability and Physicochemical Stability

2018 ◽  
Author(s):  
Maria Rosa Gigliobianco ◽  
Cristina Casadidio ◽  
Roberta Censi ◽  
Piera Di Martino
Keyword(s):  
Particle Size ◽  
Particle Surface ◽  
Poorly Soluble Drugs ◽  
Drug Bioavailability ◽  
Particle Surface Area ◽  
Drug Products ◽  
Surface Active Agents ◽  
Physicochemical Stability ◽  
Poorly Soluble ◽  
Surface Active

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.

scholarly journals Upgrading the Topical Delivery of Poorly Soluble Drugs Using Ionic Liquids as a Versatile Tool

2021 ◽  
Vol 22 (9) ◽  
pp. 4338
Author(s):  
Rita Caparica ◽  
Ana Júlio ◽  
Filipe Fernandes ◽  
Maria Eduarda M. Araújo ◽  
João Guilherme Costa ◽  
...  
Keyword(s):  
Ionic Liquids ◽  
Amino Acid ◽  
Poorly Soluble Drugs ◽  
Versatile Tool ◽  
Poorly Soluble ◽  
And Performance ◽  
The Stability ◽  
Drug Incorporation ◽  
Toxic Concentrations ◽  
The Impact

Numerous studies are continuously being carried out in pursuit of formulations with higher performance. Problems such as poor drug solubility, which hinders drug incorporation into delivery systems and bioavailability, or limitations concerning the stability and performance of the formulations may cause difficulties, since solving all these drawbacks at once is a huge challenge. Ionic liquids (ILs), due to their tunable nature, may hypothetically be synthesized for a particular application. Therefore, predicting the impact of a particular combination of ions within an IL in drug delivery could be a useful strategy. Eight ILs, two choline amino acid ILs, two imidazole halogenated ILs, and four imidazole amino acid ILs, were prepared. Their applicability at non-toxic concentrations, for improving solubility and the incorporation of the poorly soluble, ferulic, caffeic, and p-coumaric acids, as well as rutin, into topical emulsions, was assessed. Next, the impact of the ILs on the performance of the formulations was investigated. Our study showed that choosing the appropriate IL leads to a clear upgrade of a topical emulsion, by optimizing multiple features of its performance, such as improving the delivery of poorly soluble drugs, altering the viscosity, which may lead to better sensorial features, and increasing the stability over time.

scholarly journals Combinative Particle Size Reduction Technologies for the Production of Drug Nanocrystals

2014 ◽  
Vol 2014 ◽  
pp. 1-14 ◽  
Author(s):  
Jaime Salazar ◽  
Rainer H. Müller ◽  
Jan P. Möschwitzer
Keyword(s):  
Particle Size ◽  
Size Reduction ◽  
Particle Sizes ◽  
Poorly Soluble Drugs ◽  
Particle Size Reduction ◽  
Novel Technologies ◽  
Poorly Soluble ◽  
Wet Bead Milling ◽  
Standard Techniques ◽  
Reduction Effectiveness

Nanosizing is a suitable method to enhance the dissolution rate and therefore the bioavailability of poorly soluble drugs. The success of the particle size reduction processes depends on critical factors such as the employed technology, equipment, and drug physicochemical properties. High pressure homogenization and wet bead milling are standard comminution techniques that have been already employed to successfully formulate poorly soluble drugs and bring them to market. However, these techniques have limitations in their particle size reduction performance, such as long production times and the necessity of employing a micronized drug as the starting material. This review article discusses the development of combinative methods, such as the NANOEDGE, H 96, H 69, H 42, and CT technologies. These processes were developed to improve the particle size reduction effectiveness of the standard techniques. These novel technologies can combine bottom-up and/or top-down techniques in a two-step process. The combinative processes lead in general to improved particle size reduction effectiveness. Faster production of drug nanocrystals and smaller final mean particle sizes are among the main advantages. The combinative particle size reduction technologies are very useful formulation tools, and they will continue acquiring importance for the production of drug nanocrystals.

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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