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.

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.

ChemInform Abstract: Enhancement the Dissolution Rate and Solubility of Poorly Soluble Drugs: Review

ChemInform ◽  
2014 ◽  
Vol 45 (34) ◽  
pp. no-no
Author(s):  
Mubarak Abdullah Saleh ◽  
Salam A. Mohammed ◽  
Ezzat C. Abdullah ◽  
Laith A. Hashim
Keyword(s):  
Dissolution Rate ◽  
Poorly Soluble Drugs ◽  
Poorly Soluble

scholarly journals Evaluation of Poorly Soluble Drugs’ Dissolution Rate by Laser Scattering in Different Water Isotopologues

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 601
Author(s):  
Elena V. Uspenskaya ◽  
Tatiana V. Pleteneva ◽  
Ilaha V. Kazimova ◽  
Anton V. Syroeshkin
Keyword(s):  
Dissolution Rate ◽  
Isotope Effect ◽  
Targeted Delivery ◽  
Kinetic Isotope Effect ◽  
The Body ◽  
Poorly Soluble Drugs ◽  
Laser Scattering ◽  
Kinetic Isotope ◽  
Medicinal Substances ◽  
Poorly Soluble

The most important task in the design of dosage forms is to modify the pharmaceutical substances structure in order to increase solubilization, targeted delivery, controlled rate of drug administration, and its bioavailability. Screening—laboratory (in vitro) or computer (in silico)—as a procedure for selecting a prototype for the design of a drug molecule, involves several years of research and significant costs. Among a large number of solvents and diluents (alcohol, ether, oils, glycerol, Vaseline) used in the pharmaceutical industry for the manufacture of drugs water finds the greatest application. This is because all biological reactions (reactions in living systems) take place in water and distribution of the fluid in the body and the substances found within is critical for the maintenance of intracellular and extracellular functions. Modern studies in the field of the stable isotopic compositions of natural water and its structure and properties make it possible to use isotopic transformations of the water to improve the pharmacokinetic properties of medicinal substances without previous structural modification. It is known that by replacing any of the atoms in the reacting substance molecule with its isotope, it is possible to record changes in the reactivity, which are expressed as a change in the reaction rate constant, i.e., in the manifestation of the kinetic isotope effect (KIE). The article presents the results of studies on the effect of the kinetic isotope effect of a solvent—water—on increasing the solubility and dissolution rate constants of poorly soluble drugs using laser diffraction spectroscopy. The results of the studies can be successfully implemented in pharmaceutical practice to overcome the poor solubility of medicinal substances of classes II and IV, according to the biopharmaceutical classification system (BCS), in water for pharmaceutical purposes by performing its preliminary and safe isotopic modification.

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.

Comparison of Different Methods for Enhancing the Dissolution Rate of Poorly Soluble Drugs: Case of Griseofulvin

2005 ◽  
Vol 5 (3) ◽  
pp. 277-280 ◽  
Author(s):  
I. Smirnova ◽  
M. Türk ◽  
R. Wischumerski ◽  
M. A. Wahl
Keyword(s):  
Dissolution Rate ◽  
Poorly Soluble Drugs ◽  
Poorly Soluble

scholarly journals DEVELOPMENT OF NANOCRYSTAL FORMULATION WITH IMPROVED DISSOLUTION

2018 ◽  
Vol 8 (5) ◽  
pp. 118-129 ◽  
Author(s):  
Jaspreet Kaur Saini ◽  
Sandeep Kumar
Keyword(s):  
Dissolution Rate ◽  
Surface Area ◽  
Therapeutic Index ◽  
Water Soluble ◽  
Poorly Soluble Drugs ◽  
Pharmaceutical Applications ◽  
Interesting Approach ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
The One

With the advancement in modern pharmaceutical technologies, Nanotechnology is the one of the most establish technology which is used to improve the therapeutic index and to overcome the formulation challenges of poorly water-soluble compounds. Nanocrystals, in nano range, is the interesting approach for poorly soluble drugs. Due to the small size, increased surface area enhanced the dissolution rate and solubility of drug. In this paper, current technologies and methods in nanocrystal preparation, stabilization, pharmaceutical applications and limitations of nanocrystal are reviewed. Keywords: Nanocrystal, limitations, stabilization, preparation, applications

Sign in / Sign up

Export Citation Format

Share Document