scholarly journals Nanosuspension Technologies for Delivery of Poorly Soluble Drugs

2015 ◽  
Vol 2015 ◽  
pp. 1-13 ◽  
Author(s):  
Roya Yadollahi ◽  
Krasimir Vasilev ◽  
Spomenka Simovic
Keyword(s):  
Aqueous Solubility ◽  
Drug Formulation ◽  
Preparation Methods ◽  
Administration Routes ◽  
Drug Molecules ◽  
Advanced Therapies ◽  
Poorly Soluble ◽  
Minimal Damage ◽  
Processing Techniques ◽  
Cancer Tissues

Poor aqueous solubility of some drug molecules is a major problem in drug formulation. Drug nanosuspensions emerged as one solution to delivering such hydrophobic drugs. Scaling down to nanoparticles enhances drug aqueous solubility and bioavailability by increasing drug surface area that comes into contact with biological media. Nanosuspensions that have attracted particular attention are those sterically stabilised by steric polymers such as polyethylene glycol (PEG) with a typical size range of 10–100 nm. These nanoparticles are capable of accumulating in targeted areas such as cancer tissues and infarct zones with minimal damage to healthy tissues. Nanosuspensions are often prepared by commercially available methods such as high pressure homogenization, media milling, emulsification, and melt emulsification. Solidification and surface modification methods are post-processing techniques used to add particular properties for advanced therapies. In this review, we firstly describe preparation methods for nanosuspensions. Secondly, we highlight typical characterization techniques. Finally, we describe several practical application of applications for drug delivery design and different administration routes such as parenteral, pulmonary, oral, and ocular.

Review: Emerging role of nanosuspensions for drug delivery and stability

2021 ◽  
Vol 06 ◽  
Author(s):  
Hitesh Kumar Dewangan ◽  
Brijesh Yadav ◽  
Manas Kumar Jha
Keyword(s):  
Drug Delivery ◽  
Size Range ◽  
Aqueous Solubility ◽  
Active Surface ◽  
Active Surface Area ◽  
Drug Molecules ◽  
Media Milling ◽  
Advanced Therapies ◽  
Processing Techniques

: Poor aqueous solubility of some of the drug molecules are of a major concern, which can be emerged in the nano-suspension for better delivery. Coming up to the nanoparticles, it enhances the bioavailability along with the aqueous solubility of the drug which is accomplished by increasing the active surface area of the drug. The gained attention of the nanosuspension is due to its stabilization facility which is done by polymers such as polyethylene glycol (PEG) having a particular size range of 10-100 nm. Hence, to our notice, these nanoparticles have the capacity of binding in the targeted parts with a very low damage to the healthy tissues. These are seen to be prepared by various methods such as media milling, high pressure homogenization, and emulsification along with melt emulsification. Apart it can also be seen that surface modification and solidification have been used to add specific properties to the advanced therapies as post-processing techniques. These days, it is very evident that the drugs are water insoluble and thus have a poor bioavailability which have been developed from the drug delivery programmes and in order to combat this obstacle, nanotechnology have been found to be of specific interest. In order to elevate the bioavailability by increasing the dissolution rate, the methodology of reduction of the associated drug particles into its subsequent submicron range is incorporated. For oral and non-oral administration, these nanosuspensions formulations are used for delivering of the drugs.

The Emerging Role of Nanosuspensions for Drug Delivery and Stability

2021 ◽  
Vol 12 ◽  
Author(s):  
Hitesh Kumar Dewangan
Keyword(s):  
Water Solubility ◽  
Size Range ◽  
Aqueous Solubility ◽  
Active Surface ◽  
Water Soluble ◽  
Active Surface Area ◽  
Specific Interest ◽  
Advanced Therapies ◽  
Processing Techniques

: Poor solubility of some medicinal compounds is a serious challenge that can be addressed by using a nano-suspension for improved delivery. The nanoparticles enhance the bioavailability along with the aqueous solubility of the drug, which is accomplished by increasing the active surface area of the drug. The gained attention of the nanosuspension is due to its stabilization facility, which is achieved by polymers, such as polyethylene glycol (PEG), having a particular size range of 10 - 100 nm. Hence, these nanoparticles have the capacity of binding to the targeted with very low damage to the healthy tissues. These are prepared by various methods, such as milling, high-pressure homogenization, and emulsification, along with melt emulsification. Moreover, surface modification and solidification have been used to add specific properties to the advanced therapies as post-processing techniques. For many decades, it has been known that water solubility hampers the bioavailability and not all drugs are water-soluble. In order to combat this obstacle, nanotechnology has been found to be of specific interest. For elevating the bioavailability by increasing the dissolution rate, the methodology of reduction of the associated drug particles into their subsequent submicron range is incorporated. For oral and non-oral administration, these nanosuspension formulations are used for the delivery of drugs.

scholarly journals Design and Development of Liquid Drug Reservoirs for Microneedle Delivery of Poorly Soluble Drug Molecules

Pharmaceutics ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 605 ◽  
Author(s):  
Mary-Carmel Kearney ◽  
Peter E. McKenna ◽  
Helen L. Quinn ◽  
Aaron J. Courtenay ◽  
Eneko Larrañeta ◽  
...  
Keyword(s):  
Nile Red ◽  
Aqueous Solubility ◽  
Log P ◽  
Reservoir Properties ◽  
Peg 400 ◽  
Drug Molecules ◽  
Hydrophobic Compounds ◽  
Custom Made ◽  
Poorly Soluble ◽  
Poly Ethylene

The poor aqueous solubility of existing and emerging drugs is a major issue faced by the pharmaceutical industry. Water-miscible organic solvents, termed co-solvents, can be used to enhance the solubility of poorly soluble substances. Typically, drugs with poor aqueous solubility and Log P > 3 are not amenable to delivery across the skin. This study investigated the use of co-solvents as reservoirs to be used in combination with hydrogel-forming microneedles to enhance the transdermal delivery of hydrophobic compounds, namely Nile red, olanzapine and atorvastatin. A custom-made Franz cell apparatus was fabricated to test the suitability of a liquid drug reservoir in combination with polymeric microneedles. A co-solvency approach to reservoir formulation proved effective, with 83.30% ± 9.38% of Nile red dye, dissolved in 1 mL poly(ethylene glycol) (PEG 400), permeating neonatal porcine skin over 24 h. PEG 400 and propylene glycol were found to be suitable reservoir media for olanzapine and atorvastatin, with approximately 50% of each drug delivered after 24 h. This work provides crucial proof-of-concept evidence that the manipulation of microneedle reservoir properties is an effective method to facilitate microneedle-mediated delivery of hydrophobic compounds.

scholarly journals Solubility Enhancement of Cox-II Inhibitors by Cosolvency Approach

1970 ◽  
Vol 7 (2) ◽  
pp. 119-126 ◽  
Author(s):  
PR Sathesh Babu ◽  
CVS Subrahmanyam ◽  
J Thimmasetty ◽  
R Manavalan ◽  
K Valliappan ◽  
...  
Keyword(s):  
Interaction Mechanism ◽  
Chemical Properties ◽  
Aqueous Solubility ◽  
Dosage Forms ◽  
Solubility Enhancement ◽  
Peg 400 ◽  
Drug Molecules ◽  
Poorly Soluble ◽  
Solvent Blends ◽  
Major Factors

Solubility enhancement of meloxicam and rofecoxib, which are poorly soluble in water, was attempted. These are available in the form of solid dosage forms but not in solution dosage forms due to their low aqueous solubility. In this work, aqueous solubility of meloxicam and rofecoxib was improved using the biocompatible solvents such as ethanol, propylene glycol, glycerin, and PEG 400. Physico-chemical properties of the solvents such as intermolecular interactions and the ability of the solvent to form a hydrogen bond with the drug molecules were found to be the major factors involved in the dissolution of drugs. It was found that less polar solvents were found to increase solubility by greater extent, thus accentuating hydrophobic interaction mechanism. Among the solvent blends studied, water-PEG 400 had highest solubilization potential. Thus, the study generated an important dataset so as to compare effect of various cosolvents on the solubility of the drugs. Key words: Aqueous solubility, Meloxicam, Rofecoxib, Cosolvency. doi: 10.3329/dujps.v7i2.2166     Dhaka Univ. J. Pharm. Sci. 7(2): 119-126, 2008 (December)

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 In vitro and in vivo Evaluation of Ibuprofen Nanosuspensions for Enhanced Oral Bioavailability

2021 ◽  
Author(s):  
Mohsen Hedaya ◽  
Farzana Bandarkar ◽  
Aly Nada
Keyword(s):  
Particle Size ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
In Vivo Evaluation ◽  
Poorly Soluble ◽  
Extent Of Absorption ◽  
Better Than

Introduction: The objectives were to prepare, characterize and in vivo evaluate different ibuprofen (IBU) nanosuspensions prepared by ultra-homogenization, after oral administration to rabbits. Methods: The nanosuspensions produced by ultra-homogenization were tested and compared with a marketed IBU suspension for particle size, in vitro dissolution and in vivo absorption. Five groups of rabbits received orally 25 mg/kg of IBU nanosuspension, nanoparticles, unhomogenized suspension, marketed product and untreated suspension. A sixth group received 5 mg/kg IBU intravenously. Serial blood samples were obtained after IBU administration. Results: The formulated nanosuspensions showed significant decrease in particle size. Polyvinyl Pyrrolidone K30 (PP) was found to improve IBU aqueous solubility much better than the other tested polymers. Addition of Tween 80 (TW), in equal amount as PP (IBU: PP:TW, 1:2:2 w/w) resulted in much smaller particle size and better dissolution rate. The Cmax achieved were 14.8±1.64, 11.1±1.37, 9.01±0.761, 7.03±1.38 and 3.23±1.03 μg/ml and the tmax were 36±8.2, 39±8.2, 100±17.3, 112±15 and 105±17 min for the nanosuspension, nanoparticle, unhomogenized suspension, marketed IBU suspension and untreated IBU suspension in water, respectively. Bioavailability of the different formulations relative to the marketed suspension were the highest for nanosuspension> unhomogenized suspension> nanoparticles> untreated IBU suspension. Conclusion: IBU/PP/TW nanosuspensions showed enhanced in vitro dissolution as well as faster rate and higher extent of absorption as indicated from the higher Cmax, shorter tmax and larger AUC. The in vivo data supported the in vitro results. Nanosuspensions prepared by ultra-high-pressure-homogenization technique can be used as a good formulation strategy to enhance the rate and extent of absorption of poorly soluble drugs.

Exploration on the Drug Solubility Enhancement in Aqueous Medium with the Help of Endo-Functionalized Molecular Tubes: A Computational Approach

2021 ◽  
Author(s):  
Rabindranath Paul ◽  
Sandip Paul
Keyword(s):  
Pharmaceutical Industry ◽  
Aqueous Medium ◽  
Aqueous Solubility ◽  
Solubility Enhancement ◽  
Computational Approach ◽  
Drug Solubility ◽  
Drug Candidates ◽  
Drug Molecules ◽  
Molecular Tubes

One major problem in the pharmaceutical industry is the aqueous solubility of newly developed orally administered drug candidates. More than 50 % of the newly developed drug molecules suffer from...

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