scholarly journals Dendrimers as Pharmaceutical Excipients: Synthesis, Properties, Toxicity and Biomedical Applications

Materials ◽  
2019 ◽  
Vol 13 (1) ◽  
pp. 65 ◽  
Author(s):  
Ana Santos ◽  
Francisco Veiga ◽  
Ana Figueiras
Keyword(s):  
Drug Efficacy ◽  
Aqueous Solubility ◽  
Pharmaceutical Formulations ◽  
The United States ◽  
Water Soluble ◽  
European Medicines Agency ◽  
Uniform Size ◽  
Pharmaceutical Excipients ◽  
Synthesis Properties ◽  
Water Soluble Drugs

The European Medicines Agency (EMA) and the Current Good Manufacturing Practices (cGMP) in the United States of America, define excipient as the constituents of the pharmaceutical form other than the active ingredient, i.e., any component that is intended to furnish pharmacological activity. Although dendrimers do not have a pharmacopoeia monograph and, therefore, cannot be recognized as a pharmaceutical excipient, these nanostructures have received enormous attention from researchers. Due to their unique properties, like the nanoscale uniform size, a high degree of branching, polyvalency, aqueous solubility, internal cavities, and biocompatibility, dendrimers are ideal as active excipients, enhancing the solubility of poorly water-soluble drugs. The fact that the dendrimer’s properties are controllable during their synthesis render them promising agents for drug-delivery applications in several pharmaceutical formulations. Additionally, dendrimers can be used for reducing the drug toxicity and for the enhancement of the drug efficacy. This review aims to discuss the properties that turn dendrimers into pharmaceutical excipients and their potential applications in the pharmaceutical and biomedical fields.

scholarly journals Solubility enhancement of carvedilol using drug–drug cocrystallization with hydrochlorothiazide

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Shivarani Eesam ◽  
Jaswanth S. Bhandaru ◽  
Chandana Naliganti ◽  
Ravi Kumar Bobbala ◽  
Raghuram Rao Akkinepally
Keyword(s):  
Aqueous Solubility ◽  
Sem Analysis ◽  
Water Soluble ◽  
High Permeability ◽  
Poorly Water Soluble Drugs ◽  
Drug Discovery And Development ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Dissolution In Vitro

Abstract Background Increasing hydrophilicity of poorly water-soluble drugs is a major challenge in drug discovery and development. Cocrystallization is one of the techniques to enhance the hydrophilicity of such drugs. Carvedilol (CAR), a nonselective beta/alpha1 blocker, used in the treatment of mild to moderate congestive heart failure and hypertension, is classified under BCS class II with poor aqueous solubility and high permeability. Present work is an attempt to improve the solubility of CAR by preparing cocrystals using hydrochlorothiazide (HCT), a diuretic drug, as coformer. CAR-HCT (2:0.5) cocrystals were prepared by slurry conversion method and were characterized by DSC, PXRD, FTIR, Raman, and SEM analysis. The solubility, stability, and dissolution (in vitro) studies were conducted for the cocrystals. Results The formation of CAR-HCT cocrystals was confirmed based on melting point, DSC thermograms, PXRD data, FTIR and Raman spectra, and finally by SEM micrographs. The solubility of the prepared cocrystals was significantly enhanced (7.3 times), and the dissolution (in vitro) was improved by 2.7 times as compared to pure drug CAR. Further, these cocrystals were also found to be stable for 3 months (90 days). Conclusion It may be inferred that the drug–drug (CAR-HCT) cocrystallization enhances the solubility and dissolution rate of carvedilol significantly. Further, by combining HCT as coformer could well be beneficial pharmacologically too.

scholarly journals REVIEW ARTICLE: SOLUBILITY ENHANCEMENT BY SOLID DISPERSION

2017 ◽  
Vol 9 (3) ◽  
pp. 15
Author(s):  
A. N. Patil ◽  
D. M. Shinkar ◽  
R. B. Saudagar
Keyword(s):  
Solid Dispersion ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Full Potential ◽  
Drug Selection ◽  
Formulation Development ◽  
Poorly Water Soluble Drugs ◽  
New Chemical Entities ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

Enhancement of solubility, dissolution rate and bioavailability of the drug is a very challenging task in drug development, nearly 40% of the new chemical entities currently being discovered are poorly water soluble drugs. The solubility behaviour of the drugs remains one of the most challenging aspects in formulation development. This results in important products not reaching the market or not achieving their full potential. Solid dispersion is one of the techniques adopted for the formulation of such drugs and various methods are used for the preparation of solid dispersion. Solid dispersion is generally prepared with a drug which is having poor aqueous solubility and hydrophilic carrier. This article review various methods and concept of solid dispersion, criteria for drug selection, advantage and disadvantage, characterization, and application.

scholarly journals Enhancing the Oral Bioavailability of Candesartan Cilexetil Loaded Nanostructured Lipid Carriers: In Vitro Characterization and Absorption in Rats after Oral Administration

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1047
Author(s):  
Walid Anwar ◽  
Hamdy Dawaba ◽  
Mohsen Afouna ◽  
Ahmed Samy ◽  
Mohammed Rashed ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Candesartan Cilexetil ◽  
Aqueous Solubility ◽  
Systemic Circulation ◽  
Nanostructured Lipid Carriers ◽  
Water Soluble ◽  
Nanostructured Lipid Carrier ◽  
In Vitro Characterization ◽  
Water Soluble Drugs

Candesartan Cilexetil (CC) is a prodrug widely used in the treatment of hypertension and heart failure, but it has some limitations, such as very poor aqueous solubility, high affinity to P-glycoprotein efflux mechanism, and hepatic first-pass metabolism. Therefore, it has very low oral bioavailability. In this study, glyceryl monostearate (GMS) and Capryol™ 90 were selected as solid and liquid lipids, respectively, to develop CC-NLC (nanostructured lipid carrier). CC was successfully encapsulated into NLP (CC-NLC) to enhance its oral bioavailability. CC-NLC was formulated using a hot homogenization-ultrasonication technique, and the physicochemical properties were characterized. The developed CC-NLC formulation was showed in nanometric size (121.6 ± 6.2 nm) with high encapsulation efficiency (96.23 ± 3.14%). Furthermore, it appeared almost spherical in morphology under a transmission electron microscope. The surgical experiment of the designed CC-NLC for absorption from the gastrointestinal tract revealed that CC-NLC absorption in the stomach was only 15.26% of that in the intestine. Otherwise, cellular uptake study exhibit that CC-NLCs should be internalized through the enterocytes after that transported through the systemic circulation. The pharmacokinetic results indicated that the oral bioavailability of CC was remarkably improved above 2-fold after encapsulation into nanostructured lipid carriers. These results ensured that nanostructured lipid carriers have a highly beneficial effect on improving the oral bioavailability of poorly water-soluble drugs, such as CC.

scholarly journals Design and Characterization of Phosphatidylcholine-Based Solid Dispersions of Aprepitant for Enhanced Solubility and Dissolution

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 407
Author(s):  
Sooho Yeo ◽  
Jieun An ◽  
Changhee Park ◽  
Dohyun Kim ◽  
Jaehwi Lee
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Amorphous State ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Promising Alternative ◽  
Dispersion System ◽  
Enhanced Solubility ◽  
Water Soluble Drugs

This study aimed to improve the solubility and dissolution of aprepitant, a drug with poor aqueous solubility, using a phosphatidylcholine (PC)-based solid dispersion system. When fabricating the PC-based solid dispersion, we employed mesoporous microparticles, as an adsorbent, and disintegrants to improve the sticky nature of PC and dissolution of aprepitant, respectively. The solid dispersions were prepared by a solvent evaporation technique and characterized by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry, and X-ray powder diffraction. The FTIR results showed that aprepitant interacted with the PC carrier by both hydrogen bonds and van der Waals forces that can also be observed in the interaction between aprepitant and polymer carriers. The solid dispersions fabricated with only PC were not sufficient to convert the crystallinity of aprepitant to an amorphous state, whereas the formulations that included adsorbent and disintegrant successfully changed that of aprepitant to an amorphous state. Both the solubility and dissolution of aprepitant were considerably enhanced in the PC-based solid dispersions containing adsorbent and disintegrant compared with those of pure aprepitant and polymer-based solid dispersions. Therefore, these results suggest that our PC-based solid dispersion system is a promising alternative to conventional formulations for poorly water-soluble drugs, such as aprepitant.

scholarly journals Application of Hydrotropic Solubilization in Spectrophotometric Estimation of Lornoxicam from Tablets

2014 ◽  
Vol 2014 ◽  
pp. 1-4 ◽  
Author(s):  
Sindhu Abraham ◽  
Rajamanickam Deveswaran ◽  
Sharon Furtado ◽  
Srinivasan Bharath ◽  
Varadharajan Madhavan
Keyword(s):  
Aqueous Solubility ◽  
Cost Effective ◽  
Water Soluble ◽  
Alkaline Solutions ◽  
Primary Dysmenorrhoea ◽  
Cyclooxygenase 1 ◽  
Water Soluble Drugs ◽  
Label Claim ◽  
Poorly Water Soluble ◽  
Hydrotropic Agent

Lornoxicam is a selective cyclooxygenase-1 and cyclooxygenase-2 inhibitor that exhibits anti-inflammatory, analgesic, and antipyretic activities. It is used in osteoarthritis and rheumatoid arthritis; and in treatment of postoperative pain and primary dysmenorrhoea. Lornoxicam is completely insoluble in water but soluble in alkaline solutions. Hydrotropic solubilization is a technique used to increase the aqueous solubility of poorly water-soluble drugs and the present study was aimed at developing a hydrotropic technique to increase the solubility of lornoxicam, using 2 M sodium benzoate as the hydrotropic agent. Beer’s law was obeyed in the concentration range of 4–24 μg/mL at 381 nm. The solubility of lornoxicam in distilled water considerably increased with the addition of a hydrotropic agent. The analysis of tablets indicated good correlation between the amounts estimated and label claim. The LOD and LOQ of lornoxicam were found to be 0.34 μg/mL and 1.038 μg/mL, respectively, indicating good sensitivity of the proposed method. The percentage recovery was found to be 99.99%–100.21%. Thus the proposed method is new, simple, environmentally friendly, accurate, and cost effective and can be successfully employed in routine analysis of lornoxicam in tablets.

Effect of hydrotalcite-like compounds on the aqueous solubility of some poorly water-soluble drugs

2003 ◽  
Vol 92 (7) ◽  
pp. 1407-1418 ◽  
Author(s):  
Valeria Ambrogi ◽  
Giuseppe Fardella ◽  
Giuliano Grandolini ◽  
Morena Nocchetti ◽  
Luana Perioli
Keyword(s):  
Aqueous Solubility ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

scholarly journals A Short Review on Application of Liquisolid Technology

2021 ◽  
Vol 4 (1) ◽  
pp. 276-279
Author(s):  
Shaveta Sharma ◽  
Divya Sharma ◽  
Jyoti Singh
Keyword(s):  
Dissolution Rate ◽  
Aqueous Solubility ◽  
Short Review ◽  
Water Soluble ◽  
Water Soluble Drugs ◽  
Drug Involvement ◽  
Poorly Soluble ◽  
Flowing Powder ◽  
Soluble Liquid ◽  
New Formulation

In this paper we have surveyed about formulation and evaluation of Liquisolid formulations and its work in antidiabetics . Mostly poorly water soluble drugs are in research category despite of less dissolution rate and poor bioavailability. Solubility is a vital parameter to develop new formulation as industries faced serious issue regarding the poor aqueous solubility of the drugs. Various methods for solubility enhancement include modifications of the drug, involvement of co-solvents, complexation, salt formation, size reduction. A propitious technique to solve major challenges like solubility, dissolution rate and their bioavailability. This technique can be defined as the conversion of poorly soluble liquid medications into non-adherent, dry, compressible and free flowing powder mixtures with help of excipients. Many anti-diabetic drugs are belonging to BCS Class-II facing challenges like solubility and bioavailability.

Recent Advances in Nanosponges as Drug Delivery System

2013 ◽  
Vol 6 (1) ◽  
pp. 1934-1944 ◽  
Author(s):  
Uday B Bolmal ◽  
F V Manvi ◽  
Rajkumar Kotha ◽  
Sai Sowjanya Palla ◽  
Anusha Paladugu ◽  
...  
Keyword(s):  
Delivery System ◽  
Oral Delivery ◽  
Aqueous Solubility ◽  
The Body ◽  
Target Site ◽  
Water Soluble ◽  
Specific Target ◽  
Poor Solubility ◽  
Water Soluble Drugs ◽  
Important Character

Major problem of many newly developed chemical entities is their poor solubility in water and pharmacokinetic issues. These poorly-water soluble drugs show many problems in formulating them in conventional dosage forms and the critical problem associated is its very low bio-availability. Nanotechnology has attracted increasing attention during recent years and it can resolve the problems associated with solubility and bio-availability. Nanosponges are a part of nanotechnology. Nanosponges delivery system, which was originally developed for topical delivery of drugs, can also be used for controlled oral delivery of drugs using water soluble and bioerodible polymers. Nanosponges are tiny sponges with a size of about a virus, which can be filled with wide variety of drugs. These tiny sponges can circulate around the body until they encounter the specific target site and stick on the surface and begin to release the drug in a controlled and predictable manner. Because the drug can be released at the specific target site instead of circulating throughout the body it will be more effective for specific disease targeted treatment. Another important character of these sponges is their aqueous solubility; this allows the use of these systems effectively for drugs with poor solubility. 

Environment safe Method development and Validation of Dolutegravir in Bulk and Tablet dosage form by UV-Visible spectroscopy

2021 ◽  
pp. 139-144
Author(s):  
Poonam A. Borse Salunke ◽  
S.D. Barhate ◽  
Rupali S. Wagh
Keyword(s):  
Method Development ◽  
Aqueous Solubility ◽  
Solubility Enhancement ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Label Claim ◽  
Enhancement Method ◽  
Poorly Water Soluble ◽  
Tablet Dosage

To develop an environment-safe aqueous solubility enhancement method of poorly water-soluble drugs is the need of the pharmaceutical field. Because when organic solvents were used for solubility enhancement, there are many disadvantages like carcinogenicity, environment pollutant, flammable, toxicity, and cost. The hydrotropic method has been used to enhance the aqueous solubility of poorly water-soluble drugs. Dolutegravir is slightly soluble in water. To enhance aqueous solubility various hydrotropes were used and optimized the concentration of each hydrotrope. From these hydrotropes, a mixture of 10% sodium tricitrate and 10% sodium benzoate was selected because Dolutegravir was completely soluble in a mixed hydrotropic solution. Method development and analytical validation were performed. The maximum wavelength of Dolutegravir in the hydrotropic mixture was found a 268nm, and the linearity curve in the range of 5-25µg/ml. A regression coefficient was found to be 0.999. Percent label claim, accuracy (% RSD) were found 99.58%, 0.13(80%), 0.11(100%), 0.13(120%), respectively. The LOD for Dolutegravir was determined to be 0.037μg/ mL, and LOQ was found to be 0.11μg/mL.

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