scholarly journals A Comprehensive Review on the Drug: Fenofibrate

2021 ◽  
Vol 12 (3) ◽  
pp. 2164-2172
Author(s):  
Deepak Gunwal ◽  
Braham Dutt ◽  
Manjusha Choudhary ◽  
Vikas Budhwar
Keyword(s):  
Water Solubility ◽  
Degradation Products ◽  
Aqueous Solubility ◽  
Generic Medicine ◽  
Low Density ◽  
Fenofibric Acid ◽  
Ongoing Research ◽  
Bcs Class Ii ◽  
Humid Environment ◽  
Severe Hypertriglyceridemia

Fenofibrate is currently used as antihyperlipidemic drug, which has a direct effect on lowering cholesterol, triglycerides and LDL (Low-Density Lipids), VLDL (Very Low-Density Lipids) levels along with raising the level of HDL (High-density Lipids) in the blood. It also plays a significant role in insulin resistance metabolic disorder. This drug is mainly used for controlling diseases related to lipids like hypercholesterolemia, severe hypertriglyceridemia and dyslipidaemia. Along with statins, it significantly controls the level of hypercholesterolemia and hypertriglyceridemia. It belongs to the group of drugs called 'Fibrate'. Fenofibrate was patented in 1969. In 1974, it was synthesized as a derivative of clofibrate and launched at the French market. It was marketed in 1975. In 2017, it was available as a generic medicine. Presently this API is being marketed in around 85 countries all over the world. Fenofibrate is a BCS Class-II drug having poor water solubility. The poor aqueous solubility of this drug causes low bioavailability and limited permeability through the GIT membrane. This API degrades at higher temperatures and in a humid environment, with one of the resultant degradation products being fenofibric acid. In the present review, we have discussed the historical development, pharmacology, analytical profile with its physicochemical properties and ongoing research scenario on this API.

A Review on Formulation and Development of Solid Self-Nano Emulsifying Drug Delivery Systems

2021 ◽  
Vol 14 (4) ◽  
pp. 5519-5228
Author(s):  
Sunitha M Reddy ◽  
Sravani Baskarla
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Drug Loading ◽  
Aqueous Solubility ◽  
Delivery Systems ◽  
Particle Size Reduction

This article describes current strategies to enhance aqueous solubility and dissolution rate of poor soluble drugs. Most drugs in the market are lipophilic with low or poor water solubility. There are various methods to enhance solubility: co-solvency, particle size reduction, salt formation and Self Nanoemulsifying drug delivery systems, SEDDS is a novel approach to enhance solubility, dissolution rate and bioavailability of drugs. The study involves formulation and evaluation of solid self-Nano emulsifying drug delivery system (S-SNEDDS) to enhance aqueous solubility and dissolution rate. Oral route is the most convenient route for non-invasive administration. S-SNEDDS has more advantages when compared to the liquid self-emulsifying drug delivery system. Excipients were selected depends upon the drug compatibility oils, surfactants and co surfactants were selected to formulate Liquid SNEDDS these formulated liquid self-nano emulsifying drug delivery system converted into solid by the help of porous carriers, Melted binder or with the help of drying process. Conversion process of liquid to solid involves various techniques; they are spray drying; freeze drying and fluid bed coating technique; extrusion, melting granulation technique. Liquid SNEDDS has a high ability to improve dissolution and solubility of drugs but it also has disadvantages like incompatibility, decreased drug loading, shorter shelf life, ease of manufacturing and ability to deliver peptides that are prone to enzymatic hydrolysis.  

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.

Temperature Dependence of Degradation of Colored Oxo-Biodegradable Low-Density Polyethylene Films under Accelerated Thermal Aging

2017 ◽  
Vol 890 ◽  
pp. 82-85 ◽  
Author(s):  
Reymark D. Maalihan ◽  
Bryan B. Pajarito
Keyword(s):  
Thermal Aging ◽  
Degradation Products ◽  
Low Density Polyethylene ◽  
Effect Of Temperature ◽  
Low Density ◽  
Polyethylene Films ◽  
Hot Air ◽  
Taguchi Design Of Experiments ◽  
Oxidant Concentration ◽  
The Stability

This work reports the effect of temperature on degradation of colored low-density polyethylene (PE) films during thermal aging. Film samples were formulated according to Taguchi design of experiments where colorant, thickness, and pro-oxidant concentration were varied accordingly. Tensile properties of films were monitored with time during heat aging in a hot air oven at 50, 70, and 90 °C. Likewise, surfaces of aged films were analyzed to evaluate the degree of oxidation of PE during thermal aging. The Arrhenius equation was then used to predict the lifetime of PE at an in-use temperature of 30 °C. Results indicate that increasing the temperature reduces the tensile strength and modulus of films. Formation of carbonyl groups as degradation products is also observed at higher temperatures. Consequently, thermal aging at 90 °C offers the highest extent of degradation of exposed films. Regression analysis reveals that white films degrade at a higher rate than yellow and non-colored films. The presence of TiO2 in white films shortens the lifetime of PE while amine stabilizer in yellow films enhances the stability of PE during thermal aging.

scholarly journals Preclinical Evaluation of UDCA-Containing Oral Formulation in Mice for the Treatment of Wet Age-Related Macular Degeneration

Pharmaceutics ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 561 ◽  
Author(s):  
Maharjan ◽  
Kim ◽  
Jin ◽  
Ko ◽  
Song ◽  
...  
Keyword(s):  
Macular Degeneration ◽  
Oral Delivery ◽  
Water Solubility ◽  
Vision Loss ◽  
Oral Absorption ◽  
Aqueous Solubility ◽  
Oral Formulation ◽  
Preclinical Study ◽  
Age Related Macular Degeneration ◽  
Age Related

As a posterior ocular disease, wet age-related macular degeneration (WAMD) has been known to be related to vision loss, accompanying ocular complications. The intravitreous injection of VEGF antibodies has been reported to be an effective treatment to relieve symptoms of WAMD. However, the limitations of this treatment are high costs and invasiveness. For this reason, oral delivery route can be considered as a cost-effective way and the safest method to deliver drug molecules to the eyes. Accordingly, ursodeoxycholic acid (UDCA) was included in the oral formulation as the potential substance for the cure of WAMD in the animal model. Various pharmacological activities, such as antioxidant or anti-inflammatory effects, have been reported for UDCA and recent reports support the effects of UDCA in ocular treatment. However, due to poor water solubility and low pKa (around 5.0), it has been challenging to formulate aqueous solution of UDCA in the neutral pH range. In the present study, we confirmed the aqueous solubility of the oral UDCA formulation and performed a preclinical study, including pharmacokinetic profiling and WAMD model efficacy study in mice after oral administration of the drug solution. The results demonstrated that the formulation improved bioavailability of UDCA and efficiently delivered UDCA to the eye tissues after oral absorption. UDCA formulation was found to have inhibitory effects of choroidal neovascularization with a functional recovery in mice retinas. Taken together, our results suggest that the oral UDCA formulation could be used as a potent supplement for the cure of WAMD and related retinal diseases.

scholarly journals Efficient Degradation of Acesulfame by Ozone/Peroxymonosulfate Advanced Oxidation Process

Molecules ◽  
2019 ◽  
Vol 24 (16) ◽  
pp. 2874 ◽  
Author(s):  
Yu Shao ◽  
Zhicheng Pang ◽  
Lili Wang ◽  
Xiaowei Liu
Keyword(s):  
Hydroxyl Radical ◽  
Active Sites ◽  
Emerging Contaminants ◽  
Water Solubility ◽  
Advanced Oxidation Process ◽  
Negative Impact ◽  
Degradation Products ◽  
Electrical Energy ◽  
Sulfate Radical ◽  
Electrical Energy Per Order

Artificial sweeteners (ASWs), a class of emerging contaminants with good water solubility, have attracted much attention recently because of their wide use and negative impact on the aquatic environment and drinking water. Efficient technologies for removing ASWs are in urgent need. This study investigated degradation of typical ASW acesulfame by ozone-activated peroxymonosulfate process (O3/PMS) in prepared and real waters. O3/PMS can degrade >90% acesulfame in prepared water within 15 min at a low dosage of O3 (60 ± 5 µg∙min−1) and PMS (0.4 mM). Ozone, hydroxyl radical (HO•), and sulfate radical (SO4•−) were identified as contributors for ACE degradation and their contribution proportion was 27.1%, 25.4%, and 47.5% respectively. O3/PMS showed the best degradation performance at neutral pH and were sensitive to constituents such as chloride and natural organic matters. The qualitative analysis of degradation products confirmed the involvement of hydroxyl radical and sulfate radical and figured out that the active sites of ACE were the C=C bond, ether bond, and C-N bond. The electrical energy per order ACE degradation were calculated to be 4.6 kWh/m3. Our findings indicate that O3 is an efficient PMS activator and O3/PMS is promising due to its characteristic of tunable O3−HO• SO4•− ternary oxidant involving.

Central composite designed ezetimibe solid dispersion for dissolution enhancement: synthesis and in vitro evaluation

2019 ◽  
Vol 10 (10) ◽  
pp. 643-658 ◽  
Author(s):  
Neelam Sharma ◽  
Sukhbir Singh
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Solvent Evaporation ◽  
Dissolution Enhancement ◽  
Great Promise ◽  
Bcs Class Ii ◽  
Evaporation Technique ◽  
Central Composite

Aim: The current research is focused on increasing aqueous solubility and dissolution of BCS class II drug by using modified solvent evaporation technique to produce solid dispersions of ezetimibe (EZSD) using gelucire 50/13 and polyvinyl pyrollidone K30. Methodology & results: Central composite design analyzed the effect of gelucire 50/13 and polyvinyl pyrollidone K30 on the percentage of drug released in 5 and 30 min. Ezetimibe (EZ) aqueous saturation solubility (4.56 ± 0.94 μg/ml) was increased 25-fold in EZSD (115 ± 3.41 μg/ml). Cumulative drug release from EZ and optimized EZSD were observed 24.67 and 87.54% within 1 h, respectively. Conclusion: Manufacturing EZSD using modified solvent evaporation technique using rotary evaporator holds great promise for enhancing EZ's solubility and dissolution.

scholarly journals Physicochemical transfer of [3H]cholesterol from plasma lipoproteins to cultured human fibroblasts

1985 ◽  
Vol 228 (1) ◽  
pp. 219-225 ◽  
Author(s):  
B B Lundberg ◽  
L A Suominen
Keyword(s):  
Free Cholesterol ◽  
Water Solubility ◽  
Low Density Lipoprotein ◽  
Human Fibroblasts ◽  
Density Lipoprotein ◽  
Plasma Lipoproteins ◽  
Lung Fibroblasts ◽  
Cell Protein ◽  
Low Density ◽  
Free System

The transfer of free cholesterol from [3H]cholesterol-labelled plasma lipoproteins to cultured human lung fibroblasts was studied in a serum-free medium. The uptake of [3H]cholesterol depended upon time of incubation, concentration of lipoprotein in the medium, and temperature. Modified (reduced and methylated) low-density lipoprotein (LDL), which did not enter the cells by the receptor pathway, gave a somewhat lower transfer rate than unmodified LDL, but if the transfer values for native LDL were corrected for the receptor-mediated uptake of cholesterol the difference was eliminated. The initial rates of transfer of [3H]cholesterol from LDL and high-density lipoprotein (HDL) were of the same order of magnitude (0.67 +/- 0.05 and 0.75 +/- 0.06 nmol of cholesterol/h per mg of cell protein, respectively) while that from very-low-density lipoprotein (VLDL) was much lower (0.23 +/- 0.02 nmol of cholesterol/h per mg) (means +/- S.D., n = 5). The activation energy for transfer of cholesterol from reduced, methylated LDL to fibroblasts was determined to be 57.5 kJ/mol. If albumin was added to the incubation medium the transfer of [3H]cholesterol was enhanced, while that of [14C]dipalmitoyl phosphatidylcholine was decreased compared with the protein-free system. The results demonstrate that, in spite of its low water solubility, free cholesterol can move from lipoproteins to cellular membranes, probably by aqueous diffusion. We propose that physicochemical transfer of free cholesterol may be a significant mechanism for net uptake of the sterol into the artery during atherogenesis.

scholarly journals Molecular Encapsulation of Herbicide Terbuthylazine in Native and Modifiedβ-Cyclodextrin

2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
E. Manuela Garrido ◽  
Daniela Rodrigues ◽  
Nuno Milhazes ◽  
Fernanda Borges ◽  
Jorge Garrido
Keyword(s):  
Water Solubility ◽  
Analytical Techniques ◽  
Aqueous Solubility ◽  
Mean Values ◽  
H Nmr ◽  
Nmr Data ◽  
Kneading Method ◽  
Other Substances ◽  
The Mean ◽  
The Stability

The herbicide terbuthylazine (TBA) is widely used for preemergence or postemergence control of many grass and broadleaf weeds and has, besides other issues, a poor aqueous solubility profile that results in reduced bioavailability. Cyclodextrins and modified cyclodextrins were considered, among other substances, appropriate agents for improving pesticide water solubility. Therefore, the inclusion complex formation of terbuthylazine withβ-cyclodextrin (β-CD) and hydroxypropyl-β-cyclodextrin (HP-β-CD) was studied to attain its aqueous solubility enhancement. Their characterization was accomplished with different analytical techniques, namely, by UV-Vis, DSC, FTIR, and1H NMR. From the analysis of the complexation performance of the herbicide it was concluded that the interaction of terbuthylazine with CDs leads to the formation of inclusion complexes with a stoichiometry of 1 : 1. The association constants of the TBA/β-CD and TBA/HP-β-CD complexes were determined by UV. The mean values obtained for the stability constants are 460.4 ± 26.5 and 532.1 ± 27.6 to TBA/β-CD and TBA/HP-β-CD, respectively.1H NMR data corroborate the formation of the TBA/β-CD and TBA/HP-β-CD complexes synthesized by the kneading method. A formulation incorporating TBA cyclodextrin complexes might lead to an improvement in terbuthylazine bioavailability. The development of TBA-CD formulations may be interesting since it would enable, through their inclusion into the hydrophobic cavity of CDs, enhancement of solubility, bioavailability, and stability of the herbicide.

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