scholarly journals A SYSTEMATIC REVIEW ON SELF-MICRO EMULSIFYING DRUG DELIVERY SYSTEMS: A POTENTIAL STRATEGY FOR DRUGS WITH POOR ORAL BIOAVAILABILITY

2019 ◽  
Vol 11 (1) ◽  
pp. 23
Author(s):  
G V Radha ◽  
K Trideva Sastri ◽  
Sadhana Burada ◽  
Jampala Rajkumar
Keyword(s):  
Biological Effects ◽  
Water Soluble ◽  
Lipophilic Compounds ◽  
Solid Dosage ◽  
Drug Molecules ◽  
Dynamic Strategy ◽  
Lipid System ◽  
Potential Strategy ◽  
Lipid Excipients ◽  
Optimum Formula

Currently a marked interest in developing lipid-based formulations to deliver lipophilic compounds. Self-emulsifying system has emerged as a dynamic strategy for delivering poorly water-soluble compounds. These systems can embrace a wide variety of oils, surfactants, and co-solvents. An immediate fine emulsion is obtained on exposure to water/gastro-intestinal fluids. The principal interest is to develop a robust formula for biopharmaceutical challenging drug molecules. Starting with a brief classification system, this review signifies diverse mechanisms concerning lipid-based excipients besides their role in influencing bioavailability, furthermore pertaining to their structured formulation aspects. Consecutive steps are vital in developing lipid-based systems for biopharmaceutical challenging actives. Such a crucial structured development is critical for achieving an optimum formula. Hence lipid excipients are initially scrutinized for their solubility and phase behavior, along with biological effects. Blends are screened by means of simple dilution test and are consequently studied with more advanced biopharmaceutical tests. After discerning of the principle formula, diverse technologies are offered to incorporate the fill-mass either in soft/hard gelatin capsules. There is also feasibility to formulated lipid-system as a solid dosage form. Although such solid technologies are desirable but such should not undermine the biopharmaceutical potential of lipid-formulations.

Development of Solid-Self Micron Emulsifying Drug Delivery Systems

2013 ◽  
Vol 6 (2) ◽  
pp. 2014-2021
Author(s):  
Preethi Sudheer ◽  
Koushik Y ◽  
Satish P ◽  
Uma Shankar M S ◽  
R S Thakur
Keyword(s):  
Drug Delivery ◽  
Systemic Circulation ◽  
Water Soluble ◽  
Future Research ◽  
Steady Increase ◽  
Liquid Form ◽  
Lipophilic Compounds ◽  
Modern Drug ◽  
Pharmaceutical Scientist ◽  
Pharmacologically Active

As a consequence of modern drug discovery techniques, there has been a steady increase in the number of new pharmacologically active lipophilic compounds that are poorly water soluble and solubility is one of the most important parameter to achieve desired concentration of drug in systemic circulation for therapeutic response. It is a great challenge for pharmaceutical scientist to convert those molecules into orally administered formulation with sufficient bioavailability.  Among the several approaches to improve oral bioavailability of these molecules, Self-micron emulsifying drug delivery system (SMEDDS) is one of the approaches usually used to improve the bioavailability of hydrophobic drugs. However, conventional SMEDDS are mostly prepared in a liquid form, which can have several disadvantages. Accordingly, solid SMEDDS (S-SMEDDS) prepared by solidification of liquid/semisolid self-micron emulsifying (SME) ingredients into powders have gained popularity. This article provides an overview of the recent advancements in S-SMEDDS such as methodology, techniques and future research directions.

Acidic Aqueous Extraction of Hypothalamic Luteinizing Hormone Releasing Hormone to Study Biological Effects

1974 ◽  
Vol 52 (3) ◽  
pp. 754-758 ◽  
Author(s):  
S. H. Shin ◽  
C. J. Howitt
Keyword(s):  
Luteinizing Hormone ◽  
Biological Effects ◽  
Extraction Procedure ◽  
Extraction Methods ◽  
Water Soluble ◽  
Acid Extraction ◽  
Luteinizing Hormone Releasing Hormone ◽  
Releasing Hormone ◽  
Aqueous Solvent ◽  
Lh Rh

Several aqueous solvent systems were tested for their efficiency in extracting luteinizing hormone releasing hormone (LH-RH) from rat hypothalamus. Although LH-RH is a water-soluble decapeptide, neutral distilled water extracted only 10% of the LH-RH obtained using acid extraction methods. The efficiency of the acid extraction procedure suggests that in the hypothalamus the releasing hormone is bound to a relatively large molecular weight compound. Using the acidic extraction procedure, we found that hypothalamic LH-RH content is significantly lower in the castrated animal than in the normal rat.

scholarly journals Solid Dispersions : An Approach to Enhance the Bioavailability of Poorly Water-Soluble Drugs

2013 ◽  
pp. 37-46
Author(s):  
Sanjoy Kumar Das
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Historical Background ◽  
Solid Dosage ◽  
Advantages And Disadvantages ◽  
Water Soluble Drugs ◽  
Inert Carrier ◽  
Dispersion Technique

Improving oral bioavailability of drugs those given as solid dosage forms remains a challenge for the formulation scientists due to solubility problems. The dissolution rate could be the rate-limiting process in the absorption of a drug from a solid dosage form of relatively insoluble drugs. Therefore increase in dissolution of poorly soluble drugs by solid dispersion technique presents a challenge to the formulation scientists. Solid dispersion techniques have attracted considerable interest of improving the dissolution rate of highly lipophilic drugs thereby improving their bioavailability by reducing drug particle size, improving wettability and forming amorphous particles. The term solid dispersion refers to a group of solid products consisting of at least two different components, generally a hydrophilic inert carrier or matrix and a hydrophobic drug. This article reviews historical background of solid dispersion technology, limitations, classification, and various preparation techniques with its advantages and disadvantages. This review also discusses the recent advances in the field of solid dispersion technology. Based on the existing results and authors’ reflection, this review give rise to reasoning and suggested choices of carrier or matrix and solid dispersion procedure.

Encapsulation of lipid-based formulations in porous carriers for controlled drug delivery

2021 ◽  
Vol 28 ◽  
Author(s):  
Phuong H.L. Tran ◽  
Thao T.D. Tran
Keyword(s):  
Porous Materials ◽  
Controlled Drug Release ◽  
Water Soluble ◽  
Solid Dosage Forms ◽  
Pharmaceutical Ingredients ◽  
Solid Dosage ◽  
Water Soluble Drugs ◽  
Porous Carriers ◽  
Poorly Water Soluble ◽  
And Control

: Lipid-based formulations have recently been investigated as a promising approach to enhance the bioavailability of drugs, especially poorly water-soluble drugs. The encapsulation of lipid-based formulations in porous materials can result in a transformation of liquids or semisolid forms to solid dosage forms. Moreover, the specific structure of porous carriers could offer an enhanced ability to load and control active pharmaceutical ingredients. Although there have been prominent reports on lipid-based formulations and porous materials as promising technologies for controlled drug release, the overall methods of encapsulating lipid-based formulations need to be discussed for further formulation investigations. This review aims to present the key strategies used for producing porous carriers containing lipid-based formulations. We also discuss methods that enhance the encapsulation efficiency of loaded drugs within porous structures (instead of lipid-based formulations). Moreover, the critical factors that affect tablet formation are outlined. This overview of lipid-based formulations encapsulated within porous materials provides a summary of the technical methods used in the development of these formulations and their clinical translation.

scholarly journals Fruit Seeds as Sources of Bioactive Compounds: Sustainable Production of High Value-Added Ingredients from By-Products within Circular Economy

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3854 ◽  
Author(s):  
Fidelis ◽  
Moura ◽  
Kabbas Junior ◽  
Pap ◽  
Mattila ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Circular Economy ◽  
Raw Materials ◽  
Scale Up ◽  
Sustainable Use ◽  
Value Added ◽  
Water Soluble ◽  
Lipophilic Compounds

The circular economy is an umbrella concept that applies different mechanisms aiming to minimize waste generation, thus decoupling economic growth from natural resources. Each year, an estimated one-third of all food produced is wasted; this is equivalent to 1.3 billion tons of food, which is worth around US$1 trillion or even $2.6 trillion when social and economic costs are included. In the fruit and vegetable sector, 45% of the total produced amount is lost in the production (post-harvest, processing, and distribution) and consumption chains. Therefore, it is necessary to find new technological and environmentally friendly solutions to utilize fruit wastes as new raw materials to develop and scale up the production of high value-added products and ingredients. Considering that the production and consumption of fruits has increased in the last years and following the need to find the sustainable use of different fruit side streams, this work aimed to describe the chemical composition and bioactivity of different fruit seeds consumed worldwide. A comprehensive focus is given on the extraction techniques of water-soluble and lipophilic compounds and in vitro/in vivo functionalities, and the link between chemical composition and observed activity is holistically explained.

scholarly journals Riboflavin: The Health Benefits of a Forgotten Natural Vitamin

2020 ◽  
Vol 21 (3) ◽  
pp. 950 ◽  
Author(s):  
Nittiya Suwannasom ◽  
Ijad Kao ◽  
Axel Pruß ◽  
Radostina Georgieva ◽  
Hans Bäumler
Keyword(s):  
Protective Effect ◽  
Toxic Effect ◽  
Biological Effects ◽  
Health Benefits ◽  
Water Soluble ◽  
Medical Conditions ◽  
Protective Properties ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
B Vitamin

Riboflavin (RF) is a water-soluble member of the B-vitamin family. Sufficient dietary and supplemental RF intake appears to have a protective effect on various medical conditions such as sepsis, ischemia etc., while it also contributes to the reduction in the risk of some forms of cancer in humans. These biological effects of RF have been widely studied for their anti-oxidant, anti-aging, anti-inflammatory, anti-nociceptive and anti-cancer properties. Moreover, the combination of RF and other compounds or drugs can have a wide variety of effects and protective properties, and diminish the toxic effect of drugs in several treatments. Research has been done in order to review the latest findings about the link between RF and different clinical aberrations. Since further studies have been published in this field, it is appropriate to consider a re-evaluation of the importance of RF in terms of its beneficial properties.

Bio-Functionalization of Carbon Nanotubes and Intracellular Imaging

2015 ◽  
Vol 799-800 ◽  
pp. 471-474
Author(s):  
Jun Li ◽  
Yao Dong Dai
Keyword(s):  
Carbon Nanotubes ◽  
Laser Scanning ◽  
Water Solubility ◽  
Covalent Bond ◽  
Fluorescein Isothiocyanate ◽  
Water Soluble ◽  
Intracellular Imaging ◽  
Drug Molecules ◽  
Functionalization Of Carbon Nanotubes ◽  
Walled Carbon Nanotubes

Shortened single walled carbon nanotubes (SWNTs) were functionalized with chitosan (CS) oligomer to improve their water solubility and biocompatibility. The functional groups such as amino in CS benefit the further modification of other bio-functional molecules. Fluorescein isothiocyanate (FITC) were marked in CS decorated SWNTs through covalent bond for imaging and tracking SWNTs. Water soluble SWNTs wrapped by CS could also be suitable for drug delivery. Tea polyphenol (TP) and doxorubicin (DOX) drug molecules were loaded in the SWNTs system respectively through hydrogen bond and π-π interaction. The FITC labeled CS/SWNTs were co-incubated with cells and imaged under laser scanning confocal microscope (LSCM). With proper bio-functionalization, SWNTs could be easily internalized by cells via endocytosis.

scholarly journals Hydroxysafflor Yellow A: A Promising Therapeutic Agent for a Broad Spectrum of Diseases

2018 ◽  
Vol 2018 ◽  
pp. 1-17 ◽  
Author(s):  
Hui Ao ◽  
Wuwen Feng ◽  
Cheng Peng
Keyword(s):  
Broad Spectrum ◽  
Biological Effects ◽  
Carthamus Tinctorius ◽  
Water Soluble ◽  
Systemic Review ◽  
Pharmacological Effects ◽  
Hydroxysafflor Yellow A ◽  
Cell Protection ◽  
Lung Protection ◽  
Metabolism Regulation

Hydroxysafflor yellow A (HSYA) is one of the major bioactive and water-soluble compounds isolated from Carthami Flos, the flower of safflower (Carthamus tinctorius L.). As a natural pigment with favorable medical use, HSYA has gained extensive attention due to broad and effective pharmacological activities since first isolation in 1993. In clinic, the safflor yellow injection which mainly contains about 80% HSYA was approved by the China State Food and Drug Administration and used to treat cardiac diseases such as angina pectoris. In basic pharmacology, HSYA has been proved to exhibit a broad spectrum of biological effects that include, but not limited to, cardiovascular effect, neuroprotection, liver and lung protection, antitumor activity, metabolism regulation, and endothelium cell protection. Although a great number of studies have been carried out to prove the pharmacological effects and corresponding mechanisms of HYSA, a systemic review of HYSA has not yet been seen. Here, we provide a comprehensive summarization of the pharmacological effects of HYSA. Together with special attention to mechanisms of actions, this review can serve as the basis for further researches and developments of this medicinal compound.

Antioxidant Activity and Toxicity of Fullerenols with Different Number of Hydroxyl Substituents

2018 ◽  
Author(s):  
Ekaterina Kovel ◽  
Anna Sachkova ◽  
Natalia Vnukova ◽  
Grigoriy Churilov ◽  
Elena Knyazeva ◽  
...  
Keyword(s):  
Reactive Oxygen Species ◽  
Antioxidant Activity ◽  
Biological Effects ◽  
Reactive Oxygen ◽  
Water Soluble ◽  
Oxygen Species ◽  
Allotropic Form ◽  
Oxygen Groups ◽  
Pharmaceutical Agents ◽  
Derivatives Of

Fullerenols are nanosized water-soluble polyhydroxylated derivatives of fullerenes, specific allotropic form of carbon, bioactive compounds and perspective pharmaceutical agents. We studied biological effects of a series of fullerenols. Antioxidant activity and toxicity of the fullerenols were compared using bioluminescence assays (cellular and enzymatic); a content of Reactive Oxygen Species in fullerenol solutions was determined using chemiluminescence luminol method. Two groups of fullerenols with different number of hydroxyl substituents were under investigation: (I) С60Оy(OH)x, С60,70Оy(OH)x, where х+у=24–28 and (II) С60,70Оy(OH)x, Fe0,5С60Оy(OH)x, where х+у=40–42. Toxicity of the fullerenols was evaluated using effective concentrations ЕС50. Fullerenol’ antioxidant activity was investigated in model solutions of organic toxicant of oxidative type, 1,4-benzoquinone. Detoxification coefficients were calculated to analyze and compare the antioxidant activity. Higher toxicity and lower antioxidant activity were demonstrated in the solutions of fullerenols with higher number of the oxygen substituents (х+у=40–42). The differences were concerned with fullerenol’ ability to disturb Reactive Oxygen Species balance in aqueous solutions. Toxic effect of the prospective endohedral metal-fullerenol with gadolinium atom involved, Gd@C82Oy(OH)x, where х+у=40–42, was evaluated and explained by a high number of oxygen groups

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