scholarly journals EMERGING TRENDS IN ORAL BIOAVAILABILITY ENHANCEMENT

2018 ◽  
Vol 1 (2) ◽  
pp. 20-38 ◽  
Author(s):  
S Talegaonkar ◽  
A Ahmad ◽  
M Tariq ◽  
Z.I. Khan ◽  
L.M. Negi ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Active Form ◽  
Oral Route ◽  
Low Permeability ◽  
Bioavailability Enhancement ◽  
Physiological Factors ◽  
Drug Molecules ◽  
Emerging Trends ◽  
Therapeutic Molecules ◽  
Low Solubility

Oral route is one of the most accepted and convenient mode of drug administration, however low oral bioavailability of many drugs is a major concern which limits their oral administration. Optimum solubility and permeation of a drug across the intestinal epithelium is a prerequisite to reach the systematic circulation in the active form for effective action at the desired site. Physicochemical properties of the drug, physiological factors and pharmacokinetic factors are mainly responsible for their low solubility, low permeability and high metabolism which in turn into low oral bioavailability of the drug molecules. In this review, various factors which affect bioavailability of drugs and possible approaches to overcome this problem have been discussed.  The review identifies various areas for research that can be focused for improving oral bioavailability of therapeutic molecules for different classes of drugs, thus making the oral route of administration of the drugs more effective and useful.

scholarly journals RECENT NANOCOCHLEATE DRUG DELIVERY SYSTEM FOR CANCER TREATMENT: A REVIEW

2019 ◽  
pp. 28-32
Author(s):  
SUJIT NAYEK ◽  
ABHIRAMI VENKATACHALAM ◽  
SANGEETA CHOUDHURY
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Divalent Cation ◽  
Technology Use ◽  
Oral Bioavailability ◽  
Anticancer Agent ◽  
Low Permeability ◽  
Delivery Mechanism ◽  
Low Solubility

Nanocochleates are at the forefront of the fast-growing nanotechnology sector in the delivery of drugs for cancer. This nanotechnology is the use of the cationic and anionic encapsulated drug that has poor oral bioavailability. Nanocochleate is a lipid-based drug delivery in the liposomal vesicles that is converted by calcium divalent cation into nanocochleate. Nanocochleates technology use encapsulations of the anticancer agent, which have low solubility, oral bioavailability and low permeability. This paper shows and provides an overview of the benefits of nanocochleates, drug delivery mechanism, choice of prevalent components (Phospholipids and Cations), various ways of producing nanocochleates and nanocochleate stability. Nanocochleates have far fewer constraints than other traditional carriers. To characterize nanocochleates, the suitable analytical methods are required. Therefore, in the therapy of cancer, nanocochleate becomes commonly applied and more prospective drug delivery system.

Nanonization of andrographolide by a wet milling method: the effects of vitamin E TPGS and oral bioavailability enhancement

RSC Advances ◽  
2016 ◽  
Vol 6 (103) ◽  
pp. 101404-101414 ◽  
Author(s):  
Ping Du ◽  
Qikun Jiang ◽  
Rujie Yang ◽  
Cuiru Liu ◽  
Yingchao Li ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Clinical Use ◽  
Wet Milling ◽  
Bioavailability Enhancement ◽  
Glycoprotein P ◽  
P Glycoprotein ◽  
Vitamin E Tpgs ◽  
Extensive Metabolism ◽  
Milling Method ◽  
Low Solubility

Andrographolide (AND) has wide prospects in clinical use, but suffers from the restriction of poor oral bioavailability, due to its low solubility, rapid and extensive metabolism and efflux by P-glycoprotein (P-gp).

scholarly journals Application of Cryo-Electron Microscopy on Drug Discovery

2021 ◽  
Vol 27 (S1) ◽  
pp. 3250-3250
Author(s):  
Viswanath Vittaladevaram ◽  
Kranthi Kuruti
Keyword(s):  
Electron Microscopy ◽  
Protein Complexes ◽  
Lead Discovery ◽  
Biologically Relevant ◽  
Biological Targets ◽  
3 Dimensional ◽  
Drug Molecules ◽  
Cryo Electron Microscopy ◽  
Therapeutic Molecules ◽  
Novel Drug

AbstractThe key aspect for development of novel drug molecules is to perform structural determination of target molecule associated with its ligand. One such tool that provides insights towards structure of molecule is Cryo-electron microscopy which covers biological targets that are intractable. Examination of proteins can be carried out in native state, as the samples are frozen at -175 degree Celsius i.e. cryogenic temperatures. In addition to this, there were no limits for molecular and functional structures of proteins that can be imagined in 3-dimensional form. This includes ligands which unravel mechanisms that are biologically relevant. This will enable to better understand the mechanisms that are used for development of new therapeutics. Application of Cryo-electron microscopy is not limited to protein complexes and is considered as non-specific. Intervention of Cryo-EM would allow to analyse the structures and also able to dissect the interaction with therapeutic molecules. The study determines the usage of cryo-EM for providing resolutions that are acceptable for lead discovery. It also provides support for lead optimization and also for discovery of vaccines and therapeutics.

scholarly journals Oral Bioavailability and Pharmacokinetics of Trovafloxacin in Patients with AIDS

1999 ◽  
Vol 43 (12) ◽  
pp. 3005-3007 ◽  
Author(s):  
Melinda K. Lacy ◽  
David P. Nicolau ◽  
Charles H. Nightingale ◽  
Amy Geffken ◽  
Renli Teng ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Active Form ◽  
Healthy Adults ◽  
Absolute Bioavailability ◽  
Randomized Design ◽  
The Mean

ABSTRACT Trovafloxacin pharmacokinetics were evaluated in 12 subjects with AIDS. By using a randomized design, single 200-mg doses of oral trovafloxacin and intravenous alatrofloxacin were administered. The mean absolute bioavailability was 91%. The pharmacokinetics of trovafloxacin when administered orally as the active form or intravenously as the prodrug (alatrofloxacin) are not altered in subjects with AIDS compared to those in healthy adults.

scholarly journals Preparation, characterization and featuring of an inclusion complex of nerol with β-cyclodextrin

2017 ◽  
Vol 5 (2) ◽  
pp. 195
Author(s):  
Mayara Coêlho ◽  
Herlane Da Silva ◽  
Muhammad Islam ◽  
Vicente Viana ◽  
Ana Amélia Melo-Cavalcante
Keyword(s):  
Inclusion Complex ◽  
Inclusion Complexes ◽  
Biological Activities ◽  
Aqueous Media ◽  
Limiting Factor ◽  
Thermo Gravimetric ◽  
Drug Molecules ◽  
Complex Cavity ◽  
Nonpolar Molecules ◽  
Low Solubility

Nerol is an acyclic type monoterpene with important biological activities. However, the low solubility in aqueous media is a limiting factor for its user. Cyclodextrins have been widely used in order to improve the solubility, stability and bioavailability of nonpolar molecules through the formation of inclusion complexes. Thus, the present study consists in the development of nerol inclusion complex in combination with the β-cyclodextrin (β-CD) followed by characterizing by thermal analysis and spectrophotometric absorption in the infrared (FTIR). The results suggest a complexation of nerol with β-CD having detours and changed the intensity of various bands. The thermo gravimetric curve of CI found to indicate an output of solvating water molecules from the complex cavity formed for replacement of drug molecules probably included. Thus, it is concluded a possibility to obtain inclusion complexes of nerol monoterpene with β-CD, which will increase its solubility and facilitate delivery process.

Preparation, Characterization and Optimization of Irbesartan Loaded Solid Lipid Nanoparticles for Oral Delivery

2021 ◽  
pp. 97-104
Author(s):  
Kumara Swamy S ◽  
Ramesh Alli
Keyword(s):  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Oral Bioavailability ◽  
Oral Delivery ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Sustained Drug Release ◽  
Bioavailability Enhancement ◽  
Solid Lipid

The purpose of this study was to develop and evaluate irbesartan (IS) loaded solid lipid nanoparticles (SLNs; IS-SLNs) that might enhance the oral bioavailability of IS. IS, an angiotensin-receptor antagonist, used to treat hypertension. However, poor aqueous solubility and poor oral bioavailability has limited therapeutic applications of IS. Components of the SLNs include either of trimyristin/tripalmitin/tristearin/trilaurate/stearic acid/beeswax, and surfactants (Poloxamer 188 and soylecithin). The IS-SLNs were prepared by hot homogenization followed by ultrasonication method and evaluated for particle size, poly dispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE), drug content and in vitro drug release. The physical stability of optimized formulation was studied at refrigerated and room temperature for two months. The optimized IS-SLN formulation (F4) had a mean diameter of about 217.6±3.62 nm, PDI of 0.163±0.032, ZP of -28.5±4.12, assay of 99.8±0.51 and EE of 93.68±2.47%. The formulation showed sustained drug release compared with control formulation over 24 h. Optimized formulation was found to be stable over two months. IS-SLN showed nearly spherical in shape using and converted to amorphous form by DSC. Thus, the results conclusively demonstrated SLNs could be considered as an alternative delivery system for the oral bioavailability enhancement of IS.

Accessing the Blood-Brain Barrier to Treat Brain Disorders

2019 ◽  
Vol 9 (3) ◽  
pp. 198-209
Author(s):  
M. Sureshkumar ◽  
A. Pandian
Keyword(s):  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Low Molecular Weight ◽  
Brain Disorders ◽  
Permeable Membrane ◽  
Drug Molecules ◽  
Blood Brain ◽  
Therapeutic Molecules ◽  
Pass Through ◽  
The Brain

: Crossing the blood-brain barrier (BBB) and treating brain disorders by delivering therapeutic agents to specific regions of the brain is a challenge. The BBB, naturally evolved, protective physiological barrier acts as a selective permeable membrane in such a way that it allows only nonionic molecules and molecules of low molecular weight to pass through. Treating brain tumor has become a great challenge as the drug molecules of larger size are not able to cross the BBB and reach the target site. The incompetence of techniques for brain-specific delivery of therapeutic molecules has led researchers to increasingly explore the diagnosis and treatment of disorders incurable with present techniques. This article is to discuss the various techniques or methods to deliver drugs to the brain crossing the BBB.

scholarly journals Prodrugs of NSAIDs: A Review

2017 ◽  
Vol 11 (1) ◽  
pp. 146-195 ◽  
Author(s):  
Kamal Shah ◽  
Jeetendra K. Gupta ◽  
Nagendra S. Chauhan ◽  
Neeraj Upmanyu ◽  
Sushant K. Shrivastava ◽  
...  
Keyword(s):  
Active Drug ◽  
Pharmacological Action ◽  
Patient Acceptance ◽  
Synergistic Activity ◽  
Bioavailability Enhancement ◽  
Drug Molecules ◽  
Presystemic Metabolism ◽  
Pass Through ◽  
Reduced Toxicity ◽  
Mutual Prodrug

Intoroduction:Prodrug approach deals with chemical biotransformation or enzymatic conversion or involves inactive or less active bio-reversible derivatives of active drug molecules. They have to pass through enzymatic or chemical biotransformation before eliciting their pharmacological action.Methods & Materials:The two different pharmacophores combine to give synergistic activity or may help in targeting the active drug to its target. Prodrug super seeds the problems of prodrug designing, for example solubility enhancement, bioavailability enhancement, chemical stability improvement, presystemic metabolism, site specific delivery, toxicity masking, improving patient acceptance, or eradicating undesirable adverse effects.Results:As an outcome the search for a prodrug or mutual prodrug with reduced toxicity has continued during recent years. This present review emphasizes the common help to revamp physiochemical, pharmaceutical and therapeutic effectiveness of drugs.Conclusion:This gives the researcher a common platform where they can find prodrugs of commonly used NSAIDs to overcome the gastrointestinal toxicity (irritation, ulcergenocity and bleeding).

scholarly journals Levers to Improve Antibiotic Treatment of Lambs via Drinking Water in Sheep Fattening Houses: The Example of the Sulfadimethoxine/Trimethoprim Combination

Antibiotics ◽  
2020 ◽  
Vol 9 (9) ◽  
pp. 561
Author(s):  
Aude A. Ferran ◽  
Marlène Z. Lacroix ◽  
Alain Bousquet-Mélou ◽  
Ivain Duhil ◽  
Béatrice B. Roques
Keyword(s):  
Drinking Water ◽  
Oral Bioavailability ◽  
Half Life ◽  
Plasma Concentrations ◽  
Oral Route ◽  
Disease Spread ◽  
Bacterial Diseases ◽  
Terminal Half Life ◽  
High Interindividual Variability ◽  
The Individual

To limit the spread of bacterial diseases in sheep fattening houses, antibiotics are often administered collectively. Collective treatments can be delivered by drinking water but data on the drug’s solubility in water or on plasma exposure of the animals are lacking. We first assessed the solubility of products containing sulfadimethoxine (SDM), associated or not with trimethoprim (TMP), in different waters. We then compared in lambs the SDM and TMP pharmacokinetic profiles after individual intravenous (IV) and oral administrations of SDM-TMP in experimental settings (n = 8) and after a collective treatment by drinking water with SDM-TMP or SDM alone in a sheep fattening house (n = 100 for each treatment). The individual water consumption during the collective treatments was also monitored to characterize the ingestion variability. We showed that TMP had a short terminal half-life and very low oral bioavailability, demonstrating that it would be unable to potentiate SDM by oral route. Conversely, SDM had a long terminal half-life of 18 h and excellent oral bioavailability. However, delivery by drinking water resulted in a very high interindividual variability of SDM plasma concentrations, meaning that although disease spread could be controlled at the group level, some individuals would inevitably be under- or over-exposed to the antibiotic.

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