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An overview of techniques for multifold enhancement in solubility of poorly soluble drugs Mohammad Javed Ansari

Poor water solubility of newly discovered compounds has become the most common challenge in the drug development process. Indeed, poor solubility is considered as the root cause of failure of drug during drug development phases. Moreover, it has also been reported to be the main reason for bioavailability issues such as poor, inconsistent, incomplete and highly variable bioavailability of the marketed products. As per an estimate, approximately 90% of drug molecules suffer with poor water solubility at early stage and approximately 40% of the marketed drugs have bioavailability problems mainly due to poor water solubility. Solubility enhancement of the newly discovered compounds is primary research area for the pharmaceutical industries and research institutions. The conventional techniques to improve aqueous solubility of drugs employ salt formation, prodrug formation, co-crystallization, complexation, amorphous solid dispersion and use of co-solvent, surfactants or hydrotropic agents. Current advancement in the science and technology has enabled the use of relatively new techniques under the umbrella of nanotechnology. These include the development of nanocrystals, nanosuspensions, nanoemulsions, microemulsions, liposomes and nanoparticles to enhance the solubility. This review focuses on the conventional and current approaches of multifold enhancement in the solubility of poorly soluble marketed drugs, including newly discovered compounds.

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Influence of chitosan coating on the oral bioavailability of gold nanoparticles in rats Mohammad Javed Ansari

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Gold nanoparticles are one of the most extensively investigated metallic nanoparticles for several applications. It is less toxic than other metallic nanolattices. The exceptional electrical and thermal conductivity of gold make it possible to be administered as non-invasive radiofrequency irradiation therapy that produces sufficient heat to kill tumor cells. Nanoparticles are generally administered intravenously instead of orally due to negligible oral absorption and cellular uptake. This study evaluated the oral bioavailability of gold nanoparticles coated with chitosan (C-AuNPs), a natural mucoadhesive polymer. We employed traditional method of evaluating bioavailability that involve estimation of maximum concentrations and area under the curve of 3 nm chitosan coated gold nanoparticles (C-AuNPs) in the rat plasma following intravenous and oral administrations (0.8 mg and 8 mg/kg body weight respectively). The oral bioavailability of C-AuNPs was found to be 2.46% (approximately 25 folds higher than polyethylene glycol (PEG) coated gold nanoparticles, reported earlier). These findings suggest that chitosan coating could be better than PEG coating for the enhancement of oral bioavailability of nanoparticles.

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Enhanced Oral Bioavailability of Ibrutinib Encapsulated Poly (Lactic-co- Glycolic Acid) Nanoparticles: Pharmacokinetic Evaluation in Rats Mohammad Javed Ansari
Abstract:

Background: The poor oral bioavailability of newly discovered chemical entities and marketed formulations are usually related to poor aqueous solubility or poor permeability, leading to drug failure in the development phases or therapeutic failure in a clinical setting. However, advancement in drug formulations and delivery technologies have enabled scientists to improve the bioavailability of formulations by enhancing solubility or permeability.

Objective: This study reports the enhancement of the oral bioavailability of ibrutinib (IBR), a poorly soluble anticancer drug in Wistar albino rats.

Methods: IBR loaded nanoparticles were formulated through the nanoprecipitation method by utilizing poly lactide-co-glycolide (PLGA) as a safe, biodegradable and biocompatible polymer, and poloxamer or pluronic 127 as a stabilizer. Animals were administered with a dose of 10 mg/kg of IBR suspension or an equivalent amount of IBR loaded nanoparticles. Plasma samples were extracted and analyzed by state of the art UPLC-MS/MS technique. Pharmacokinetic (PK) parameters and bioavailability were calculated by non-compartmental analysis.

Results: There was an approximately 4.2-fold enhancement in the oral bioavailability of IBR-loaded nanoparticles, as compared to the pure IBR suspension. The maximum plasma concentration (Cmax; 574.31 ± 56.20 Vs 146.34 ± 5.37 ng/mL) and exposure (AUC; 2291.65 ± 263.83 vs 544.75 ± 48.33 ng* h/mL) of IBR loaded nanoparticles were significantly higher than those exhibited through pure IBR suspension.

Conclusion: The outcomes of the present study suggested the potential of PLGA nanoparticles in the enhancement of bioavailability and the therapeutic efficacy of IBR.

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Transport Phenomenon of Nanoparticles in Animals and Humans Mohammad Javed Ansari

Nanoparticles (NPs) are microscopic objects with at least one dimension less than 100 nm. These were first discovered by Michael Faraday in 1857 when he prepared gold nanoparticles and observed that nanostructured gold produced red color. This distinct feature of nanoparticles could be due to very small size. NPs are very small compared to the wavelengths of light, hence absorb light in the blue-green portion of the spectrum (~450 nm) and reflect the red light (~700 nm) thus yield a rich red color. NPs also possess very high surface to mass ratio that could be utilized in several application areas wherein a very high surface area is required. Nanoparticles witnessed tremendous growth in research and application areas especially in medicine in twentieth century after discovery of carbon nanotubes in 1991. Nanoparticles have been explored in medicine as targeted delivery carriers to deliver macromolecules such as proteins, enzymes, to the target organ up to cellular levels. Of late, these carriers have been employed to treat several tumors owing to its capacity to deliver chemotherapeutic agents to the tumor cells only thus improving efficacy and minimizing side effects of anticancer agents.

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Nano-encapsulation and characterization of baricitinib using poly-lactic-glycolic acid co-polymer Mohammad Javed Ansari

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Baricitinib is a recently approved anti-rheumatic drug having very poor aqueous solubility and hence its performance suffers from low or inconsistent oral bioavailability. The purpose of the study was to develop and evaluate poly lactic-co-glycolic acid (PLGA) nanoparticles of baricitinib in order to enhance in vitro dissolution and performance. Nano-suspension of baricitinib with or without PLGA, a biodegradable, FDA approved semi-synthetic polymer, was developed by nanoprecipitation method. Research methodology employed a quantitative research utilizing experimental design wherein effect of independent variables such as amount of polymer, drug: polymer ratio, types of solvent, and solvent: anti-solvent ratio were evaluated over the size and size distribution of nanoparticles along with entrapment efficiencies. Among the several organic phases evaluated, acetone was found to be suitable solvent for drug and polymer. The aqueous phase (anti-solvent) was deionized water containing 1% w/v إقرأ المزيد

Influences of Ferulic Acid on Pharmacokinetics of Carbamazepine in Rats: Possible Mechanism of Herb/food-drug Interactions Mohammad Javed Ansari

Background and Objective: Carbamazepine (CBZ), an antiepileptic drug, possesses pharmacokinetic properties that make it susceptible to interaction with co-administered ingredients, such as dietary and herbal supplements and drugs. Ferulic acid (FA) possesses anti-epileptogenic, antidepressant and antioxidant activity and is used as adjuvant therapy for epilepsy. In this study, we evaluated the effects of concomitant administration of FA on CBZ pharmacokinetics and explored a possible interaction mechanism. Materials and Methods:Rats received a single CBZ dose (80 mg kg–1 orally [p.o.]) with and without pretreatment with FA (40 mg kg–1 p.o. every day for 7 days). Plasma CBZ levels were determined using a reversed-phase-high performance liquid chromatography bioassay. Pharmacokinetic parameters were estimated using non-compartmental analysis. Results: Following pretreatment with FA, CBZ exhibited increases in area under concentration-time curve (AUC0-t) (100.32%), half-life (T1/2) (212%) and mean residence time (MRT) (180%) compared with the group treated with CBZ alone (pbioavailability of CBZ was accompanied by down regulated expression of cytochrome (CYP) 3A2, CYP2C11 and permeability-glycoprotein 1 (P-gp 1) (also known as multidrug resistance 1 [MDR1]) at the protein level in hepatic and intestinal tissues and increased intestinal absorption. Conclusion: The study findings indicate that metabolic inhibition of CYP450 and P-gP (MDR1) leads to a reduced rate of CBZ elimination and interactions with FA in the intestine. Therefore, patients who receive concomitant administration of FA and CBZ should be monitored carefully.

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A Brief Review on the Principles of Human Cadaver Preservation and Monitoring of Microbial Degradation المعتصم عثمان أحمد

Putrefaction and decay of preserved cadaver and body parts is one of the major issues that the faculties of medicines in various third world countries are facing. In this study we focus on the meaning of body preservation, causes of putrefaction and we highlight our personal experiences at the Faculty of Medicine in Prince Sattam bin Abdulaziz University in KSA, in preserving the body cadavers. We studied different physical and chemical methods of preservation of cadavers and body parts at the faculty and their efficiency in preventing bacteria and fungi that cause putrefaction and decay.

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Bacterial Contamination of Saudi Arabian paper currency: A report from Al-Kharj المعتصم عثمان أحمد

Currency is a public support tool for exchange of commodity and services. It’s prevalent practice for acquiring bread to broast and bath to bed has connected all human being together irrespective of race and occupation. Currency notes along with their denomination values also carry pathogens if contaminated and will act as an agent for infection transference. Therefore the objective of this cross-sectional study was to assess the load microbial pathogens of paper currency collected in selected public places of Al-Kharj, Saudi Arabia.

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Pharmacognostical, Antibacterial and Antioxidant Studies of Aerial Parts of Pulicaria somalensis (Family: Asteraceae) المعتصم عثمان أحمد

Plant P. somalensis (family-Asteraceae), distributed all over the world, especially in North America, Europe, Southern Africa, South Western China, Central Asia and Mediterranean region except, of Antarctica continent . The family Asteraceae, which contains about 1,620 genera and 23,600 species, is one of the largest angiosperm plant families among the dicotyledonous . Few plants of this family are shrubs, creepers and climber but the majority of plants of this family is herbaceous in nature. There are several key elements present in this family, such as fused anthers, fruits with single ovules and capitulum inflorescence, which are used for the detection of their species . Many members of this rich family have long been used in folk medicines . Antibiotics were widespread in natural crude drugs and exercised since their innovation in the 20th century. However, the emergence of multi-drug resistant pathogens, it becomes a global challenge to the medical world to investigate an active antibiotic . It is now widely recognized that there is a need to develop novel antibiotic agents to minimize the risk of antimicrobial resistance. Most of the species of this genus have been well explored for their medicinal values. The standardization of P. somalensis can be achieved by stepwise pharmacognostic studies . Accurate identification and quality assertion of the preliminary materials are essential requirements to ensure the reproducible quality of herbal medicine, which will contribute to its safety and efficacy. The simple pharmacognostic method used in standardization of plant material includes its morphological and anatomical characters . Oxidative damage...

Evaluation of Antifungal Activity of Olive Oil Based Nanoemulsion المعتصم عثمان أحمد

Topical delivery as an option to oral delivery of drugs has several advantages such as reduced adverse effects, improved efficacy and patient compliance especially for the drugs that having extensive first effect metabolism . However, a very few number of drugs with low dose, low molecular weight and high octanol-water partition coefficients can be successfully delivered, because of the anatomical structure of the barrier layer of skin. Topical delivery is better than painful hypodermic injections that produce hazardous biological waste and causes disease transmission because of needle contaminations . To achieve successful transdermal drug delivery, enhancement of skin permeability is of prime concern. Recently several physical, electrical, chemical and biochemical techniques have been proposed to increase the permeability of the skin. Among these, modification of permeability by chemical method is most widely used owing to economical, simple and rapid. Chemical permeation enhancers either improve the solubility or partition coefficient or increase the diffusion of drugs across the skin. However these are always toxic and irritant to the skin. This led to quest of natural skin penetration enhancers. Oleic acid, an unsaturated fatty acid in olive oil has demonstrated skin penetration potential in various studies However, there is very limited permeation enhancement study of olive oil on human skin . Olive oil as such may be used as permeation enhance especially for lipophillic drugs. In one study on the use of olive oil in blood-vessel suturing, olive oil was found to be non-irritating when compared to Vaseline Paraffin oil ....

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