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Fulltext Encapsulation of Black Seed Oil in Alginate Beads as a pH-Sensitive Carrier for Intestine-Targeted Drug Delivery: In Vitro, In Vivo and Ex Vivo Study

Azad AK, Al-Mahmood SMA, Chatterjee B, Wan Sulaiman WMA, Elsayed TM, Doolaanea AA

Pharmaceutics, 2020 Mar 02;12(3).
PMID: 32131539 DOI: 10.3390/pharmaceutics12030219

Black seed oil (BSO) has been used for various therapeutic purposes around the world since ancient eras. It is one of the most prominent oils used in nutraceutical formulations and daily consumption for its significant therapeutic value is common phenomena. The main aim of this study was to develop alginate-BSO beads as a controlled release system designed to control drug release in the gastrointestinal tract (GIT). Electrospray technology facilitates formulation of small and uniform beads with higher diffusion and swelling rates resulting in process performance improvement. The effect of different formulation and process variables was evaluated on the internal and external bead morphology, size, shape, encapsulation efficiency, swelling rate, in vitro drug release, release mechanism, ex vivo mucoadhesive strength and gastrointestinal tract qualitative and quantitative distribution. All the formulated beads showed small sizes of 0.58 ± 0.01 mm (F8) and spherical shape of 0.03 ± 0.00 mm. The coefficient of weight variation (%) ranged from 1.37 (F8) to 3.93 (F5) ng. All formulations (F1-F9) were studied in vitro for release characteristics and swelling behaviour, then the release data were fitted to various equations to determine the exponent (ns), swelling kinetic constant (ks), swelling rate (%/h), correlation coefficient (r2) and release kinetic mechanism. The oil encapsulation efficiency was almost complete at 90.13% ± 0.93% in dried beads. The maximum bead swelling rate showed 982.23 (F8, r2 = 0.996) in pH 6.8 and the drug release exceeded 90% in simulated gastrointestinal fluid (pH 6.8). Moreover, the beads were well distributed throughout various parts of the intestine. This designed formulation could possibly be advantageous in terms of increased bioavailability and targeted drug delivery to the intestine region and thus may find applications in some diseases like irritable bowel syndrome.

Matched MeSH terms: Biological Availability
LC-MS/MS simultaneous quantification of apomorphine and its major metabolites in human plasma: Application to clinical comparative bioavailability evaluation for the apomorphine sublingual film and a subcutaneous product

Chen YL, Shi L, Agbo F, Yong SH, Tan PS, Ngounou Wetie AG

J Pharm Biomed Anal, 2020 Oct 25;190:113493.
PMID: 32795778 DOI: 10.1016/j.jpba.2020.113493

A liquid chromatography-tandem mass spectrometry (LC-MS/MS) method has been developed and validated for the simultaneous quantification of apomorphine and its metabolites apomorphine sulfate and norapomorphine in human plasma for supporting clinical development of a novel apomorphine sublingual thin film (APL) for the treatment of Parkinson's disease. Analytes and internal standards (IS) were extracted from human plasma by Oasis HLB SPE cartridge, followed by a reversed phase LC-MS/MS analysis using multiple reaction monitoring (MRM) in positive mode (m/z 268 → 237 for apomorphine, 348 → 237 for apomorphine sulfate, and 348 → 237 for norapomorphine). Stable isotope-labeled compounds were used as IS for respective analytes. The validated curve ranges were 0.02-20 ng/mL, 10-1000 ng/mL, and 0.5-20 ng/mL for apomorphine, apomorphine sulfate and norapomorphine, respectively. Extraction recoveries were found to be 73.4 % (apomorphine), 81.1 % (apomorphine sulfate), and 58.6 % (norapomorphine). Established long-term plasma frozen storage stabilities were 504 days at -20 °C and276 days at -60 °C, respectively. The method has been successfully used for analyzing pharmacokinetics (PK) samples collected from a comparative bioavailability study of APL and the marketed apomorphine subcutaneous (s.c.) product Apo-go®. The results demonstrated that the 15-mg APL film administrated via sublingual produced comparable PK characteristics of apomorphine when compared to the commercial product Apo-go (2-mg) via s.c. administration, hence establishing the dose regimen for this sublingual formulation. It was also noticed that the sublingual 15-mg APL film produced a significantly higher apomorphine sulfate metabolite level than the 2-mg s.c. Apo-go, and both treatments yielded a negligible level of norapomorphine metabolite in humans.

Matched MeSH terms: Biological Availability
Fulltext Oral bioavailability enhancement of acyclovir from solid lipid nanoparticles drug delivery system

Haniza Hassan, Ahmad Fuad Shamsuddin, Ekram Alias, Meor Mohd Redzuan Meor Mohd Affandi, Siti Khadijah Adam, Rusliza Basir

Malaysian Journal of Medicine and Health Sciences, 2019;15(107):2-2.
MyJurnal

Introduction:Acyclovir, a widely marketed antiviral drug is used for the treatment of Herpes Simplex infection. High doses of acyclovir are prescribed to patients to attain its maximum therapeutic effect due to its poor absorption and low oral bioavailability. The current therapeutics regiment of acyclovir are known to cause unwarranted adverse effects, thus prompted the need for a suitable drug carrier to improve the pharmacokinetic limitations. Develop-ment of solid lipid nanoparticles for oral delivery of acyclovir proposed in this study aimed to enhance acyclovir oral bioavailability. Methods: Comprehensive experiments and a series of optimization process were carried out to ensure reproducibility and assurance of product quality. The physicochemical characteristics of the solid lipid nanoparticles developed from plant-based solid lipid, Biogapress Vegetal 297 ATO with polysorbate 80 as an emul-sifying agent were also evaluated. Results: The spherical-shaped nanoparticles had an average size of 123 nm with good drug entrapment efficiency, up to 80%. The in vitro drug release study showed that solid lipid nanoparticles had prolonged acyclovir release in simulated intestinal fluid for 24 hours. The nanoparticles formulation was con-sidered stable during storage at refrigerated temperature for at least three months. In vivo oral bioavailability study showed that acyclovir-loaded solid lipid nanoparticles possessed superior oral bioavailability when compared with the commercial acyclovir suspension. Conclusion: In conclusion, this study exhibited the feasibility of solid lipid nanoparticles as an oral delivery vehicle for acyclovir and therefore represent a new promising therapeutic concept of nanoparticulate delivery system.

Matched MeSH terms: Biological Availability
Fulltext Acyclovir-Loaded Solid Lipid Nanoparticles: Optimization, Characterization and Evaluation of Its Pharmacokinetic Profile

Hassan H, Bello RO, Adam SK, Alias E, Meor Mohd Affandi MMR, Shamsuddin AF, et al.

Nanomaterials (Basel), 2020 Sep 09;10(9).
PMID: 32916823 DOI: 10.3390/nano10091785

Acyclovir is an antiviral drug used for the treatment of herpes simplex virus infection. Its oral bioavailability is low; therefore, frequent and high doses are prescribed for optimum therapeutic efficacy. Moreover, the current therapeutic regimen of acyclovir is associated with unwarranted adverse effects, hence prompting the need for a suitable drug carrier to overcome these limitations. This study aimed to develop solid lipid nanoparticles (SLNs) as acyclovir carriers and evaluate their in vivo pharmacokinetic parameters to prove the study hypothesis. During the SLN development process, response surface methodology was exploited to optimize the composition of solid lipid and surfactant. Optimum combination of Biogapress Vegetal 297 ATO and Tween 80 was found essential to produce SLNs of 134 nm. The oral bioavailability study showed that acyclovir-loaded SLNs possessed superior oral bioavailability when compared with the commercial acyclovir suspension. The plasma concentration of acyclovir-loaded SLNs was four-fold higher than the commercial suspension. Thus, this investigation presented promising results that the method developed for encapsulation of acyclovir offers potential as an alternative pathway to enhance the drug's bioavailability. In conclusion, this study exhibited the feasibility of SLNs as an oral delivery vehicle for acyclovir and therefore represents a new promising therapeutic concept of acyclovir treatment via a nanoparticulate drug delivery system.

Matched MeSH terms: Biological Availability
Fulltext A Comprehensive Review on Source, Types, Effects, Nanotechnology, Detection, and Therapeutic Management of Reactive Carbonyl Species Associated with Various Chronic Diseases

Fuloria S, Subramaniyan V, Karupiah S, Kumari U, Sathasivam K, Meenakshi DU, et al.

Antioxidants (Basel), 2020 Nov 02;9(11).
PMID: 33147856 DOI: 10.3390/antiox9111075

Continuous oxidation of carbohydrates, lipids, and amino acids generate extremely reactive carbonyl species (RCS). Human body comprises some important RCS namely hexanal, acrolein, 4-hydroxy-2-nonenal, methylglyoxal, malondialdehyde, isolevuglandins, and 4-oxo-2- nonenal etc. These RCS damage important cellular components including proteins, nucleic acids, and lipids, which manifests cytotoxicity, mutagenicity, multitude of adducts and crosslinks that are connected to ageing and various chronic diseases like inflammatory disease, atherosclerosis, cerebral ischemia, diabetes, cancer, neurodegenerative diseases and cardiovascular disease. The constant prevalence of RCS in living cells suggests their importance in signal transduction and gene expression. Extensive knowledge of RCS properties, metabolism and relation with metabolic diseases would assist in development of effective approach to prevent numerous chronic diseases. Treatment approaches for RCS associated diseases involve endogenous RCS metabolizers, carbonyl metabolizing enzyme inducers, and RCS scavengers. Limited bioavailability and bio efficacy of RCS sequesters suggest importance of nanoparticles and nanocarriers. Identification of RCS and screening of compounds ability to sequester RCS employ several bioassays and analytical techniques. Present review describes in-depth study of RCS sources, types, properties, identification techniques, therapeutic approaches, nanocarriers, and their role in various diseases. This study will give an idea for therapeutic development to combat the RCS associated chronic diseases.

Matched MeSH terms: Biological Availability
Fulltext Pharmacology and Pharmacokinetics of Vitamin E: Nanoformulations to Enhance Bioavailability

Mohd Zaffarin AS, Ng SF, Ng MH, Hassan H, Alias E

Int J Nanomedicine, 2020;15:9961-9974.
PMID: 33324057 DOI: 10.2147/IJN.S276355

Vitamin E belongs to the family of lipid-soluble vitamins and can be divided into two groups, tocopherols and tocotrienols, with four isomers (alpha, beta, gamma and delta). Although vitamin E is widely known as a potent antioxidant, studies have also revealed that vitamin E possesses anti-inflammatory properties. These crucial properties of vitamin E are beneficial in various aspects of health, especially in neuroprotection and cardiovascular, skin and bone health. However, the poor bioavailability of vitamin E, especially tocotrienols, remains a great limitation for clinical applications. Recently, nanoformulations that include nanovesicles, solid-lipid nanoparticles, nanostructured lipid carriers, nanoemulsions, and polymeric nanoparticles have shown promising outcomes in improving the efficacy and bioavailability of vitamin E. This review focuses on the pharmacological properties and pharmacokinetics of vitamin E and current advances in vitamin E nanoformulations for future clinical applications. The limitations and future recommendations are also discussed in this review.

Matched MeSH terms: Biological Availability
Cetyltrimethylammonium bromide-nanocrystalline cellulose (CTAB-NCC) based microemulsions for enhancement of topical delivery of curcumin

Zainuddin N, Ahmad I, Zulfakar MH, Kargarzadeh H, Ramli S

Carbohydr Polym, 2021 Feb 15;254:117401.
PMID: 33357890 DOI: 10.1016/j.carbpol.2020.117401

Low bioavailability and poor water solubility have limited the utilization of curcumin in conventional dosing methods. As an alternative, microemulsions as drug carrier can improve curcumin delivery. A cetyltrimethylammonium bromide-nanocrystalline cellulose (CTAB-NCC)-based microemulsion was developed and its potential use as a topical delivery method for curcumin was investigated. The effect of microemulsion's particle size and its microstructure as well as the presence of the CTAB-NCC nanoparticle on the topical delivery of curcumin was studied. In vitro permeation studies showed higher penetration rate of curcumin from the oil-in-water type-microemulsions. The skin permeation profile of curcumin followed Higuchi release kinetics. Furthermore, use of the (CTAB-NCC)-based microemulsion enhanced curcumin accumulation in the skin and these system showed non cytotoxicity effect on L929 cell line. These results showed the potential of (CTAB-NCC)-based microemulsions as controlled-release topical systems for the delivery of curcumin and potentially other lipophilic drugs.

Matched MeSH terms: Biological Availability
Biomimetic amphiphilic chitosan nanoparticles: Synthesis, characterization and antimicrobial activity

Ahmad N, Wee CE, Wai LK, Zin NM, Azmi F

Carbohydr Polym, 2021 Feb 15;254:117299.
PMID: 33357867 DOI: 10.1016/j.carbpol.2020.117299

Naturally derived antimicrobial peptides (AMPs) are an attractive source of new antimicrobial agents. However, clinical application of AMPs is associated with poor bioavailability and toxicity. In this study, we address these limitations by designing a new series of chitosan derivatives to mimic the amphiphilic topology of AMPs. The synthesized chitosan derivatives were found to self-assemble into nanoparticles in the aqueous environment. Among the compounds, a chitosan derivative grafted with arginine and oleic acid (CH-Arg-OA) exhibited the most potent antimicrobial activity, especially against Gram-negative bacteria. It also caused minimal cell death when tested in HEK293 and HepG2 cell lines, thus confirming the role of cationicity and lipophilicity for selective bacteria targeting. CH-Arg-OA exhibited its antimicrobial activity by disrupting bacterial membranes and causing the leakage of cytoplasmic contents. Thus, amphiphilic chitosan nanoparticles offer a great promise as a new class of AMPs mimics that is effective against Gram-negative bacteria.

Matched MeSH terms: Biological Availability
Fulltext In situ ophthalmic gel forming systems of poloxamer 407 and hydroxypropyl methyl cellulose mixtures for sustained ocular delivery of chloramphenicole: optimization study by factorial design

Kurniawansyah IS, Rusdiana T, Sopyan I, Ramoko H, Wahab HA, Subarnas A

Heliyon, 2020 Nov;6(11):e05365.
PMID: 33251348 DOI: 10.1016/j.heliyon.2020.e05365

Background: Conventional drug delivery systems have some major drawbacks such as low bioavailability, short residence time and rapid precorneal drainage. An in situ gel drug delivery system provides several benefits, such as prolonged pharmacological duration of action, simpler production techniques, and low cost of manufacturing. This research aims to get the optimum formula of chloramphenicol in situ gel based on the physical evaluation.
Methods: The effects of independent variables (poloxamer 407 and hydroxypropyl methyl cellulose (HPMC) concentration) on various dependent variables (gelling capacity, pH and viscosity) were investigated by using 32 factorial design and organoleptic evaluation was done with descriptive analysis.
Results: The optimized formula of chloramphenicol in situ gel yielded 9 variations of poloxamer 407 and HPMC bases composition in % w/v as follows, F1 (5; 0.45), F2 (7.5; 0.45), F3 (10; 0.45), F4 (5; 0.725), F5 (7.5; 0.725), F6 (10; 0.725), F7 (5; 1), F8 (7.5; 1), F9 (10; 1). The results indicated that the organoleptic, pH, and gelling capacity parameters matched all formulas (F1-F9), however, the viscosity parameter only matched F3, F6, F8, and F9. Based on factorial design, F6 had the best formula with desirability value of 0.54, but the design recommended that formula with the composition bases of poloxamer 407 and HPMC at the ratio of 8.16 % w/v and 0.77 % w/v, respectively, was the optimum formula with a desirability value of 0.69.
Conclusion: All formulas have met the Indonesian pharmacopoeia requirements based on the physical evaluation, especially formula 6 (F6), which was supported by the result of factorial design analysis.

Matched MeSH terms: Biological Availability
Seasonal variation of total mercury transfer through a tropical mangrove food web, Setiu Wetlands

Siau YF, Le DQ, Suratman S, Jaaman SA, Tanaka K, Kotaro S

Mar Pollut Bull, 2021 Jan;162:111878.
PMID: 33341077 DOI: 10.1016/j.marpolbul.2020.111878

Seasonal variations in total mercury concentrations [Hg] and trophic transfer through the food web were assessed using stable isotopic tracers for the Setiu Wetlands, Terengganu. The [Hg] measured in surface sediments and biota varied inversely between wet and dry seasons. Increased rainfall and water disturbance during the wet season are suggested as the main factors releasing Hg from surface sediments and enhancing the bioavailability of Hg to biota. The elevated Hg levels associated with the leaf stage suggested that litterfall and atmospheric deposition may be the main Hg inputs into mangrove food webs. The positive relationships between log [Hg] and δ15N provided evidence for Hg biomagnification, however low trophic magnification slopes in both seasons indicated that the ecological risk of Hg in the wetland would be negligible. The [Hg] in fish and commercial crabs were below the permitted limits for human consumption.

Matched MeSH terms: Biological Availability
Fulltext Comparative bioavailability study of two ketoconazole tablet preparations

Yuen KH, Wong JW, Billa N, Choy WP, Julianto T

Med J Malaysia, 1999 Dec;54(4):482-6.
PMID: 11072466

The bioavailability of a generic preparation of ketoconazole (Zorinax from Xepa-Soul Pattinson, Malaysia) was evaluated in comparison with the innovator product (Nizoral from Janssen Pharmaceutica, Switzerland). Eighteen healthy male volunteers participated in the study conducted according to a two-way crossover design. The bioavailability was compared using the parameters, total area under the plasma concentration-time curve (AUC0-infinity), peak plasma concentration (Cmax) and time to reach peak plasma concentration (Tmax). No statistically significant difference was observed between the values of the two products in all the three parameters. Moreover, the 90% confidence interval for the ratio of the logarithmic transformed AUC0-infinity and Cmax values of Zorinax over Nizoral was found to lie between 0.82-1.04 and 0.83-1.02, respectively, being within the acceptable equivalence limit of 0.80-1.25. These findings indicate that the two preparations are comparable in the extent and rate of absorption. In addition, the elimination rate constant (ke) and apparent volume of distribution (Vd) were calculated. For both parameters, there was no statistically significant difference between the values obtained from the data of the two preparations. Moreover, the values are comparable to those reported in the literature.

Matched MeSH terms: Biological Availability
Pharmacokinetics of artemisinin-type compounds

Navaratnam V, Mansor SM, Sit NW, Grace J, Li Q, Olliaro P

Clin Pharmacokinet, 2000 Oct;39(4):255-70.
PMID: 11069212

Various compounds of the artemisinin family are currently used for the treatment of patients with malaria worldwide. They are characterised by a short half-life and feature the most rapidly acting antimalarial drugs to date. They are increasingly being used, often in combination with other drugs, although our knowledge of their main pharmacological features (including their absorption, distribution, metabolism and excretion) is still incomplete. Such data are particularly important in the case of combinations. Artemisinin derivatives are converted primarily, but to different extents, to the bioactive metabolite artenimol after either parenteral or gastrointestinal administration. The rate of conversion is lowest for artelinic acid (designed to protect the molecule against metabolism) and highest for the water-soluble artesunate. The absolute and relative bioavailability of these compounds has been established in animals, but not in humans, with the exception of artesunate. Oral bioavailability in animals ranges, approximately, between 19 and 35%. A first-pass effect is highly probably for all compounds when administered orally. Artemisinin compounds bind selectively to malaria-infected erythrocytes to yet unidentified targets. They also bind modestly to human plasma proteins, ranging from 43% for artenimol to 81.5% for artelinic acid. Their mode of action is still not completely understood, although different theories have been proposed. The lipid-soluble artemether and artemotil are released slowly when administered intramuscularly because of the 'depot' effect related to the oil formulation. Understanding the pharmacokinetic profile of these 2 drugs helps us to explain the characteristics of the toxicity and neurotoxicity. The water-soluble artesunate is rapidly converted to artenimol at rates that vary with the route of administration, but the processes need to be characterised further, including the relative contribution of pH and enzymes in tissues, blood and liver. This paper intends to summarise contemporary knowledge of the pharmacokinetics of this class of compounds and highlight areas that need further research.

Matched MeSH terms: Biological Availability
Simple liquid chromatographic method for the determination of naltrexone in human plasma using amperometric detection

Peh KK, Billa N, Yuen KH

J Chromatogr B Biomed Sci Appl, 1997 Nov 07;701(1):140-5.
PMID: 9389350

A simple liquid chromatographic method using amperometric detection was developed for the determination of naltrexone in human plasma. Prior to analysis, naltrexone and the internal standard (naloxone) were extracted from plasma samples using a 9:1 mixture of chloroform and isopropyl alcohol. The mobile phase comprised 0.1 M disodium hydrogen orthophosphate (pH 3.5) and acetonitrile (85.5:14.5, v/v). Analysis was run at a flow-rate of 0.8 ml/min with the detector operating under oxidative mode at an applied potential of +0.95 V. The method is specific and sensitive with a detection limit of approximately 1 ng/ml at a signal-to-noise ratio of 3:1. Mean recovery value of the extraction procedure was about 93%, while the within day and between day coefficient of variation and percent error values of the assay method were all less than 10%. The calibration curve was linear over a concentration range of 1.5-100 ng/ml.

Matched MeSH terms: Biological Availability
Simple high-performance liquid chromatographic method for the determination of ranitidine in human plasma

Wong CF, Peh KK, Yuen KH

J Chromatogr B Biomed Sci Appl, 1998 Oct 23;718(1):205-10.
PMID: 9832378

A simple high-performance liquid chromatographic method was developed for the determination of ranitidine in human plasma. Prior to analysis, ranitidine and the internal standard (metoprolol) were extracted from alkalinized plasma samples using dichloromethane. The mobile phase was 0.05 M potassium dihydrogenphosphate-acetonitrile (88:12, v/v) adjusted to pH 6.5. Analysis was run at a flow-rate of 1.3 ml/min and at a detection wavelength of 229 nm. The method is sensitive with a detection limit of 1 ng/ml at a signal-to-noise ratio of 3:1, while the quantification limit was set at 15 ng/ml. The calibration curve was linear over a concentration range of 15-2000 ng/ml. Mean recovery value of the extraction procedure was about 90%, while the within-day and between-day coefficients of variation and percent error values of the assay method were all less than 15%.

Matched MeSH terms: Biological Availability
In vivo/in vitro correlation of experimental sustained-release theophylline formulations

Yuen KH, Desmukh AA, Newton JM

Pharm Res, 1993 Apr;10(4):588-92.
PMID: 8483843

A novel multiparticulate sustained-release theophylline formulation, which consisted of spherical drug pellets coated with a rate-controlling membrane, was evaluated in vivo. Two preparations that differ solely in the coat thickness, and hence rate of in vitro drug release, were studied in comparison with a solution of the drug. Both preparations produced serum concentration profiles that are reflective of a slow and sustained rate of absorption. The in vivo release versus time profiles calculated using a deconvolution procedure showed that the two preparations differed in the rate but not the extent of drug release. Satisfactory correlation was also obtained between the in vivo and the in vitro results. When the two preparations were further compared using the parameters, time to reach peak concentration (Tp), peak concentration (Cp), and total area under the serum concentration versus time curves (AUC), a statistically significant difference was observed in the Tp and Cp values but not the AUC values, suggesting that the preparations differed in the rate but not the extent of absorption. In addition, the extent of absorption from both preparations was comparable to that obtained with the drug solution.

Matched MeSH terms: Biological Availability
Relative bioavailability of the hydrochloride, sulphate and ethyl carbonate salts of quinine

Jamaludin A, Mohamad M, Navaratnam V, Selliah K, Tan SC, Wernsdorfer WH, et al.

Br J Clin Pharmacol, 1988 Feb;25(2):261-3.
PMID: 3358888

The hydrochloride, sulphate and ethylcarbonate salts of quinine were given in single oral doses (600 mg base equivalent) to nine healthy male subjects according to a cross-over design. No statistically significant differences were noted in the plasma drug concentration-time profiles although inter- and intra-subject variation in AUC, Cmax and tmax values was appreciable. The ethylcarbonate salt may be preferred for use in paediatric patients because of its neutral taste.

Matched MeSH terms: Biological Availability
Fulltext Clozapine-sodium starch glycolate dispersions: in vitro dissolution behaviour, physicochemical characterisation and release kinetic model fitting

Venkateskumar Krishnamoorthy, Verma Priya Ranjan Prasad, Suchandrasen Sen

Malaysian Journal of Pharmaceutical Science, 2013;11(2):49-70.
MyJurnal

exhibits extensive first pass metabolism with poor oral bioavailability (27%–50%) limiting its therapeutic efficiency. The present study involved an attempt to enhance its aqueous solubility by formulating as solid dispersions (SDs) using sodium starch glycollate (SSG) as a carrier. The dispersions were formulated by dispersion method and evaluated by phase solubility, drug content, in vitro release and mathematical modelling. Solid state characterisation of samples was carried out by X-ray diffraction (XRD), differential scanning calorimetric (DSC), Fourier transform infrared spectrophotometry (FTIR), near infrared (NIR), Raman analysis and wettability studies. The phase solubility and thermodynamic parameters indicated the spontaneity and solubilisation effect of carrier. The release rate from the dispersions was higher than pure drug and found to increase with an increase in carrier content. The optimised dispersions were selected based on release studies, profiles and dissolution parameters. XRD, DSC, FTIR, NIR and Raman analysis proved the crystallinity reduction, changes in crystal quality and compatibility between drug and carriers. Wettability studies proved the increased wettability in selected dispersions. Based on the findings, possible mechanisms that would have contributed to dissolution enhancement of CLZ were suggested. Such findings could be extrapolated to enhance the aqueous solubility of other poorly water-soluble drugs.

Matched MeSH terms: Biological Availability
Fulltext Bioactive molecules: current trends in discovery, synthesis, delivery and testing

Yew Beng Kang, Pichika R Mallikarjuna, Davamani A Fabian, Adinarayana Gorajana, Chooi Ling Lim, Eng Lai Tan

International e-Journal of Science, Medicine & Education, 2013;7(11):32-46.
MyJurnal

Important bioactive molecules are molecules that are pharmacologically active derived from natural sources and through chemical synthesis. Over the years many of such molecules have been discovered through bioprospective endeavours. The discovery of taxol from the pacific yew tree bark that has the ability in stabilising cellular microtubules represents one of the hallmarks of success of such endeavours. In recent years, the discovery process has been aided by the rapid development
of techniques and technologies in chemistry and biotechnology. The progress in advanced genetics and computational biology has also transformed the way hypotheses are formulated as well as the strategies for drug discovery. Of equal importance is the use of advanced drug delivery vehicles in enhancing the efficacy and bioavailability of bioactive molecules. The availability of suitable animal models for testing and validation is yet another major determinant in increasing the prospect for
clinical trials of bioactive molecules.

Matched MeSH terms: Biological Availability
Fulltext Effect of germination on total dietary fibre and total sugar in selected legumes

Megat, R.M.R., Azrina, A., Norhaizan, M.E.

International Food Research Journal, 2016;23(1):257-261.
MyJurnal

Legume is a plant in the family of Fabaceae (or Leguminosae) that is cultivated and consumed
throughout the world. Legume’s role in human health appears to be limited because of several
limiting factors such as low protein and starch digestibility, poor mineral bioavailability and
high antinutritional factors. Germination is defined as a process that occurs during seed growth
that starts with uptake of water until the emergence of radicle through the surrounding structure.
It has been suggested that germination is a cheaper and more effective technology that can
improve the quality of legumes by increasing their nutritional value. This study was conducted
to compare changes in dietary fibre and total sugar compositions after germination process in
kidney, mung, soy beans and peanuts. Total dietary fibre was found to be significantly increased
(p

Matched MeSH terms: Biological Availability
Improvement of wheat straw anaerobic digestion through alkali pre-treatment: Carbohydrates bioavailability evaluation and economic feasibility

Romero-Güiza MS, Wahid R, Hernández V, Møller H, Fernández B

Sci Total Environ, 2017 Oct 01;595:651-659.
PMID: 28402918 DOI: 10.1016/j.scitotenv.2017.04.006

Lignocellulosic biomasses such as wheat straw are widely used as a feedstock for biogas production. However, these biomasses are mainly composed of a compact fibre structure and therefore, it is recommended to treat them prior to its usage for biogas production in order to improve their bioavailability. The aim of this work is to evaluate, in terms of performance stability, methane yield and economic feasibility, two different scenarios: a mesophilic codigestion of wheat straw and animal manure with or without a low-energy demand alkaline pre-treatment (0.08gKOHgTS-1of wheat straw, for 24h and at 25°C). Besides this, said pre-treatment was also analysed based on the improvement of the bioavailable carbohydrate content in the untreated versus the pre-treated wheat straw. The results pointed out that pre-treated wheat straw prompted a more stable performance (in terms of pH and alkalinity) and an improved methane yield (128% increment) of the mesophilic codigestion process, in comparison to the "untreated" scenario. The pre-treatment increased the content of cellulose, hemicellulose and other compounds (waxes, pectin, oil, etc.) in the liquid fraction, from 5% to 60%, from 11.5% to 39.1% TS and from 57% to 79% of the TS in the liquid fraction for the untreated and pre-treated wheat straws, respectively. Finally, the pre-treated scenario gained an energy surplus of a factor 13.5 and achieved a positive net benefit of 90.4€tVS-WS-1d-1, being a favourable case for an eventual scale-up of the combined process.

Matched MeSH terms: Biological Availability

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