Displaying publications 41 - 60 of 235 in total

Abstract:
Sort:
  1. Bioavailability of polycyclic aromatic hydrocarbons (PAHs) to short-neck clam (Paphia undulata) from sediment matrices in mudflat ecosystem of the west coast of Peninsular Malaysia
    Keshavarzifard M, Zakaria MP, Hwai TS
    Environ Geochem Health, 2017 Jun;39(3):591-610.
    PMID: 27216263 DOI: 10.1007/s10653-016-9835-z
    The bioaccumulation and bioavailability of polycyclic aromatic hydrocarbons (PAHs) were characterized in sediment and Paphia undulata (short-neck clam) from six mudflat areas in the west coasts of Peninsular Malaysia. The concentrations of total PAHs varied from 357.1 to 6257.1 and 179.9 ± 7.6 to 1657.5 ± 53.9 ng g -1 dry weight in sediment and short-neck clam samples, respectively. PAHs can be classified as moderate to very high level of pollution in sediments and moderate to high level of pollution in short-neck clams. The diagnostic ratios of individual PAHs and principal component analysis indicate both petrogenic and pyrogenic sources with significant dominance of pyrogenic source. The first PAHs biota-sediment accumulation factors and relative biota-sediment accumulation factors data for short-neck clam were obtained in this study, indicating a preferential accumulation of lower molecular weight PAHs. Evaluation of PAH levels in sediments and short-neck clams indicates that short-neck clam could be introduced as a good biomonitor in mudflats. The results also demonstrated that under environmental conditions, the sedimentary load of hydrocarbons appears to be one of the factors controlling their bioavailability to biota.
    Matched MeSH terms: Biological Availability
  2. Fulltext Comparative pharmacokinetics of a proliposome formulation of Ginkgo biloba extract and Ginaton in rats by a sensitive ultra performance liquid chromatography-tandem mass spectrometry method
    Zheng B, Xing G, Bi Y, Yan G, Wang J, Cheng Y, et al.
    Saudi J Biol Sci, 2016 Jan;23(1):54-65.
    PMID: 26858539 DOI: 10.1016/j.sjbs.2015.08.009
    As a novel oral drug delivery system, proliposome was applied to improve the solubility of active components of Ginkgo biloba extract (GbE). There are currently few reports focusing on the pharmacokinetic characteristics of proliposome of GbE (GbP). A rapid and sensitive ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for the simultaneous quantification of active components of GbP and a commercial tablet product (Ginaton) in rat plasma was developed and successfully validated. The method was applied to the comparative pharmacokinetic evaluation of GbP and Ginaton in rat plasma. The results indicated that GbP has a significant effect on absorption, elimination and bioavailability of flavonoids and terpenoid lactones in comparison with Ginaton. The obtained results would be helpful for evaluating the absorption mechanism in the gastrointestinal tract in pharmacokinetic level and guiding the development of the novel oral drug delivery system.
    Matched MeSH terms: Biological Availability
  3. Formulation and optimization of gastric floating drug delivery system using Central composite design and its biopharmaceutical evaluation
    Meka VS, Thing LK, Gorajana A, Kolapalli VR
    Pak J Pharm Sci, 2015 Jul;28(4):1373-87.
    PMID: 26142528
    The present work investigates the formulation and biopharmaceutical estimation of gastric floating drug delivery system (GFDDS) of propranolol HCl using semi-synthetic polymer carboxymethyl ethyl cellulose (CMEC) and a synthetic polymer polyethylene oxide (PEO). A central composite design was applied for optimization of polymer quantity (CMEC or PEO) and sodium bicarbonate concentration as independent variables. The dependent variables evaluated were: % of drug release at 1 hr (D1hr), % drug release at 3 hr (D3hr) and time taken for 95% of drug release (t95). Numerical optimization and graphical optimization were conducted to optimize the response variables. All observed responses of statistically optimized formulations were in high treaty with predicted values. Accelerated stability studies were conducted on the optimized formulations at 40 ± 2°C/75% ± 5% RH and confirm that formulations were stable. Optimized formulations were evaluated for in vivo buoyancy characterization in human volunteers and were found buoyant in gastric fluid. Gastric residence time was enhanced in the fed but not the fasted state. The optimized formulations and marketed formulation were administered to healthy human volunteers and evaluated for pharmacokinetic parameters. Mean residence time (MRT) was prolonged and AUC levels were increased for both optimized floating tablets when compared with marketed product. High relative bioavailability obtained with optimized gastric floating tablets compared to commercial formulation, indicated the improvement of bioavailability.
    Matched MeSH terms: Biological Availability
  4. 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
  5. 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
  6. 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
  7. 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
  8. Fulltext Recent Progress of Chitosan and Chitosan Derivatives-Based Nanoparticles: Pharmaceutical Perspectives of Oral Insulin Delivery
    Seyam S, Nordin NA, Alfatama M
    Pharmaceuticals (Basel), 2020 Oct 14;13(10).
    PMID: 33066443 DOI: 10.3390/ph13100307
    Diabetes mellitus is a chronic endocrine disease, affecting more than 400 million people around the world. Patients with poorly controlled blood glucose levels are liable to suffer from life-threatening complications, such as cardiovascular, neuropathy, retinopathy and even premature death. Today, subcutaneous parenteral is still the most common route for insulin therapy. Oral insulin administration is favourable and convenient to the patients. In contrast to injection route, oral insulin delivery mimics the physiological pathway of endogenous insulin secretion. However, oral insulin has poor bioavailability (less than 2%) due to the harsh physiological environment through the gastrointestinal tract (GIT). Over the last few decades, many attempts have been made to achieve an effective oral insulin formulation with high bioavailability using insulin encapsulation into nanoparticles as advanced technology. Various natural polymers have been employed to fabricate nanoparticles as a delivery vehicle for insulin oral administration. Chitosan, a natural polymer, is extensively studied due to the attractive properties, such as biodegradability, biocompatibility, bioactivity, nontoxicity and polycationic nature. Numerous studies were conducted to evaluate chitosan and chitosan derivatives-based nanoparticles capabilities for oral insulin delivery. This review highlights strategies that have been applied in the recent five years to fabricate chitosan/chitosan derivatives-based nanoparticles for oral insulin delivery. A summary of the barriers hurdle insulin absorption rendering its low bioavailability such as physical, chemical and enzymatic barriers are highlighted with an emphasis on the most common methods of chitosan nanoparticles preparation. Nanocarriers are able to improve the absorption of insulin through GIT, deliver insulin to the blood circulation and lower blood glucose levels. In spite of some drawbacks encountered in this technology, chitosan and chitosan derivatives-based nanoparticles are greatly promising entities for oral insulin delivery.
    Matched MeSH terms: Biological Availability
  9. 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
  10. 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
  11. Influence of chloride ions on the reduction of mercury species in the presence of dissolved organic matter
    Lee S, Roh Y, Kim KW
    Environ Geochem Health, 2019 Feb;41(1):71-79.
    PMID: 29761243 DOI: 10.1007/s10653-018-0121-0
    Mercuric species, Hg(II), interacts strongly with dissolved organic matter (DOM) through the oxidation, reduction, and complexation that affect the fate, bioavailability, and cycling of mercury, Hg, in aquatic environments. Despite its importance, the reactions between Hg(II) and DOM have rarely been studied in the presence of different concentrations of chloride ions (Cl-) under anoxic conditions. Here, we report that the extent of Hg(II) reduction in the presence of the reduced DOM decreases with increasing Cl- concentrations. The rate constants of Hg(II) reduction ranged from 0.14 to 1.73 h-1 in the presence of Cl- and were lower than the rate constant (2.41 h-1) in the absence of Cl-. Using a thermodynamic model, we showed that stable Hg(II)-chloride complexes were formed in the presence of Cl-. We further examined that H(0) was oxidized to Hg(II) in the presence of the reduced DOM and Cl- under anoxic conditions, indicating that Hg(II) reduction is inhibited by the Hg(0) oxidation. Therefore, the Hg(II) reduction by the reduced DOM can be offset due to the Hg(II)-chloride complexation and Hg(0) oxidation in chloride-rich environments. These processes can significantly influence the speciation of Hg and have an important implication for the behavior of Hg under environmentally relevant concentrations.
    Matched MeSH terms: Biological Availability
  12. Fulltext Levofloxacin: Insights Into Antibiotic Resistance and Product Quality
    Izadi E, Afshan G, Patel RP, Rao VM, Liew KB, Meor Mohd Affandi MMR, et al.
    Front Pharmacol, 2019;10:881.
    PMID: 31474853 DOI: 10.3389/fphar.2019.00881
    Counterfeit and substandard medicines are recognized as one of serious threats to public health. The product quality of antibacterial medicine will compromise patients' recovery and increase the chance of antibacterial resistance. The review aims to provide a summary of low quality levofloxacin issues and the risk factors as well as suggesting the aspects of product quality that need to be regulated strictly. Quality of the active ingredient, levofloxacin, has an important role to contribute to successful therapy. The poor quality of raw material, directly and indirectly, causes treatment failure as the presence of insufficient dose, mislabeled content, and poor dissolution characteristics can lead to lower bioavailability. Identifying and reporting these factors can potentially help in improving the quality of drug marketed in various developing countries and may also reduce the incidences of treatment failure. Dissolution test is used for testing the dissolution profiles and the rate of drug release from solid formulation such as oral formulations, thus providing information regarding the in vivo performance of a formulation and its bioequivalence. On the other hand, quality-testing procedures are used for comparing the quality of products.
    Matched MeSH terms: Biological Availability
  13. Lapatinib nano-delivery systems: a promising future for breast cancer treatment
    Bonde GV, Yadav SK, Chauhan S, Mittal P, Ajmal G, Thokala S, et al.
    Expert Opin Drug Deliv, 2018 05;15(5):495-507.
    PMID: 29521126 DOI: 10.1080/17425247.2018.1449832
    INTRODUCTION: Breast cancer stands the second prominent cause of death among women. For its efficient treatment, Lapatinib (LAPA) was developed as a selective tyrosine kinase inhibitor of receptors, overexpressed by breast cancer cells. Various explored delivery strategies for LAPA indicated its controlled release with enhanced aqueous solubility, improved bioavailability, decreased plasma protein binding, reduced dose and toxicity to the other organs with maximized clinical efficacy, compared to its marketed tablet formulation.

    AREAS COVERED: This comprehensive review deals with the survey, performed through different electronic databases, regarding various challenges and their solutions attained by fabricating delivery systems like nanoparticles, micelle, nanocapsules, nanochannels, and liposomes. It also covers the synthesis of novel LAPA-conjugates for diagnostic purpose.

    EXPERT OPINION: Unfortunately, clinical use of LAPA is restricted because of its extensive albumin binding capacity, poor oral bioavailability, and poor aqueous solubility. LAPA is marketed as the oral tablet only. Therefore, it becomes imperative to formulate alternate efficient multiparticulate or nano-delivery systems for administration through non-oral routes, for active/passive targeting, and to scale-up by pharmaceutical scientists followed by their clinical trials by clinical experts. LAPA combinations with capecitabine and letrozole should also be tried for breast cancer treatment.

    Matched MeSH terms: Biological Availability
  14. Model for bioavailability and metal reduction from soil amended with petroleum wastewater by rye-grass L
    Ahmad A, Sreedhar Reddy S, Rumana G
    Int J Phytoremediation, 2019;21(5):471-478.
    PMID: 30648407 DOI: 10.1080/15226514.2018.1537243
    To assess the tolerance, the rye-grass L. grown on soil amended with petroleum wastewater (PWW) containing four metals lead, zinc, nickel and mercury. The PWW (25 to 50%) showed remarkable increase in length and biomass. Chlorophyll 'a and b' increased with an increase of PWW from 25-50% while such contents decreased on increasing the 75-100% compared to control. The mass balance performed on the system showed the removal of 90-97.6% lead, 85.5-92.9% zinc, 78.9-85.5% nickle and 47.6-27.5% mercury. The model for the maximum metal reduction rate (Rmax) was much better for Pb (89.5) and Zn (72.1) with respect to Ni (57.3) and Hg (32.4). Survival of rye-grass (30-days, statics, and renewal exposures) was increased by 50% as compared to control. The toxicity index Y of PWW showed 0-25% deficiency level, 25-50% tolerance level, 50-90% toxic level and 90-100% lethal level. The experimental data showing high correlation coefficient (R2 = 0.98).
    Matched MeSH terms: Biological Availability
  15. Fulltext Sinensetin: An Insight on Its Pharmacological Activities, Mechanisms of Action and Toxicity
    Han Jie L, Jantan I, Yusoff SD, Jalil J, Husain K
    Front Pharmacol, 2020;11:553404.
    PMID: 33628166 DOI: 10.3389/fphar.2020.553404
    Sinensetin, a plant-derived polymethoxylated flavonoid found in Orthosiphon aristatus var. aristatus and several citrus fruits, has been found to possess strong anticancer activities and a variety of other pharmacological benefits and promising potency in intended activities with minimal toxicity. This review aims to compile an up-to-date reports of published scientific information on sinensetin pharmacological activities, mechanisms of action and toxicity. The present findings about the compound are critically analyzed and its prospect as a lead molecule for drug discovery is highlighted. The databases employed for data collection are mainly through Google Scholar, PubMed, Scopus and Science Direct. In-vitro and in-vivo studies showed that sinensetin possessed strong anticancer activities and a wide range of pharmacological activities such as anti-inflammatory, antioxidant, antimicrobial, anti-obesity, anti-dementia and vasorelaxant activities. The studies provided some insights on its several mechanisms of action in cancer and other disease states. However, more detail mechanistic studies are needed to understand its pharmacological effects. More in vivo studies in various animal models including toxicity, pharmacokinetic, pharmacodynamic and bioavailability studies are required to assess its efficacy and safety before submission to clinical studies. In this review, an insight on sinensetin pharmacological activities and mechanisms of action serves as a useful resource for a more thorough and comprehensive understanding of sinensetin as a potential lead candidate for drug discovery.
    Matched MeSH terms: Biological Availability
  16. 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
  17. 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
  18. 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
  19. 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
  20. 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
Related Terms
Filters
Contact Us

Please provide feedback to Administrator (afdal@afpm.org.my)

External Links