Displaying publications 21 - 40 of 240 in total

Abstract:
Sort:
  1. Convolution and validation of in vitro-in vivo correlation of water-insoluble sustained-release drug (domperidone) by first-order pharmacokinetic one-compartmental model fitting equation
    Bose A, Wui WT
    Eur J Drug Metab Pharmacokinet, 2013 Sep;38(3):191-200.
    PMID: 23264125 DOI: 10.1007/s13318-012-0116-7
    The experimental study presents a brief and comprehensive perspective on the methods of developing a Level A in vitro-in vivo correlation (IVIVC) for extended oral dosage forms of water-insoluble drug domperidone. The study also evaluates the validity and predictability of in vitro-in vivo correlation using the convolution technique by one-compartmental first-order kinetic equation. The IVIVC can be substituted as a surrogate for in vivo bioavailability study for the documentation of bioequivalence studies as mandatory from any regulatory authorities. The in vitro drug release studies for different formulations (fast, moderate, slow) were conducted in different dissolution mediums. The f (2) metric (similarity factor) was used to analyze the dissolution data for determination of the most discriminating dissolution method. The in vivo pharmacokinetics parameters of all the formulations were determined by using liquid chromatography mass spectrometry (LC/MS) methods. The absorption rate constant and percentage of absorption of drugs at different time intervals were calculated by using data convolution. In vitro drug release and in vivo absorption correlation were found to be a linear correlation model, which was developed by using percent absorbed drug release versus percent drug dissolved from the three formulations. Internal and external validation was performed to validate the IVIVC. Predicted domperidone concentrations were obtained by convolution technique using first-order one-compartmental fitting equation. Prediction errors estimated for C (max) and AUC (0-infinity) were found to be within the limit.
    Matched MeSH terms: Biological Availability
  2. Fulltext Impact of prebiotics on equol production from soymilk isoflavones by two Bifidobacterium species
    Mustafa SE, Mustafa S, Ismail A, Abas F, Abd Manap MY, Ahmed Hamdi OA, et al.
    Heliyon, 2020 Oct;6(10):e05298.
    PMID: 33134584 DOI: 10.1016/j.heliyon.2020.e05298
    The influence of commercial prebiotics (fructo-oligosaccharides and inulin) and sugars (glucose and sucrose) on enhancing equol production from soymilk isoflavones by Bifidobacterium longum BB536 and Bifidobacterium breve ATCC 15700 was evaluated in vitro. Sterilized soymilk was inoculated with each bacterial species at 37 °C for 48 h. The growth and β-glucosidase enzyme activity for the two Bifidobacterium species in soymilk throughout fermentation were assessed. The highest viable count for B. breve (8.75 log CFU/ml) was reached at 36 h and for B. longum (8.55 log CFU/ml) at 24 h. Both bacterial species displayed β-glucosidase activity. B. breve showed increased enzyme activity (4.126 U) at 36 h, while B. longum exhibited maximum activity (3.935 U) at 24 h of fermentation. Among the prebiotics screened for their effect in isoflavones transformation to equol, inulin delivered the highest effect on equol production. The co-culture of B. longum BB536 and B. breve ATCC15700 in soymilk supplemented with inulin produced the highest level (11.49 mmol/l) of equol at 48 h of fermentation process. Level of daidzin declined whereas that of daidzein increased, and then gradually decreased due to formation of equol when soymilk was fermented using bifidobacterial. This suggests that the nutritional value of soymilk may be increased by increasing bioavailability of the bioactive ingredients. Collectively these data identify probiotics and prebiotic combinations suitable for inclusion in soymilk to enhance equol production.
    Matched MeSH terms: Biological Availability
  3. Fulltext Bioavailability and leaching of Cd and Pb from contaminated soil amended with different sizes of biochar
    Fahmi AH, Samsuri AW, Jol H, Singh D
    R Soc Open Sci, 2018 Nov;5(11):181328.
    PMID: 30564418 DOI: 10.1098/rsos.181328
    Biochars have been successfully used to reduce bioavailability and leaching of heavy metals in contaminated soils. The efficiency of biochar to immobilize heavy metals can be increased by reducing the particle size, which can increase the surface area and the cation exchange capacity (CEC). In this study, the empty fruit bunch biochar (EFBB) of oil palm was separated into two particle sizes, namely, fine (F-EFBB < 50 µm) and coarse (C-EFBB > 2 mm), to treat the contaminated soil with Cd and Pb. Results revealed that the addition of C-EFBB and F-EFBB increased the pH, electrical conductivity and CEC of the contaminated soil. The amounts of synthetic rainwater extractable and leachable Cd and Pb significantly decreased with the EFBB application. The lowest extractable and leachable Cd and Pb were observed from 1% F-EFBB-treated soil. The amount of extractable and leachable Cd and Pb decreased with increasing incubation times and leaching cycles. The application of F-EFBB to Cd and Pb-contaminated soil can immobilize the heavy metals more than that of C-EFBB. Therefore, the EFBB can be recommended for the remediation of heavy metal-contaminated soils, and a finer particle size can be applied at a lower application rate than the coarser biochar to achieve these goals.
    Matched MeSH terms: Biological Availability
  4. Enzymatic hydrolysis: Sialylated mucin (SiaMuc) glycoprotein of edible swiftlet's nest (ESN) and its molecular weight distribution as bioactive ESN SiaMuc-glycopeptide hydrolysate
    Hui Yan T, Lim SJ, Babji AS, Rawi MH, Sarbini SR
    Int J Biol Macromol, 2021 Apr 01;175:422-431.
    PMID: 33561458 DOI: 10.1016/j.ijbiomac.2021.02.007
    Bioactive edible swiftlet's nest (ESN) sialylated-mucin (SiaMuc) hydrolysate is produced by alcalase hydrolysis. Enzymatic hydrolysis of ESN breakdown high-valued ESN SiaMuc-glycoprotein into bioactive SiaMuc-glycopeptide. This is a breakthrough for the issue of insolubility and low extraction rate in ESN, and even increases the bioavailability of ESN nutritional functionality and health benefits. Hydrolysis of ESN SiaMuc-glycoprotein was performed for 1 to 4 h and its effect on physicochemical properties, molecular weight (MW) distribution, SiaMuc-glycoprotein and glycopeptide integrity were determined. Other than improvement in solubility and bioavailability as SiaMuc-glycopeptide, results from SDS-PAGE revealed that MW of SiaMuc-glycoprotein decreased from 42.0-148.8 kDa to 17.7-142.7 kDa with increasing hydrolysis period. Further hydrolysis from maximized DH (90 min) showed an insignificant effect on the MW of ESN SiaMuc-glycopeptide and remained constant at 15.2 kDa. This highlights that enzymatic hydrolysis only influences macro SiaMuc-glycoprotein fractions (142.7, 115.3 and 102.7 kDa), while the majority of SiaMuc-glycopeptide fractions from 36.6-98.6 kDa remained intact. Conclusively, alcalase hydrolysis of ESN showed high recovery in the form of bioactive ESN SiaMuc-glycopeptide. Therefore, enzymatic biotechnology is an economic alternative applicable on ESN that broaden industrial utilization by reducing the MW without destroying the quality of bioactive SiaMuc-glycoprotein.
    Matched MeSH terms: Biological Availability
  5. Fulltext Nanotechnology-Based Strategies for Berberine Delivery System in Cancer Treatment: Pulling Strings to Keep Berberine in Power
    Javed Iqbal M, Quispe C, Javed Z, Sadia H, Qadri QR, Raza S, et al.
    Front Mol Biosci, 2020;7:624494.
    PMID: 33521059 DOI: 10.3389/fmolb.2020.624494
    Cancer is a multifactorial disease characterized by complex molecular landscape and altered cell pathways that results in an abnormal cell growth. Natural compounds are target-specific and pose a limited cytotoxicity; therefore, can aid in the development of new therapeutic interventions for the treatment of this versatile disease. Berberine is a member of the protoberberine alkaloids family, mainly present in the root, stem, and bark of various trees, and has a reputed anticancer activity. Nonetheless, the limited bioavailability and low absorption rate are the two major hindrances following berberine administration as only 0.5% of ingested berberine absorbed in small intestine while this percentage is further decreased to 0.35%, when enter in systemic circulation. Nano-based formulation is believed to be an ideal candidate to increase absorption percentage as at nano scale level, compounds can absorb rapidly in gut. Nanotechnology-based therapeutic approaches have been implemented to overcome such problems, ultimately promoting a higher efficacy in the treatment of a plethora of diseases. This review present and critically discusses the anti-proliferative role of berberine and the nanotechnology-based therapeutic strategies used for the nano-scale delivery of berberine. Finally, the current approaches and promising perspectives of latest delivery of this alkaloid are also critically analyzed and discussed.
    Matched MeSH terms: Biological Availability
  6. Fulltext Improvement of gastroprotective and anti-ulcer effect of kenaf seed oil-in-water nanoemulsions in rats
    Cheong AM, Tan ZW, Patrick NO, Tan CP, Lim YM, Nyam KL
    Food Sci Biotechnol, 2018 Aug;27(4):1175-1184.
    PMID: 30263848 DOI: 10.1007/s10068-018-0342-0
    Kenaf seed oil-in-water nanoemulsions (KSON) and kenaf seed oil-in-water macroemulsions were produced to access their gastroprotective effect against indomethacin- and ethanol-induced ulcers in comparison with non-emulsified kenaf seed oil (KSO). Emulsifier mixture (EM) that used to emulsify KSO was also included in the study. Ulcer index, stomach tissue oxidative status, and histopathological changes in indomethacin-induced and ethanol-induced ulcer models were both evaluated. KSON had demonstrated good gastroprotective effect against both ulcer models than non-emulsified KSO and KSOM. In addition, the gastroprotective effect of KSON was comparable to the standard drug, Omeprazole. EM also exhibited gastroprotective effect, especially in indomethacin-induced ulcers. This may be attributed to its high antioxidant activity and cytoprotective effect of sodium caseinate contained in the EM. Results supported that KSON enhanced the bioavailability of native KSO; therefore it offers gastroprotective effect for the prevention of gastric ulceration as a natural alternative to the synthetic drug.
    Matched MeSH terms: Biological Availability
  7. Opening eyes to therapeutic perspectives of bioactive polyphenols and their nanoformulations against diabetic neuropathy and related complications
    Khursheed R, Singh SK, Wadhwa S, Gulati M, Kapoor B, Awasthi A, et al.
    Expert Opin Drug Deliv, 2021 04;18(4):427-448.
    PMID: 33356647 DOI: 10.1080/17425247.2021.1846517
    Introduction: Diabetic neuropathy (DN) is one of the major complications arising from hyperglycaemia in diabetic patients. In recent years polyphenols present in plants have gained attention to treat DN. The main advantages associated with them are their action via different molecular pathways to manage DN and their safety. However, they failed to gain clinical attention due to challenges associated with their formulation development such as lipophilicity,poor bioavailability, rapid systemic elimination, and enzymatic degradation.Area covered: This article includes different polyphenols that have shown their potential against DN in preclinical studies and the research carried out towards development of their nanoformulations in order to overcome aforementioned issues.Expert opinion: In this review various polyphenol based nanoformulations such as nanospheres, self-nanoemulsifying drug delivery systems, niosomes, electrospun nanofibers, metallic nanoparticles explored exclusively to treat DN are discussed. However, the literature available related to polyphenol based nanoformulations to treat DN is limited. Moreover, these experiments are limited to preclinical studies. Hence, more focus is required towards  development of nanoformulations using simple and single step process as well as inexpensive and non-toxic excipients so that a stable, scalable, reproducible and non-toxic formulation could be achieved and clinical trials could be initiated.
    Matched MeSH terms: Biological Availability
  8. Fulltext Bioavailability of heavy metal in rice using in vitro digestion model
    Omar, N. A., Praveena, S. M., Hashim, Z., Aris, A. Z.
    International Food Research Journal, 2013;20(6):2979-2985.
    MyJurnal
    Rice is a carbohydrate, one of the plant-based foods that can accumulate heavy metal from soil and the irrigation water. Since total heavy metal always overestimates the amount of heavy metal available in rice, bioavailability of heavy metal is always preferred. Many studies have been done and found that in vitro methods offer an appealing alternative to human and animal studies. They can be simple, rapid, low in cost and may provide insights which not achievable in the in vivo studies. In vitro digestion model for rice may differ from other in vitro digestion models applied in soil or other type of foods studies. This review aims to provide an overview of in vitro digestion model used to determine bioavailability of heavy metal in rice, summarize health risk assessment application of heavy metal in rice studies and highlight the importance of health risk assessment to be included in the studies. Future exploration of in vitro digestion model and health risk assessment application on the bioavailability of heavy metal in rice was also suggested.
    Matched MeSH terms: Biological Availability
  9. Comparative study of the bioavailability and dissolution behavior of five brands of tetracycline capsules
    Gan EK, Lim BS, Mahmud N
    Med J Malaysia, 1978 Sep;33(1):72-5.
    PMID: 750900
    Matched MeSH terms: Biological Availability
  10. Antibody-Mediated Therapy against HIV/AIDS: Where Are We Standing Now?
    Awi NJ, Teow SY
    J Pathog, 2018;2018:8724549.
    PMID: 29973995 DOI: 10.1155/2018/8724549
    Acquired immunodeficiency syndrome (AIDS) cases are on the rise globally. To date, there is still no effective measure to eradicate the causative agent, human immunodeficiency virus (HIV). Highly active antiretroviral therapy (HAART) is being used in HIV/AIDS management, but it results in long-term medication and has major drawbacks such as multiple side effects, high cost, and increasing the generation rate of escape mutants. In addition, HAART does not control HIV-related complications, and hence more medications and further management are required. With this, other alternatives are urgently needed. In the past, small-molecule inhibitors have shown potent antiviral effects, and some of them are now being evaluated in clinical trials. The challenges in developing these small molecules for clinical use include the off-target effect, poor stability, and low bioavailability. On the other hand, antibody-mediated therapy has emerged as an important therapeutic modality for anti-HIV therapeutics development. Many antiviral antibodies, namely, broad neutralizing antibodies (bnAbs) against multiple strains of HIV, have shown promising effects in vitro and in animal studies; further studies are ongoing in clinical trials to evaluate their uses in clinical applications. This short review aims to discuss the current development of therapeutic antibodies against HIV and the challenges in adopting them for clinical use.
    Matched MeSH terms: Biological Availability
  11. Fulltext Does cooking affect the phytate content in local soy based dishes?
    Shimi, G., Hasnah, H.
    International Food Research Journal, 2013;20(5):2873-2880.
    MyJurnal
    This study aimed to determine the effect of cooking on phytate content and the inhibitory effects of phytate on the bioavailability of minerals in eight Malaysian soy based dishes. Phytate was analyzed by using anion-exchange chromatography while minerals were analyzed by using Atomic Absorption Spectrophotometer. Molar ratios were obtained by dividing the mole of phytate to minerals. Phytate content was reduced in cooked dishes compared to the raw ones but it was not significantly different (P > 0.05). Raw, cooked and whole dish soy products contained 257.14-900.00, 182.14-803.57 and 289.29-910.71 mg/100 g phytate, respectively. Boiling and steaming have reduced most phytate content in the food samples. Molar ratios for phytate/minerals in these samples (phytate/Ca >0.17; phytate/Fe >1) indicated that phytate content inhibited the absorption of calcium and iron. However, the ratio for Ca × phytate/Zn in all samples was less than 200 which showed that phytate did not affect the bioavailability of zinc.
    Matched MeSH terms: Biological Availability
  12. Preparation, in-vitro and in-vivo characterisation of CoQ10 microparticles: electrospraying-enhanced bioavailability
    Fung WY, Liong MT, Yuen KH
    J Pharm Pharmacol, 2016 Feb;68(2):159-69.
    PMID: 26730452 DOI: 10.1111/jphp.12502
    OBJECTIVES: This study aimed to prepare Coenzyme Q10 (CoQ10) microparticles using electrospraying technology, and evaluate the in-vitro properties and in-vivo oral bioavailability.
    KEY FINDINGS: Electrospraying was successfully used to prepare CoQ10 to enhance its solubility and dissolution properties. In-vitro evaluation of the electrosprayed microparticles showed bioavailability-enhancing properties such as reduced crystallinity and particle size. The formulation was evaluated using dissolution study and in-vivo oral bioavailability using rat model. The dissolution study revealed enhanced dissolution properties of electrosprayed microparticles compared with physical mixture and raw material. The absorption profiles showed increasing mean plasma levels CoQ10 in the following order: raw material < physical mixture < electrosprayed microparticles.
    CONCLUSION: Based on the findings in this study, electrospraying is a highly prospective technology to produce functional nano- and micro-structures as delivery vehicles for drugs with poor oral bioavailability due to rate-limiting solubility.
    Matched MeSH terms: Biological Availability
  13. Recent Advances in Drug Delivery of Polymeric Nano-Micelles
    Aziz ZABA, Ahmad A, Mohd-Setapar SH, Hassan H, Lokhat D, Kamal MA, et al.
    Curr Drug Metab, 2017;18(1):16-29.
    PMID: 27654898 DOI: 10.2174/1389200217666160921143616
    In clinical studies, drugs with hydrophobic characteristic usually reflect low bioavailability, poor drug absorption, and inability to achieve the therapeutic concentration in blood. The production of poor solubility drugs, in abundance, by pharmaceutical industries calls for an urgent need to find the alternatives for resolving the above mentioned shortcomings. Poor water solubility drugs loaded with polymeric micelle seem to be the best alternative to enhance drugs solubility and bioavailability. Polymeric micelle, formed by self-assembled of amphiphilic block copolymers in aqueous environment, functioned as solubilizing agent for hydrophobic drug. This review discusses the fundamentals of polymeric micelle as drug carrier through representative literature, and demonstrates some applications in various clinical trials. The structure, characteristic, and formation of polymeric micelle have been discussed firstly. Next, this manuscript focuses on the potential of polymeric micelles as drug vehicle in oral, transdermal routes, and anti-cancer agent. Several results from previous studies have been reproduced in this review in order to prove the efficacy of the micelles in delivering hydrophobic drugs. Lastly, future strategies to broaden the application of polymeric micelles in pharmaceutical industries have been highlighted.
    Matched MeSH terms: Biological Availability
  14. Fulltext Development and Evaluation of Self-Emulsifying Drug-Delivery System-Based Tablets for Simvastatin, a BCS Class II Drug
    Bashir MA, Khan A, Shah SI, Ullah M, Khuda F, Abbas M, et al.
    Drug Des Devel Ther, 2023;17:261-272.
    PMID: 36726738 DOI: 10.2147/DDDT.S377686
    BACKGROUND: Self-emulsifying drug-delivery systems (SEDDSs) are designed to improve the oral bioavailability of poorly water-soluble drugs. This study aimed at formulating and characterization of SEDDS-based tablets for simvastatin using castor and olive oils as solvents and Tween 60 as surfactant.

    METHODS: The liquids were adsorbed on microcrystalline cellulose, and all developed formulations were compressed using 10.5 mm shallow concave round punches.

    RESULTS: The resulting tablets were evaluated for different quality-control parameters at pre- and postcompression levels. Simvastatin showed better solubility in a mixture of oils and Tween 60 (10:1). All the developed formulations showed lower self-emulsification time (˂200 seconds) and higher cloud point (˃60°C). They were free of physical defects and had drug content within the acceptable range (98.5%-101%). The crushing strength of all formulations was in the range of 58-96 N, and the results of the friability test were within the range of USP (≤1). Disintegration time was within the official limits (NMT 15 min), and complete drug release was achieved within 30 min.

    CONCLUSION: Using commonly available excipients and machinery, SEDDS-based tablets with better dissolution profile and bioavailability can be prepared by direct compression. These S-SEDDSs could be a better alternative to conventional tablets of simvastatin.

    Matched MeSH terms: Biological Availability
  15. Higher Risks of Copper Toxicity in Turbid Waters: Quantifying the Bioavailability of Particle-Bound Metals to Set Site-Specific Water Quality Criteria
    Cao X, Yu ZX, Xie M, Pan K, Tan QG
    Environ Sci Technol, 2023 Jan 17;57(2):1060-1070.
    PMID: 36595456 DOI: 10.1021/acs.est.2c06447
    In coastal waters, particulate metals constitute a substantial fraction of the total metals; however, the prevalent water quality criteria are primarily based on dissolved metals, seemingly neglecting the contribution of particulate metals. Here we developed a method to quantify the toxicity risk of particulate metals, and proposed a way to calculate modifying factors (MFs) for setting site-specific criteria in turbid waters. Specifically, we used a side-by-side experimental design to study copper (Cu) bioaccumulation and toxicity in an estuarine clam, Potamocorbula laevis, under the exposure to "dissolved only" and "dissolved + particulate" 65Cu. A toxicokinetic-toxicodynamic model (TK-TD) was used to quantify the processes of Cu uptake, ingestion, assimilation, egestion, and elimination, and to relate mortality risk to tissue Cu. We find that particulate Cu contributes 40-67% of the Cu bioaccumulation when the suspended particulate matter (SPM) ranges from 12 to 229 mg L-1. The Cu-bearing SPM also increases the sensitivity of organisms to internalized Cu by decreasing the internal threshold concentration (CIT) from 141 to 76.8 μg g-1. MFs were derived based on the TK-TD model to consider the contribution of particulate Cu (in the studied SPM range) for increasing Cu bioaccumulation (MF = 1.3-2.2) and toxicity (MF = 2.3-3.9). Water quality criteria derived from dissolved metal exposure need to be lowered by dividing by an MF to provide adequate protection. Overall, the method we developed provides a scientifically sound framework to manage the risks of metals in turbid waters.
    Matched MeSH terms: Biological Availability
  16. Chemical speciation and bioavailability of rare earth elements (REEs) in the ecosystem: a review
    Khan AM, Bakar NKA, Bakar AFA, Ashraf MA
    Environ Sci Pollut Res Int, 2017 Oct;24(29):22764-22789.
    PMID: 27722986 DOI: 10.1007/s11356-016-7427-1
    Rare earths (RE), chemically uniform group of elements due to similar physicochemical behavior, are termed as lanthanides. Natural occurrence depends on the geological circumstances and has been of long interest for geologist as tools for further scientific research into the region of ores, rocks, and oceanic water. The review paper mainly focuses to provide scientific literature about rare earth elements (REEs) with potential environmental and health effects in understanding the research. This is the initial review of RE speciation and bioavailability with current initiative toward development needs and research perceptive. In this paper, we have also discussed mineralogy, extraction, geochemistry, analytical methods of rare earth elements. In this study, REEs with their transformation and vertical distribution in different environments such as fresh and seawater, sediments, soil, weathering, transport, and solubility have been reported with most recent literature along key methods of findings. Speciation and bioavailability have been discussed in detail with special emphasis on soil, plant, and aquatic ecosystems and their impacts on the environment. This review shows that REE gained more importance in last few years due to their detrimental effects on living organisms, so their speciation, bioavailability, and composition are much more important to evaluate their health risks and are discussed thoroughly as well.
    Matched MeSH terms: Biological Availability
  17. Effect of monsoon on microplastic bioavailability and ingestion by zooplankton in tropical coastal waters of Sabah
    Tang CN, Kuwahara VS, Leong SCY, Moh PY, Yoshida T
    Mar Pollut Bull, 2023 Aug;193:115182.
    PMID: 37352797 DOI: 10.1016/j.marpolbul.2023.115182
    Plankton seasonality in tropical coastal waters is becoming more apparent as a result of monsoon-driven changes in environmental conditions, but research on the monsoonal variation of microplastics (MP) is still limited. We examined the monsoonal variation of MP in the water column and their ingestion by zooplankton in Sepanggar Bay, Sabah, Malaysia. MP concentrations were significantly higher during the Southwest monsoon whereas MP ingestions showed no monsoonal difference across major zooplankton taxa. Canonical Correspondence Analysis (CCA) and Generalized Additive Models (GAM) indicate that MP concentrations were driven by changes in rainfall and salinity while MP bioavailability to zooplankton was consistent regardless of monsoon. MP ingestion increased progressively up the planktonic food chain, and bioavailability of fibers and small-sized MP of high-density polymers to zooplankton was proportionately higher. Distinct changes in the MP concentration relative to the monsoons provide new insights into the seasonal variation of MP in tropical coastal ecosystems.
    Matched MeSH terms: Biological Availability
  18. Lopinavir-Loaded Self-Nanoemulsifying Drug Delivery System for Enhanced Solubility: Development, Characterisation and Caco-2 Cell Uptake
    Khan AA, Akhtar S, Yadav Y, Atiya A, Alelwani W, Bannunah AM, et al.
    Curr Drug Deliv, 2023;20(10):1474-1486.
    PMID: 35980056 DOI: 10.2174/1567201819666220817111054
    BACKGROUND: The antiretroviral protease inhibitor drug, lopinavir (LPV), is used to treat HIV-1 infection. LPV is known to have limited oral bioavailability, which may be attributed to its poor aqueous solubility, low efficacy and high first-pass metabolism. Self-nanoemulsifying drug delivery systems (SNEDDS) for LPV have been developed and optimised to counter the current issues.

    METHODS: The titration method was used to prepare LPV-loaded SNEDDS (LPV-SNEDDS). Six different pseudo-ternary phase diagrams were constructed to identify the nanoemulsifying region. The developed formulations were chosen in terms of globule size < 100 nm, dispersity ≤ 0.5, dispersibility (Grade A) and% transmittance > 85. Heating-cooling cycle, freeze-thaw cycle, and centrifugation studies were performed to confirm the stability of the developed SNEDDS.

    RESULTS: The final LPV-SNEDDS (L-14) droplet size was 58.18 ± 0.62 nm, with polydispersity index, zeta potential, and entrapment efficiency (EE%) values of 0.326 ± 0.005, -22.08 ± 1.2 mV, and 98.93 ± 1.18%, respectively. According to high-resolution transmission electron microscopy (HRTEM) analysis, the droplets in the optimised formulation were < 60 nm in size. The selected SNEDDS released nearly 99% of the LPV within 30 min, which was significantly (p < 0.05) higher than the LPV-suspension in methylcellulose (0.5% w/v). It indicates the potential use of SNEDDS to enhance the solubility of LPV, which eventually could help improve the oral bioavailability of LPV. The Caco-2 cellular uptake study showed a significantly (p < 0.05) higher LPV uptake from the SNEEDS (LPV-SNEDDS-L-14) than the free LPV (LPV-suspension).

    CONCLUSION: The LPV-SNEDDS could be a potential carrier for LPV oral delivery.

    Matched MeSH terms: Biological Availability
  19. A Comprehensive Review on the Role of Polymers in Ocular Drug Delivery
    Paramjot, Wadhwa S, Sharma A, Singh SK, Vishwas S, Kumar R, et al.
    Curr Drug Deliv, 2024;21(1):16-37.
    PMID: 36627785 DOI: 10.2174/1567201820666230110140312
    Amongst different routes of drug delivery systems, ophthalmic drug delivery still requires a careful investigation and strict parameter measurements because the eyes are one of the most sensitive parts of the body and require special attention. The conventional systems for eyes lead to rapid elimination of formulation and hence very small contact time on the ocular epithelium. The current review article covers various types of polymers used in ocular drug delivery along with their applications/ limitations. Polymers are widely used by researchers in prodrug techniques and as a penetration enhancer in ocular delivery. This article covers the role and use of different polymeric systems which makes the final formulation a promising candidate for ophthalmic drug delivery. The researchers are still facing multiple challenges in order to maintain the therapeutic concentration of the drug in the eyes because of its complex structure. There are several barriers that further restrict the intraocular entry of the drug. In order to remove/reduce such challenges, these days various types of polymers are used for ocular delivery in order to develop different drug carrier systems for better efficacy and stability. The polymers used are highly helpful in increasing residence time by increasing the viscosity at the ocular epithelium layer. Such preparations also get easily permeated in ocular cells. The combination of different polymeric properties makes the final formulation stable with prolonged retention, high viscosity, high permeability, and better bioavailability, making the final formulation a promising candidate for ocular drug delivery.
    Matched MeSH terms: Biological Availability
  20. Solid Lipid Nanoparticles of Atovaquone Based on 2(4) Full-Factorial Design
    Mohtar N, A K Khan N, Darwis Y
    Iran J Pharm Res, 2015;14(4):989-1000.
    PMID: 26664366
    Solid lipid nanoparticles of atovaquone (ATQ-SLN) were prepared by high shear homogenization method using tripalmitin, trilaurin, and Compritol 888 ATO as the lipid matrices and Phospholipon 90H, Tween 80, and poloxamer 188 as the surfactants. Optimization of the formulations was conducted using 6 sets of 2(4) full-factorial design based on four independent variables that were the number of homogenizing cycles, concentration of the lipid, concentration of the co-surfactant, and concentration of the main surfactant. The dependent variables were particle size and polydispersity index (PdI). The homogenizing cycles showed a negative influence on the dependent variables which reduced both the particle size and the PdI value. Moreover, a combination of certain percentages of the main surfactant and co-surfactant also showed a negative influence that reduced both the particle size and PdI value. Selected formulations from each design were further characterized for the entrapment efficiency and yield. The optimised formulation of ATQ-SLN consisted of trilaurin, Phospholipon 90H and Tween 80 with a particle size of 89.4 ± 0.2 nm and entrapment efficiency of 83.0 ± 1.7%. The in-vitro release evaluation of the formulation showed a complete and immediate release of ATQ from the SLN that could be a solution to improve the poor aqueous solubility and hence poor bioavailability of the drug.
    Matched MeSH terms: Biological Availability
Related Terms
Filters
Contact Us

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

External Links