Displaying publications 61 - 80 of 198 in total

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  1. Fulltext Nano-Formulation of Ethambutol with Multifunctional Graphene Oxide and Magnetic Nanoparticles Retains Its Anti-Tubercular Activity with Prospects of Improving Chemotherapeutic Efficacy
    Saifullah B, Maitra A, Chrzastek A, Naeemullah B, Fakurazi S, Bhakta S, et al.
    Molecules, 2017 Oct 12;22(10).
    PMID: 29023384 DOI: 10.3390/molecules22101697
    Tuberculosis (TB) is a dreadful bacterial disease, infecting millions of human and cattle every year worldwide. More than 50 years after its discovery, ethambutol continues to be an effective part of the World Health Organization's recommended frontline chemotherapy against TB. However, the lengthy treatment regimens consisting of a cocktail of antibiotics affect patient compliance. There is an urgent need to improve the current therapy so as to reduce treatment duration and dosing frequency. In this study, we have designed a novel anti-TB multifunctional formulation by fabricating graphene oxide with iron oxide magnetite nanoparticles serving as a nano-carrier on to which ethambutol was successfully loaded. The designed nanoformulation was characterised using various analytical techniques. The release of ethambutol from anti-TB multifunctional nanoparticles formulation was found to be sustained over a significantly longer period of time in phosphate buffer saline solution at two physiological pH (7.4 and 4.8). Furthermore, the nano-formulation showed potent anti-tubercular activity while remaining non-toxic to the eukaryotic cells tested. The results of this in vitro evaluation of the newly designed nano-formulation endorse its further development in vivo.
    Matched MeSH terms: Drug Liberation
  2. Multiboronic acid-conjugated chitosan scaffolds with glucose selectivity to insulin release
    Siddiqui NA, Billa N, Roberts CJ
    J Biomater Sci Polym Ed, 2017 Jun;28(8):781-793.
    PMID: 28278045 DOI: 10.1080/09205063.2017.1301774
    The principal challenge for the use of boronic acids (BA) as glucose sensors is their lack of specificity for glucose. We examined the selectivity of and insulin release from two boronic acids- (2-formyl-3-thienylboronic acid (FTBA) and 4-formylphenylboronic acid (FPBA)) conjugated chitosan scaffolds to glucose and fructose. Adsorption of glucose to BA: chitosan conjugates was dose-dependent up to 1:1 at 35 and 42% for FPBA and FTBA respectively but the FTBA conjugates adsorbed more glucose and fructose at respective FPBA ratios. The affinity of both BA conjugates to glucose decreased with increase in BA ratio. On the other hand, the affinity of both BA conjugates for fructose decreased from ratio 1:1 to 2:1 then rose again at 3:1. Insulin release from FPBA nanoparticles (FPBAINP) and FTBA nanoparticles (FTBAINP) were both concentration-dependent within glyceamically relevant values (1-3 mg/ml glucose and 0.002 mg/ml fructose). Furthermore, the total amounts of insulin released from FPBAINP in both the media were higher than from FTBAINP. Both FPBAINP and FTBAINP have the potential for development as a glucose-selective insulin delivery system in physiological settings.
    Matched MeSH terms: Drug Liberation*
  3. Mucoadhesive guargum hydrogel inter-connected chitosan-g-polycaprolactone micelles for rifampicin delivery
    Yuan X, Amarnath Praphakar R, Munusamy MA, Alarfaj AA, Suresh Kumar S, Rajan M
    Carbohydr Polym, 2019 Feb 15;206:1-10.
    PMID: 30553301 DOI: 10.1016/j.carbpol.2018.10.098
    Natural polymer guar gum has one of the highest viscosities in water solution and hence, these are significantly used in pharmaceutical applications. Guar gum inter-connected micelles as a new carrier has been developed for poor water soluble rifampicin drug. The hydrogel inter-connected micelle core was formulated as a hydrophilic inner and hydrophobic outer core by using guar gum/chitosan/polycaprolactone and the carrier interaction with rifampicin was confirmed by FT-IR. The morphological observations were carried out through TEM, SEM and AFM analysis. The encapsulation efficiency and in-vitro drug release behavior of prepared hydrogel based micelle system was analyzed by UV-vis spectrometry. The anti-bacterial activity against K. pneumoniae and S. aureus was studied by observing their ruptured surface by SEM. The cytotoxicity study reveals that the pure polymeric system has no toxic effect whereas drug loaded ones showed superior activity against THP-1 cells. From the cell apoptosis analyses, the apoptosis was carried out in a time dependent manner. The cell uptake behavior was also observed in THP-1 cells which indicate that the hydrogel based micelle system is an excellent material for the mucoadhesive on intracellular alveolar macrophage treatment.
    Matched MeSH terms: Drug Liberation
  4. Fulltext Morphological Changes and Cellular Uptake of Functionalized Graphene Oxide Loaded with Protocatechuic Acid and Folic Acid in Hepatocellular Carcinoma Cancer Cell
    Buskaran K, Hussein MZ, Mohd Moklas MA, Fakurazi S
    Int J Mol Sci, 2020 Aug 16;21(16).
    PMID: 32824281 DOI: 10.3390/ijms21165874
    The development of nanocomposites has swiftly changed the horizon of drug delivery systems in defining a new platform. Major understanding of the interaction of nanocomposites with cells and how the interaction influences intracellular uptake is an important aspect to study in order to ensure successful utilisation of the nanocomposites. Studies have suggested that the nanocomposites' ability to permeate into biological cells is attributable to their well-defined physicochemical properties with nanoscale size, which is relevant to the nanoscale components of biology and cellular organelles. The functionalized graphene oxide coated with polyethylene glycol, loaded with protocatechuic acid and folic acid (GOP-PCA-FA) nanocomposite intracellular uptake was analysed using transmission electron microscope. The accumulation of fluorescent-labelled nanocomposites in the HepG2 cell was also analysed using a fluorescent microscope. In vitro cellular uptake showed that there was uptake of the drug from 24 h into the cells and the release study using fluorescently tagged nanocomposite demonstrated that release and accumulation were observed at 24 h and 48 h. Moreover, the migration ability of tumor cells is a key step in tumor progression which was observed 48 h after treatment. The GOP serves as a potential nanocarrier system which is capable of improving the therapeutic efficacy of drugs and biomolecules in medical as well as pharmaceutical applications through the enhanced intracellular release and accumulation of the encapsulated drugs. Nonetheless, it is essential to analyse the translocation of our newly developed GOP-PCA-FA, and its efficiency for drug delivery, effective cellular uptake, and abundant intracellular accumulation would be compromised by possible untoward side effects.
    Matched MeSH terms: Drug Liberation
  5. Molecular Evaluation of Oral Immunogenicity of Hepatitis B Antigen Delivered by Hydrogel Microparticles
    Chen XY, Butt AM, Mohd Amin MCI
    Mol Pharm, 2019 09 03;16(9):3853-3872.
    PMID: 31398038 DOI: 10.1021/acs.molpharmaceut.9b00483
    The development of oral vaccine formulation is crucial to facilitate an effective mass immunization program for various vaccine-preventable diseases. In this work, the efficacy of hepatitis B antigen delivered by bacterial nanocellulose/poly(acrylic acid) composite hydrogel microparticles (MPs) as oral vaccine carriers was assessed to induce both local and systemic immunity. Optimal pH-responsive swelling, mucoadhesiveness, protein drug loading, and drug permeability were characterized by MPs formulated with minimal irradiation doses and acrylic acid concentration. The composite hydrogel materials of bacterial nanocellulose and poly(acrylic acid) showed significantly greater antigen release in simulated intestinal fluid while ensuring the integrity of antigen. In in vivo study, mice orally vaccinated with antigen-loaded hydrogel MPs showed enhanced vaccine immunogenicity with significantly higher secretion of mucosal immunoglobulin A, compared to intramuscular vaccinated control. The splenocytes from the same group demonstrated lymphoproliferation and significant increased secretion of interleukin-2 cytokines upon stimulation with hepatitis B antigen. Expression of CD69 in CD4+ T lymphocytes and CD19+ B lymphocytes in splenocytes from mice orally vaccinated with antigen-loaded hydrogel MPs was comparable to that of the intramuscular vaccinated control, indicating early activation of lymphocytes elicited by our oral vaccine formulation in just two doses. These results demonstrated the potential of antigen-loaded hydrogel MPs as an oral vaccination method for hepatitis B.
    Matched MeSH terms: Drug Liberation
  6. Fulltext Modified methods of nanoparticles synthesis in pH-sensitive nano-carriers production for doxorubicin delivery on MCF-7 breast cancer cell line
    Hamidu A, Mokrish A, Mansor R, Razak ISA, Danmaigoro A, Jaji AZ, et al.
    Int J Nanomedicine, 2019;14:3615-3627.
    PMID: 31190815 DOI: 10.2147/IJN.S190830
    Purpose: Modified top-down procedure was successfully employed in the synthesis of aragonite nanoparticles (NPs) from cheaply available natural seawater cockle shells. This was with the aim of developing a pH-sensitive nano-carrier for effective delivery of doxorubicin (DOX) on MCF-7 breast cancer cell line. Methods: The shells were cleaned with banana pelts, ground using a mortar and pestle, and stirred vigorously on a rotary pulverizing blending machine in dodecyl dimethyl betane solution. This simple procedure avoids the use of stringent temperatures and unsafe chemicals associated with NP production. The synthesized NPs were loaded with DOX to form DOX-NPs. The free and DOX-loaded NPs were characterized for physicochemical properties using field emission scanning electron microscopy, transmission electron microscopy, zeta potential analysis, Fourier transform infrared spectroscopy, and X-ray diffraction. The release profile, cytotoxicity, and cell uptake were evaluated. Results: NPs had an average diameter of 35.50 nm, 19.3% loading content, 97% encapsulation efficiency, and a surface potential and intensity of 19.1±3.9 mV and 100%, respectively. A slow and sustained pH-specific controlled discharge profile of DOX from DOX-NPs was observed, clearly showing apoptosis/necrosis induced by DOX-NPs through endocytosis. The DOX-NPs had IC50 values 1.829, 0.902, and 1.0377 µg/mL at 24, 48, and 72 hrs, while those of DOX alone were 0.475, 0.2483, and 0.0723 µg/mL, respectively. However, even at higher concentration, no apparent toxicity was observed with the NPs, revealing their compatibility with MCF-7 cells with a viability of 92%. Conclusions: The modified method of NPs synthesis suggests the tremendous potential of the NPs as pH-sensitive nano-carriers in cancer management because of their pH targeting ability toward cancerous cells.
    Matched MeSH terms: Drug Liberation
  7. Mimosa pudica L., a High-Value Medicinal Plant as a Source of Bioactives for Pharmaceuticals
    Muhammad G, Hussain MA, Jantan I, Bukhari SNA
    Compr Rev Food Sci Food Saf, 2016 Mar;15(2):303-315.
    PMID: 33371596 DOI: 10.1111/1541-4337.12184
    Mimosa pudica Linn. (Family: Mimosaceae) is used as an ornamental plant due to its thigmonastic and nyctinastic movements. M. pudica is also used to avoid or cure several disorders like cancer, diabetes, hepatitis, obesity, and urinary infections. M. pudica is famous for its anticancer alkaloid, mimosine, along with several valuable secondary metabolites like tannins, steroids, flavonoids, triterpenes, and glycosylflavones. A wide array of pharmacological properties like antioxidant, antibacterial, antifungal, anti-inflammatory, hepatoprotective, antinociceptive, anticonvulsant, antidepressant, antidiarrheal, hypolipidemic activities, diuretic, antiparasitic, antimalarial, and hypoglycemic have been attributed to different parts of M. pudica. Glucuronoxylan polysaccharide extruded from seeds of M. pudica is used for drug release formulations due to its high swelling index. This review covers a thorough examination of functional bioactives as well as pharmacological and phytomedicinal attributes of the plant with the purpose of exploring its pharmaceutical and nutraceutical potentials.
    Matched MeSH terms: Drug Liberation
  8. Fulltext Microwave-assisted Preparation of Cross-linked Gelatin-Paracetamol Matrices: Optimization Using the D-optimal Design
    Kuang TK, Kang YB, Segarra I, Kanwal U, Ahsan M, Bukhari NI
    Turk J Pharm Sci, 2021 04 20;18(2):167-175.
    PMID: 33902255 DOI: 10.4274/tjps.galenos.2020.48902
    Objectives: This study was conducted to assess the effect of microwave heating on the preparation of paracetamol cross-linked gelatin matrices by using the design of experiment (DoE) approach and explore the influence of the duration of microwave irradiation, the concentrations of crosslinker, and the amount of sodium bicarbonate (salt) on paracetamol release. These parameters were also compared with those of the matrices prepared via conventional heating.

    Materials and Methods: Twenty gel matrices were prepared with different durations of microwave irradiation, amounts of maize, and concentrations of sodium bicarbonate as suggested by Design Expert (DX®). The percentage drug release, the coefficient of variance (CV) in release, and the mean dissolution time (MDT) were the properties explored in the designed experimentation.

    Results: Target responses were dependent on microwave irradiation time, cross-linker amount, and salt concentration. Classical and microwave heating did not demonstrate statistically significant difference in modifying the percentage of drug released from the matrices. However, the CVs of microwave-assisted formulations were lower than those of the gel matrices prepared via classical heating. Thus, microwave heating produced lesser variations in drug release. The optimized gel matrices demonstrated that the observed percentage of drug release, CV, and MDT were within the prediction interval generated by DX®. The release mechanism of the matrix formulations followed the Peppas-Korsmeyer anomalous transport model.

    Conclusion: The DoE-supported microwave-assisted approach could be applied to optimize the critical factors of drug release with less variation.

    Matched MeSH terms: Drug Liberation
  9. Methotrexate and beta-carotene loaded-lipid polymer hybrid nanoparticles: a preclinical study for breast cancer
    Jain A, Sharma G, Kushwah V, Garg NK, Kesharwani P, Ghoshal G, et al.
    Nanomedicine (Lond), 2017 Aug;12(15):1851-1872.
    PMID: 28703643 DOI: 10.2217/nnm-2017-0011
    AIM: This work was intended to investigate the targeting potential of fructose-tethered lipid-polymeric hybrid nanoparticles (F-BC-MTX-LPHNPs) co-loaded with beta carotene (BC) and methotrexate (MTX) in breast cancer therapeutics and find out the possible protective role of BC on MTX-induced toxicity.

    MATERIALS & METHODS: F-BC-MTX-LPHNPs were fabricated using self-assembled nano-precipitation technique. Fructose was conjugated on the surface of the particles. The in vitro cytotoxicity, sub-cellular localization and apoptotic activity of F-BC-MTX-LPHNPs were evaluated against MCF-7 breast cancer cells. The antitumor potential of F-BC-MTX-LPHNPs was further studied.

    RESULTS & CONCLUSION: Outcomes suggested that F-BC-MTX-LPHNPs induced the highest apoptosis index (0.89) against MCF-7 cells. Following 30 days of treatment, the residual tumor progression was assessed to be approximately 32%, in animals treated with F-BC-MTX-LPHNPs. F-BC-MTX-LPHNPs are competent to selectively convey the chemotherapeutic agent to the breast cancers. Beta carotene ameliorated MTX-induced hepatic and renal toxicity.

    Matched MeSH terms: Drug Liberation
  10. Fulltext Mechanism-based selection of stabilization strategy for amorphous formulations: Insights into crystallization pathways
    Edueng K, Mahlin D, Larsson P, Bergström CAS
    J Control Release, 2017 06 28;256:193-202.
    PMID: 28412224 DOI: 10.1016/j.jconrel.2017.04.015
    We developed a step-by-step experimental protocol using differential scanning calorimetry (DSC), dynamic vapour sorption (DVS), polarized light microscopy (PLM) and a small-scale dissolution apparatus (μDISS Profiler) to investigate the mechanism (solid-to-solid or solution-mediated) by which crystallization of amorphous drugs occurs upon dissolution. This protocol then guided how to stabilize the amorphous formulation. Indapamide, metolazone, glibenclamide and glipizide were selected as model drugs and HPMC (Pharmacoat 606) and PVP (K30) as stabilizing polymers. Spray-dried amorphous indapamide, metolazone and glibenclamide crystallized via solution-mediated nucleation while glipizide suffered from solid-to-solid crystallization. The addition of 0.001%-0.01% (w/v) HPMC into the dissolution medium successfully prevented the crystallization of supersaturated solutions of indapamide and metolazone whereas it only reduced the crystallization rate for glibenclamide. Amorphous solid dispersion (ASD) formulation of glipizide and PVP K30, at a ratio of 50:50% (w/w) reduced but did not completely eliminate the solid-to-solid crystallization of glipizide even though the overall dissolution rate was enhanced both in the absence and presence of HPMC. Raman spectroscopy indicated the formation of a glipizide polymorph in the dissolution medium with higher solubility than the stable polymorph. As a complementary technique, molecular dynamics (MD) simulations of indapamide and glibenclamide with HPMC was performed. It was revealed that hydrogen bonding patterns of the two drugs with HPMC differed significantly, suggesting that hydrogen bonding may play a role in the greater stabilizing effect on supersaturation of indapamide, compared to glibenclamide.
    Matched MeSH terms: Drug Liberation
  11. Fulltext Mathematical Model for Estimating Parameters of Swelling Drug Delivery Devices in a Two-Phase Release
    Setapa A, Ahmad N, Mohd Mahali S, Mohd Amin MCI
    Polymers (Basel), 2020 Dec 05;12(12).
    PMID: 33291495 DOI: 10.3390/polym12122921
    Various swelling drug delivery devices are promising materials for control drug delivery because of their ability to swell and release entrapped therapeutics, in response to physiological stimuli. Previously, many mathematical models have been developed to predict the mechanism of drug release from a swelling device. However, some of these models do not consider the changes in diffusion behaviour as the device swells. Therefore, we used a two-phase approach to simplify the mathematical model considering the effect of swelling on the diffusion coefficient. We began by defining a moving boundary problem to consider the swelling process. Landau transformation was used for mitigating the moving boundary problem. The transformed problem was analytically solved using the separation of variables method. Further, the analytical solution was extended to include the drug release in two phases where each phase has distinct diffusion coefficient and continuity condition was applied. The newly developed model was validated by the experimental data of bacterial cellulose hydrogels using the LSQCURVEFIT function in MATLAB. The numerical test showed that the new model exhibited notable improvement in curve fitting, and it was observed that the initial effective diffusion coefficient of the swelling device was lower than the later effective diffusion coefficient.
    Matched MeSH terms: Drug Liberation
  12. Magnetic nanocellulose alginate hydrogel beads as potential drug delivery system
    Supramaniam J, Adnan R, Mohd Kaus NH, Bushra R
    Int J Biol Macromol, 2018 Oct 15;118(Pt A):640-648.
    PMID: 29894784 DOI: 10.1016/j.ijbiomac.2018.06.043
    Magnetic nanocellulose alginate hydrogel beads are produced from the assembly of alginate and magnetic nanocellulose (m-CNCs) as a potential drug delivery system. The m-CNCs were synthesized from cellulose nanocrystals (CNCs) that were isolated from rice husks (RH) by co-precipitation method and were incorporated into alginate-based hydrogel beads with the aim of enhancing mechanical strength and regulating drug release behavior. Ibuprofen was chosen as a model drug. The prepared CNCs, m-CNCs and the alginate hydrogel beads were characterized by various physicochemical techniques such as Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), scanning electron microscope (SEM) and vibrating sample magnetometer studies (VSM). Besides the magnetic property, the presence of m-CNCs increased the integrity of the alginate hydrogel beads and the swelling percentage. The drug release study exhibited a controlled release profiles and based on the drug release data, the drug release mechanism was analyzed and discussed based on mathematical models such as Korsmeyer-Peppas and Peppas-Sahlin.
    Matched MeSH terms: Drug Liberation
  13. Magnesium-zinc scaffold loaded with tetracycline for tissue engineering application: In vitro cell biology and antibacterial activity assessment
    Dayaghi E, Bakhsheshi-Rad HR, Hamzah E, Akhavan-Farid A, Ismail AF, Aziz M, et al.
    Mater Sci Eng C Mater Biol Appl, 2019 Sep;102:53-65.
    PMID: 31147024 DOI: 10.1016/j.msec.2019.04.010
    Recently, porous magnesium and its alloys are receiving great consideration as biocompatible and biodegradable scaffolds for bone tissue engineering application. However, they presented poor antibacterial performance and corrosion resistance which limited their clinical applications. In this study, Mg-Zn (MZ) scaffold containing different concentrations of tetracycline (MZ-xTC, x = 1, 5 and 10%) were fabricated by space holder technique to meet the desirable antibacterial activity and corrosion resistance properties. The MZ-TC contains total porosity of 63-65% with pore sizes in the range of 600-800 μm in order to accommodate bone cells. The MZ scaffold presented higher compressive strength and corrosion resistance compared to pure Mg scaffold. However, tetracycline incorporation has less significant effect on the mechanical and corrosion properties of the scaffolds. Moreover, MZ-xTC scaffolds drug release profiles show an initial immediate release which is followed by more stable release patterns. The bioactivity test reveals that the MZ-xTC scaffolds are capable of developing the formation of HA layers in simulated body fluid (SBF). Next, Staphylococcus aureus and Escherichia coli bacteria were utilized to assess the antimicrobial activity of the MZ-xTC scaffolds. The findings indicate that those scaffolds that incorporate a high level concentration of tetracycline are tougher against bacterial organization than MZ scaffolds. However, the MTT assay demonstrates that the MZ scaffolds containing 1 to 5% tetracycline are more effective to sustain cell viability, whereas MZ-10TC shows some toxicity. The alkaline phosphatase (ALP) activity of the MZ-(1-5)TC was considerably higher than that of MZ-10TC on the 3 and 7 days, implying higher osteoblastic differentiation. All the findings suggest that the MZ-xTC scaffolds containing 1 to 5% tetracycline is a promising candidate for bone tissue healing due to excellent antibacterial activity and biocompatibility.
    Matched MeSH terms: Drug Liberation
  14. Fulltext Lyophilized Amorphous Dispersion of Telmisartan in a Combined Carrier-Alkalizer System: Formulation Development and In Vivo Study
    Al-Japairai KAS, Alkhalidi HM, Mahmood S, Almurisi SH, Doolaanea AA, Al-Sindi TA, et al.
    ACS Omega, 2020 Dec 22;5(50):32466-32480.
    PMID: 33376884 DOI: 10.1021/acsomega.0c04588
    Telmisartan suffers from low oral bioavailability due to its poor water solubility. The research work presents a formulation of solid dispersed (SD) telmisartan formulation as a ternary mixture of a drug, a polymeric carrier (poly(vinylpyrrolidone) (PVP) K30), and an alkalizer (Na2CO3). The preparation method, which was lyophilization of an aqueous solution containing the ingredients, was free from any organic solvent. The developed SD formulations resulted in a significant improvement in in vitro dissolution (>90% drug dissolution in 15 min) compared to pure telmisartan. Solid-state characterization by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD) studies indicated the conversion of crystalline telmisartan into an amorphous form. Fourier transform infrared (FTIR) spectroscopy revealed the drug-polymer interaction that was responsible for reducing the chances of recrystallization. A short-term stability study showed that selected SD formulations were stable in terms of in vitro dissolution and retained their amorphous structure in ambient and accelerated conditions over 2 months. Selected formulations (drug/PVP K30/Na2CO3 as 1:1:2 or 1:2:2 weight ratio) resulted in >2.48 times relative oral bioavailability compared to marketed formulations. It was considered that the incorporation of an alkalizer and a hydrophilic polymer, and amorphization of telmisartan by lyophilization, could enhance in vitro dissolution and improve oral bioavailability.
    Matched MeSH terms: Drug Liberation
  15. Lycopene loaded whey protein isolate nanoparticles: An innovative endeavor for enhanced bioavailability of lycopene and anti-cancer activity
    Jain A, Sharma G, Ghoshal G, Kesharwani P, Singh B, Shivhare US, et al.
    Int J Pharm, 2018 Jul 30;546(1-2):97-105.
    PMID: 29715533 DOI: 10.1016/j.ijpharm.2018.04.061
    The work entails a novel strategy of formulating the lycopene loaded whey protein isolate nanoparticles (LYC-WPI-NPs) solely using the rational blend of biomacromolecule without using equipment-intensive techniques. The LYC-WPI-NPs were fabricated as a substantial drug delivery platform, with maximum entrapment, spatial and controlled release manners, exceptional plasma concentration, and perspective for discrepancy delivery of therapeutics. Prepared nano-formulations were measured in ultra-fine size (100-350 nm) with sphere-shaped. The percent lycopene entrapment of prepared LYC-WPI-NPs was estimated in the range to 50 and 65%. In vitro percent cumulative release study demonstrated deaden and extended release i.e. approximately 75% following 16th h. The in vitro percent cell survival (cytotoxicity study) of prepared nanoparticles was evaluated against MCF-7 breast cancer cells by MTT based colorimetric assay. Sub-cellular localization of lycopene when delivered by LYC-WPI-NPs was assessed by HPLC (high performance liquid chromatography). The WPI-NPs enhance the oral bioavailability of lycopene by controlling its release from nano-formulation and facilitating its absorption through lymphatic pathways. Prophylactic anticancer efficacy of LYC-WPI-NPs was evaluated thereafter on experimentally induced breast cancer animal model. Conclusively, it may quite reasonable that lycopene loaded protein nanoparticles are competent to improve the biopharmaceutical attributes of lycopene and demonstrated prophylactic anticancer activity, decrease tumor proliferation and increase the survival rate of treated animals, thus signifying their feasible usefulness in cancer therapeutic and intervention.
    Matched MeSH terms: Drug Liberation
  16. Low-melting-point polymeric nanoshells for thermal-triggered drug release under hyperthermia condition
    Dabbagh A, Mahmoodian R, Abdullah BJ, Abdullah H, Hamdi M, Abu Kasim NH
    Int J Hyperthermia, 2015;31(8):920-9.
    PMID: 26670340 DOI: 10.3109/02656736.2015.1094147
    The aim of this paper was to synthesise core-shell nanostructures comprised of mesoporous silica core and a low melting-point polyethylene glycol (PEG) nanoshell with a sharp gel-liquid phase transition for rapid drug release at hyperthermia temperature range.
    Matched MeSH terms: Drug Liberation
  17. 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: Drug Liberation
  18. Kondogogu gum-Zn(+2)-pectinate emulgel matrices reinforced with mesoporous silica for intragastric furbiprofen delivery
    Bera H, Nadimpalli J, Kumar S, Vengala P
    Int J Biol Macromol, 2017 Nov;104(Pt A):1229-1237.
    PMID: 28688948 DOI: 10.1016/j.ijbiomac.2017.07.027
    Flurbiprofen (FLU), a non-steroidal anti-inflammatory drug, exhibits limited clinical response due to its poor physicochemical properties. This study aimed at developing reliable drug carriers for intrgastric FLU delivery with a view to improve biopharmaceutical characteristics of drug and modulate its release in a controlled manner. In this context, FLU-loaded kondogogu gum (KG)-Zn(+2)-low methoxyl (LM) pectinate emulgel matrices reinforced with calcium silicate (CS) were accomplished by ionotropic gelation technique employing zinc acetate as cross-linker and characterized for their in vitro performances. All the formulations demonstrated excellent drug encapsulation efficiency (DEE, 46-87%) and sustained drug release behavior (Q7h, 70-91%). These quality attributes were remarkably influenced by polymer-blend (LM pectin:KG) ratios, low-density oil types and CS inclusion. The drug release profile of the FLU-loaded optimized matrices (F-7) was best fitted in Korsmeyer-Peppas model with Fickian diffusion driven mechanism. It also conferred excellent in vitro gastroretention capabilities. Moreover, the drug-excipient compatibility, alteration of crystallinity and thermal behavior of drug and surface morphology of matrices were evidenced with the results of FTIR, XRD, DSC and SEM analyses, respectively. Thus, the newly developed matrices are appropriate for sustained intragastric FLU delivery and simultaneous zinc supplementation for effective inflammation and arthritis management.
    Matched MeSH terms: Drug Liberation
  19. Investigation on the effect of polymer and starch on the tablet properties of lyophilized orally disintegrating tablet
    Liew KB, Peh KK
    Arch Pharm Res, 2021 Aug;44(8):1-10.
    PMID: 25579848 DOI: 10.1007/s12272-014-0542-y
    Orally disintegrating tablet (ODT) is a user friendly and convenient dosage form. The study aimed to investigate the effect of polymers and wheat starch on the tablet properties of lyophilized ODT, with dapoxetine as model drug. Three polymers (hydroxypropylmethyl cellulose, carbopol 934P and Eudragit® EPO) and wheat starch were used as matrix forming materials in preparation of lyophilized ODT. The polymeric dispersion was casted into a mould and kept in a freezer at -20 °C for 4 h before freeze dried for 12 h. It was found that increasing in HPMC and Carbopol 934P concentrations produced tablets with higher hardness and longer disintegration time. In contrast, Eudragit® EPO was unable to form tablet with sufficient hardness at various concentrations. Moreover, HPMC seems to have a stronger effect on tablet hardness compared to Carbopol 934P at the same concentration level. ODT of less friable was obtained. Wheat starch acted as binder which strengthen the hardness of ODTs and prolonged the disintegration time. ODT comprising of HPMC and wheat starch at ratio of 2:1 was found to be optimum based upon the tablet properties. The optimum formulation was palatable and 80 % of the drug was released within 30 min in the dissolution study.
    Matched MeSH terms: Drug Liberation
  20. Investigation on solution-to-gel characteristic of thermosensitive and mucoadhesive biopolymers for the development of moxifloxacin-loaded sustained release periodontal in situ gels
    Sheshala R, Quah SY, Tan GC, Meka VS, Jnanendrappa N, Sahu PS
    Drug Deliv Transl Res, 2019 04;9(2):434-443.
    PMID: 29392681 DOI: 10.1007/s13346-018-0488-6
    The objectives of present research were to develop and characterize thermosensitive and mucoadhesive polymer-based sustained release moxifloxacin in situ gels for the treatment of periodontal diseases. Poloxamer- and chitosan-based in situ gels are in liquid form at room temperature and transform into gel once administered into periodontal pocket due to raise in temperature to 37 °C. Besides solution-to-gel characteristic of polymers, their mucoadhesive nature aids the gel to adhere to mucosa in periodontal pocket for prolonged time and releases the drug in sustained manner. These formulations were prepared using cold method and evaluated for pH, solution-gel temperature, syringeability and viscosity. In vitro drug release studies were conducted using dialysis membrane at 37 °C and 50 rpm. Antimicrobial studies carried out against Aggregatibacter actinomycetemcomitans (A.A.) and Streptococcus mutans (S. Mutans) using agar cup-plate method. The prepared formulations were clear and pH was at 7.01-7.40. The viscosity of formulations was found to be satisfactory. Among the all, formulations comprising of 21% poloxamer 407 and 2% poloxamer 188 (P5) and in combination with 0.5% HPMC (P6) as well as 2% chitosan and 70% β-glycerophosphate (C6) demonstrated an ideal gelation temperature (33-37 °C) and sustained the drug release for 8 h. Formulations P6 and C6 showed promising antimicrobial efficacy with zone of inhibition of 27 mm for A.A. and 55 mm for S. Mutans. The developed sustained release in situ gel formulations could enhance patient's compliance by reducing the dosing frequency and also act as an alternative treatment to curb periodontitis.
    Matched MeSH terms: Drug Liberation
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