Displaying publications 81 - 100 of 200 in total

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  1. Moniri M, Boroumand Moghaddam A, Azizi S, Abdul Rahim R, Zuhainis SW, Navaderi M, et al.
    Int J Nanomedicine, 2018;13:5097-5112.
    PMID: 30254435 DOI: 10.2147/IJN.S164573
    Background: In recent years, bacterial nanocellulose (BNC) based nanocomposites have been developed to promote healing property and antibacterial activity of BNC wound dressing. Molecular study can help to better understanding about interaction of genes and pathways involved in healing progression.

    Objectives: The aim of this study was to prepare bacterial nanocellulose/silver (BNC/Ag) nanocomposite films as ecofriendly wound dressing in order to assess their physical, cytotoxicity and antimicrobial properties. The in vitro molecular study was performed to evaluate expression of genes involved in healing of wounds after treatment with BNC/Ag biofilms.

    Study design materials and methods: Silver nanoparticles were formed by using Citrullus colocynthis extract within new isolated bacterial nanocellulose (BNC) RM1. The nanocomposites were characterized using X-ray diffraction, Fourier transform infrared, and field emission scanning electron microscopy. Besides, swelling property and Ag release profile of the nanocomposites were studied. The ability of nanocomposites to promote wound healing of human dermal fibroblast cells in vitro was studied. Bioinformatics databases were used to identify genes with important healing effect. Key genes which interfered with healing were studied by quantitative real time PCR.

    Results: Spherical silver nanoparticles with particle size ranging from 20 to 50 nm were synthesized and impregnated within the structure of BNC. The resulting nanocomposites showed significant antibacterial activities with inhibition zones ranging from 7±0.25 to 16.24±0.09 mm against skin pathogenic bacteria. Moreover, it was compatible with human fibroblast cells (HDF) and could promote in vitro wound healing after 48h. Based on bioinformatics databases, the genes of TGF-β1, MMP2, MMP9, CTNNB1, Wnt4, hsa-miR-29b-3p and hsa-miR-29c-3p played important role in wound healing. The nanocomposites had an effect in expression of the genes in healing. Thus, the BNC/Ag nanocomposite can be used to heal wound in a short period and simple manner.

    Conclusion: This eco-friendly nanocomposite with excellent antibacterial activities and healing property confirming its utility as potential wound dressings.

    Matched MeSH terms: Drug Liberation
  2. 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
  3. Pramanik A, Xu Z, Shamsuddin SH, Khaled YS, Ingram N, Maisey T, et al.
    ACS Appl Mater Interfaces, 2022 Mar 09;14(9):11078-11091.
    PMID: 35196008 DOI: 10.1021/acsami.1c21655
    Nanomedicines, while having been approved for cancer therapy, present many challenges such as low stability, rapid clearance, and nonspecificity leading to off-target toxicity. Cubosomes are porous lyotropic liquid crystalline nanoparticles that have shown great premise as drug delivery vehicles; however, their behavior in vivo is largely underexplored, hindering clinical translation. Here, we have engineered cubosomes based on the space group Im3m that are loaded with copper acetylacetonate as a model drug, and their surfaces are functionalized for the first time with Affimer proteins via copper-free click chemistry to actively target overexpressed carcinoembryonic antigens on LS174T colorectal cancer cells. Unlike nontargeted cubosomes, Affimer tagged cubosomes showed preferential accumulation in cancer cells compared to normal cells not only in vitro (2D monolayer cell culture and 3D spheroid models) but also in vivo in colorectal cancer mouse xenografts, while exhibiting low nonspecific absorption and toxicity in other vital organs. Cancerous spheroids had maximum cell death compared to noncancerous cells upon targeted delivery. Xenografts subjected to targeted drug-loaded cubosomes showed a 5-7-fold higher drug accumulation in the tumor tissue compared to the liver, kidneys, and other vital organs, a significant decrease in tumor growth, and an increased survival rate compared to the nontargeted group. This work encompasses the first thorough preclinical investigation of Affimer targeted cubosomes as a cancer therapeutic.
    Matched MeSH terms: Drug Liberation
  4. Ullah F, Javed F, Othman MBH, Khan A, Gul R, Ahmad Z, et al.
    J Biomater Sci Polym Ed, 2018 03;29(4):376-396.
    PMID: 29285989 DOI: 10.1080/09205063.2017.1421347
    Addressing the functional biomaterials as next-generation therapeutics, chitosan and alginic acid were copolymerized in the form of chemically crosslinked interpenetrating networks (IPNs). The native hydrogel was functionalized via carbodiimide (EDC), catalyzed coupling of soft ligand (1,2-Ethylenediamine) and hard ligand (4-aminophenol) to replace -OH groups in alginic acid units for extended hydrogel- interfaces with the aqueous and sparingly soluble drug solutions. The chemical structure, Lower solution critical temperature (LCST ≈ 37.88 °C), particle size (Zh,app ≈ 150-200 nm), grain size (160-360 nm), surface roughness (85-250 nm), conductivity (37-74 mv) and zeta potential (16-32 mv) of native and functionalized hydrogel were investigated by using FT-IR, solid state-13C-NMR, TGA, DSC, FESEM, AFM and dynamic light scattering (DLS) measurements. The effective swelling, drug loading (47-78%) and drug release (53-86%) profiles were adjusted based on selective functionalization of hydrophobic IPNs due to electrostatic complexation and extended interactions of hydrophilic ligands with the aqueous and drug solutions. Drug release from the hydrogel matrices with diffusion coefficient n ≈ 0.7 was established by Non- Fickian diffusion mechanism. In vitro degradation trials of the hydrogel with a 20% loss of wet mass in simulated gastric fluid (SGF) and 38% loss of wet mass in simulated intestinal fluid (SIF), were investigated for 400 h through bulk erosion. Consequently, a slower rate of drug loading and release was observed for native hydrogel, due to stronger H-bonding, interlocking and entanglement within the IPNs, which was finely tuned and extended by the induced hydrophilic and functional ligands. In the light of induced hydrophilicity, such functional hydrogel could be highly attractive for extended release of sparingly soluble drugs.
    Matched MeSH terms: Drug Liberation
  5. Senjoti FG, Mahmood S, Jaffri JM, Mandal UK
    Iran J Pharm Res, 2016;15(1):53-70.
    PMID: 27610147
    An oral sustained-release floating tablet formulation of metformin HCl was designed and developed. Effervescence and swelling properties were attributed on the developed tablets by sodium bicarbonate and HPMC-PEO polymer combination, respectively. Tablet composition was optimized by response surface methodology (RSM). Seventeen (17) trial formulations were analyzed according to Box-Behnken design of experiment where polymer content of HPMC and PEO at 1: 4 ratio (A), amount of sodium bi-carbonate (B), and amount of SSG (C) were adopted as independent variables. Floating lag time in sec (Y1), cumulative percent drug released at 1 h (Y2) and 12 h (Y3) were chosen as response variables. Tablets from the optimized formulation were also stored at accelerated stability condition (40°C and 75% RH) for 3 months to assess their stability profile. RSM could efficiently optimize the tablet composition with excellent prediction ability. In-vitro drug release until 12 h, floating lag time, and duration of floating were dependent on the amount of three selected independent variables. Optimized tablets remained floating for more than 24 h with a floating lag time of less than 4 min. Based on best fitting method, optimized formulation was found to follow Korsmeyer-Peppas release kinetic. Accelerated stability study revealed that optimized formulation was stable for three months without any major changes in assay, dissolution profile, floating lag time and other physical properties.
    Matched MeSH terms: Drug Liberation
  6. Ashrafizadeh M, Delfi M, Zarrabi A, Bigham A, Sharifi E, Rabiee N, et al.
    J Control Release, 2022 Nov;351:50-80.
    PMID: 35934254 DOI: 10.1016/j.jconrel.2022.08.001
    The site-specific delivery of antitumor agents is of importance for providing effective cancer suppression. Poor bioavailability of anticancer compounds and the presence of biological barriers prevent their accumulation in tumor sites. These obstacles can be overcome using liposomal nanostructures. The challenges in cancer chemotherapy and stimuli-responsive nanocarriers are first described in the current review. Then, stimuli-responsive liposomes including pH-, redox-, enzyme-, light-, thermo- and magneto-sensitive nanoparticles are discussed and their potential for delivery of anticancer drugs is emphasized. The pH- or redox-sensitive liposomes are based on internal stimulus and release drug in response to a mildly acidic pH and GSH, respectively. The pH-sensitive liposomes can mediate endosomal escape via proton sponge. The multifunctional liposomes responsive to both redox and pH have more capacity in drug release at tumor site compared to pH- or redox-sensitive alone. The magnetic field and NIR irradiation can be exploited for external stimulation of liposomes. The light-responsive liposomes release drugs when they are exposed to irradiation; thermosensitive-liposomes release drugs at a temperature of >40 °C when there is hyperthermia; magneto-responsive liposomes release drugs in presence of magnetic field. These smart nanoliposomes also mediate co-delivery of drugs and genes in synergistic cancer therapy. Due to lack of long-term toxicity of liposomes, they can be utilized in near future for treatment of cancer patients.
    Matched MeSH terms: Drug Liberation
  7. Faisalina AF, Sonvico F, Colombo P, Amirul AA, Wahab HA, Majid MIA
    Nanomaterials (Basel), 2020 Oct 26;10(11).
    PMID: 33114572 DOI: 10.3390/nano10112123
    Polyhydroxyalkanoate (PHA) copolymers show a relatively higher in vivo degradation rate compared to other PHAs, thus, they receive a great deal of attention for a wide range of medical applications. Nanoparticles (NPs) loaded with poorly water-soluble anticancer drug docetaxel (DCX) were produced using poly(3-hydroxybutyrate-co-4-hydroxybutyrate), P(3HB-co-4HB), copolymers biosynthesised from Cupriavidus malaysiensis USMAA1020 isolated from the Malaysian environment. Three copolymers with different molar proportions of 4-hydroxybutirate (4HB) were used: 16% (PHB16), 30% (PHB30) and 70% (PHB70) 4HB-containing P(3HB-co-4HB). Blank and DCX-loaded nanoparticles were then characterized for their size and size distribution, surface charge, encapsulation efficiency and drug release. Preformulation studies showed that an optimised formulation could be achieved through the emulsification/solvent evaporation method using PHB70 with the addition of 1.0% PVA, as stabilizer and 0.03% VitE-TPGS, as surfactant. DCX-loaded PHB70 nanoparticles (DCX-PHB70) gave the desired particle size distribution in terms of average particle size around 150 nm and narrow particle size distribution (polydispersity index (PDI) below 0.100). The encapsulation efficiency result showed that at 30% w/w drug-to-polymer ratio: DCX- PHB16 NPs were able to encapsulate up to 42% of DCX; DCX-PHB30 NPs encapsulated up to 46% of DCX and DCX-PHB70 NPs encapsulated up to 50% of DCX within the nanoparticle system. Approximately 60% of DCX was released from the DCX-PHB70 NPs within 7 days for 5%, 10% and 20% of drug-to-polymer ratio while for the 30% and 40% drug-to-polymer ratios, an almost complete drug release (98%) after 7 days of incubation was observed.
    Matched MeSH terms: Drug Liberation
  8. Bera H, Kumar S, Maiti S
    Int J Biol Macromol, 2018 Oct 15;118(Pt A):149-159.
    PMID: 29932998 DOI: 10.1016/j.ijbiomac.2018.06.085
    Olive oil-entrapped diethanolamine-modified high-methoxyl pectin (DMP)-gellan gum (GG)-bionanofiller composites were developed for controlled intragastric delivery of metformin HCl (MFM). DMP had a degree of amidation of 48.7% and was characterized further by FTIR, XRD and DSC analyses. MFM-loaded composites were subsequently accomplished by green synthesis via ionotropic gelation technique using zinc acetate as cross-linker. The thermal, X-ray and infrared analyses suggested an environment in the composites compatible with the drug, except certain degree of attenuation in drug's crystallinity. Scanning electron microscopy revealed almost spherical shape of the composites. Depending upon the mass ratios of GG:DMP, types of nanofiller (neusilin/bentonite/Florite) and oil inclusion, the composites exhibited variable drug encapsulation efficiency (DEE, 50-85%) and extended drug release behaviours (Q8h, 69-94%) in acetate buffer (pH 4.5). The optimized oil-entrapped Florite R NF/GG: DMP (1:1) composites eluted MFM via case-II transport mechanism and its drug release data was best fitted in zero-order kinetic model. The optimized formulation demonstrated excellent gastroretentive properties and substantial hypoglycemic effect in streptozotocin-induced diabetic rats. These novel hybrid matrices were thus found suitable for controlled intragastric delivery of MFM for the management of type 2 diabetes.
    Matched MeSH terms: Drug Liberation
  9. Ayub AD, Chiu HI, Mat Yusuf SNA, Abd Kadir E, Ngalim SH, Lim V
    Artif Cells Nanomed Biotechnol, 2019 Dec;47(1):353-369.
    PMID: 30691309 DOI: 10.1080/21691401.2018.1557672
    The application of layer-by-layer (LbL) approach on nanoparticle surface coating improves the colon-specific drug delivery of insoluble drugs. Here, we aimed to formulate a self-assembled cysteamine-based disulphide cross-linked sodium alginate with LbL self-assembly to improve the delivery of paclitaxel (PCX) to colonic cancer cells. Cysteamine was conjugated to the backbone of oxidized SA to form a core of self-assembled disulphide cross-linked nanospheres. P3DL was selected for PCX loading and fabricated LbL with poly(allylamine hydrochloride) (PAH) and poly(4-styrenesulfonic acid-co-maleic acid) sodium salt (PSSCMA) resulting from characterization and drug release studies. P3DL-fabricated PCX-loaded nanospheres (P3DL/PAH/PSSCMA) exhibited an encapsulation efficiency of 77.1% with cumulative drug release of 45.1%. Dynamic light scattering analysis was reported at 173.6 ± 2.5 nm with polydispersity index of 0.394 ± 0.105 (zeta potential= -58.5 mV). P3DL/PAH/PSSCMA demonstrated a pH-dependent swelling transition; from pH 1 to 7 (102.2% increase). The size increased by 33.0% in reduction response study after incubating with 10 mM glutathione (day 7). HT-29 cells showed high viabilities (86.7%) after treatment with the fabricated nanospheres at 0.8 µg/mL. Cellular internalization was successful with more than 70.0% nanospheres detected in HT-29 cells. Therefore, this fabricated nanospheres may be considered as potential nanocarriers for colon cancer-targeted chemotherapeutic drug delivery.
    Matched MeSH terms: Drug Liberation
  10. Amin, M.C.I., Soom, R.M., Ahmad, I., Lian, H.H.
    MyJurnal
    This study was carried out to determine the physicochemical properties of carboxymethyl cellulose (CMC) derived from cellulose of palm oil empty fruit bunch (EFB) and its use asa film-coating agent. Samples were prepared at various concentrations and then their physicochemical properties were studied including the viscosity, pH, tensile strength of films, surface properties of the films and dissolution studies on coated tablets. CMC EFB showed lower viscosity than commercial CMC product at the concentration of 1%, 2% and 3% with the values of 44.0cp, 299.9cp, 358.9cp and 90.0cp, 689.9cp, 5569.0cp respectively. The tensile strength of the films for CMC EFB were 7.85MPa, 14.79MPa, 10.36MPa while the commercial CMC exhibited higher values of 21.72MPa, 35.14MPa and 26.9MPa at similar concentration. The scanning electron microscope showed different surface properties of the films for both of them where the commercial CMC is smoother in texture and very transparent unlike its counterpart. However, dissolution studies on paracetamol tablets coated using the samples showed no significant difference (p>0.05) in drug release profile between the two materials. Hence, CMC EFB has a greater potential to be developed as a competitive tablet-coating agent despite the differences in its physicochemical properties.
    Matched MeSH terms: Drug Liberation
  11. Ng SF, Leow HL
    Drug Dev Ind Pharm, 2015;41(11):1902-9.
    PMID: 25758412 DOI: 10.3109/03639045.2015.1019888
    It has been established that microbial biofilms are largely responsible for the recalcitrance of many wound infections to conventional antibiotics. It was proposed that the efficacy of antibiotics could be optimized via the inhibition of bacterial biofilm growth in wounds. The combination of antibiofilm agent and antibiotics into a wound dressing may be a plausible strategy in wound infection management. Xylitol is an antibiofilm agent that has been shown to inhibit the biofilm formation. The purpose of this study was to develop an alginate film containing xylitol and gentamicin for the treatment of wound infection. Three films, i.e. blank alginate film (SA), alginate film with xylitol (F5) and alginate film with xylitol and gentamicin (AG), were prepared. The films were studied for their physical properties, swelling ratio, moisture absorption, moisture vapor transmission rate (MVTR), mechanical and rheology properties, drug content uniformity as well as in vitro drug release properties. Antimicrobial and antibiofilm in vitro studies on Staphylococcus aureus and Pseudomonas aeruginosa were also performed. The results showed that AG demonstrates superior mechanical properties, rheological properties and a higher MVTR compared with SA and F5. The drug flux of AG was higher than that of commercial gentamicin cream. Furthermore, antimicrobial studies showed that AG is effective against both S. aureus and P. aeruginosa, and the antibiofilm assays demonstrated that the combination was effective against biofilm bacteria. In summary, alginate films containing xylitol and gentamicin may potentially be used as new dressings for the treatment of wound infection.
    Matched MeSH terms: Drug Liberation
  12. Setyawati MI, Kutty RV, Leong DT
    Small, 2016 Oct;12(40):5601-5611.
    PMID: 27571230 DOI: 10.1002/smll.201601669
    Targeted drug delivery is one of the key challenges in cancer nanomedicine. Stoichiometric and spatial control over the antibodies placement on the nanomedicine vehicle holds a pivotal role to overcome this key challenge. Here, a DNA tetrahedral is designed with available conjugation sites on its vertices, allowing to bind one, two, or three cetuximab antibodies per DNA nanostructure. This stoichiometrically definable cetuximab conjugated DNA nanostructure shows enhanced targeting on the breast cancer cells, which results with higher overall killing efficacy of the cancer cells.
    Matched MeSH terms: Drug Liberation
  13. Nair RS, Morris A, Billa N, Leong CO
    AAPS PharmSciTech, 2019 Jan 10;20(2):69.
    PMID: 30631984 DOI: 10.1208/s12249-018-1279-6
    Curcumin-loaded chitosan nanoparticles were synthesised and evaluated in vitro for enhanced transdermal delivery. Zetasizer® characterisation of three different formulations of curcumin nanoparticles (Cu-NPs) showed the size ranged from 167.3 ± 3.8 nm to 251.5 ± 5.8 nm, the polydispersity index (PDI) values were between 0.26 and 0.46 and the zeta potential values were positive (+ 18.1 to + 20.2 mV). Scanning electron microscopy (SEM) images supported this size data and confirmed the spherical shape of the nanoparticles. All the formulations showed excellent entrapment efficiency above 80%. FTIR results demonstrate the interaction between chitosan and sodium tripolyphosphate (TPP) and confirm the presence of curcumin in the nanoparticle. Differential scanning calorimetry (DSC) studies of Cu-NPs indicate the presence of curcumin in a disordered crystalline or amorphous state, suggesting the interaction between the drug and the polymer. Drug release studies showed an improved drug release at pH 5.0 than in pH 7.4 and followed a zero order kinetics. The in vitro permeation studies through Strat-M® membrane demonstrated an enhanced permeation of Cu-NPs compared to aqueous curcumin solution (p ˂ 0.05) having a flux of 0.54 ± 0.03 μg cm-2 h-1 and 0.44 ± 0.03 μg cm-2 h-1 corresponding to formulations 5:1 and 3:1, respectively. The cytotoxicity assay on human keratinocyte (HaCat) cells showed enhanced percentage cell viability of Cu-NPs compared to curcumin solution. Cu-NPs developed in this study exhibit superior drug release and enhanced transdermal permeation of curcumin and superior percentage cell viability. Further ex vivo and in vivo evaluations will be conducted to support these findings.
    Matched MeSH terms: Drug Liberation
  14. Rozman NAS, Tong WY, Leong CR, Anuar MR, Karim S, Ong SK, et al.
    Sci Rep, 2020 02 24;10(1):3307.
    PMID: 32094395 DOI: 10.1038/s41598-020-60364-0
    Essential oil of Homalomena pineodora inhibits diabetic pathogens; however, the activity was not sustainable when applied as wound dressing. This study aims to synthesise the essential oil nanoparticle using chitosan. The nanoparticles were synthesised with ion gelation method, confirmed by spectroscopic analysis. The spherical nanoparticles display a size of 70 nm, with strong surface charge of +24.10 mV. The nanoparticles showed an initial burst release followed by a slow release pattern for 72 h, following the first order of kinetic. The release behaviour was ideal for wound dressing. The antimicrobial activity was broad spectrum. The formation of nanoparticle enhanced the antimicrobial efficacy of the essential oil. The nanoparticle also showed a concentration-dependent killing behaviour on time-kill assay. In the 3D collagen wound models, the nanoparticles reduced the microbial growth by 60-80%. In conclusion, H. pineodora nanoparticles showed pharmaceutical potential in inhibiting microbial growth on diabetic ulcers.
    Matched MeSH terms: Drug Liberation
  15. Kuche K, Maheshwari R, Tambe V, Mak KK, Jogi H, Raval N, et al.
    Nanoscale, 2018 May 17;10(19):8911-8937.
    PMID: 29722421 DOI: 10.1039/c8nr01383g
    The search for effective and non-invasive delivery modules to transport therapeutic molecules across skin has led to the discovery of a number of nanocarriers (viz.: liposomes, ethosomes, dendrimers, etc.) in the last few decades. However, available literature suggests that these delivery modules face several issues including poor stability, low encapsulation efficiency, and scale-up hurdles. Recently, carbon nanotubes (CNTs) emerged as a versatile tool to deliver therapeutics across skin. Superior stability, high loading capacity, well-developed synthesis protocol as well as ease of scale-up are some of the reason for growing interest in CNTs. CNTs have a unique physical architecture and a large surface area with unique surface chemistry that can be tailored for vivid biomedical applications. CNTs have been thus largely engaged in the development of transdermal systems such as tuneable hydrogels, programmable nonporous membranes, electroresponsive skin modalities, protein channel mimetic platforms, reverse iontophoresis, microneedles, and dermal buckypapers. In addition, CNTs were also employed in the development of RNA interference (RNAi) based therapeutics for correcting defective dermal genes. This review expounds the state-of-art synthesis methodologies, skin penetration mechanism, drug liberation profile, loading potential, characterization techniques, and transdermal applications along with a summary on patent/regulatory status and future scope of CNT based skin therapeutics.
    Matched MeSH terms: Drug Liberation
  16. Samrot AV, Kudaiyappan T, Bisyarah U, Mirarmandi A, Faradjeva E, Abubakar A, et al.
    Int J Nanomedicine, 2020;15:7097-7115.
    PMID: 33061370 DOI: 10.2147/IJN.S259653
    Background: Plant gums consist of polysaccharides which can be used in the preparation of nanocarriers and provide a wide application in pharmaceutical applications including as drug delivery agents and the matrices for drug release. The objectives of the study were to collect plant gums from Araucaria heterophylla L and Prosopis chilensis L and to extract and characterize their polysaccharides. Then to utilize these plant gum-derived polysaccharides for the formulation of nanocarriers to use for drug loading and to examine their purpose in drug delivery in vitro.

    Methods: Plant gum was collected, polysaccharide was extracted, purified, characterized using UV-Vis, FTIR, TGA and GCMS and subjected to various bioactive studies. The purified polysaccharide was used for making curcumin-loaded nanocarriers using STMP (sodium trimetaphosphate). Bioactivities were performed on the crude, purified and drug-loaded nanocarriers. These polysaccharide-based nanocarriers were characterized using UV-Vis spectrophotometer, FTIR, SEM, and AFM. Drug release kinetics were performed for the drug-loaded nanocarriers.

    Results: The presence of glucose, xylose and sucrose was studied from the UV-Vis and GCMS analysis. Purified polysaccharides of both the plants showed antioxidant activity and also antibacterial activity against Bacillus sp. Purified polysaccharides were used for nanocarrier synthesis, where the size and shape of the nanocarriers were studied using SEM analysis and AFM analysis. The size of the drug-loaded nanocarriers was found to be around 200 nm. The curcumin-loaded nanocarriers were releasing curcumin slow and steady.

    Conclusion: The extracted pure polysaccharide of A. heterophylla and P. chilensis acted as good antioxidants and showed antibacterial activity against Bacillus sp. These polysaccharides were fabricated into curcumin-loaded nanocarriers whose size was below 200 nm. Both the drug-loaded nanocarriers synthesized using A. heterophylla and P. chilensis showed antibacterial activity with a steady drug release profile. Hence, these natural exudates can serve as biodegradable nanocarriers in drug delivery.

    Matched MeSH terms: Drug Liberation
  17. Bera H, Kumar S
    Int J Biol Macromol, 2018 Mar;108:1053-1062.
    PMID: 29122714 DOI: 10.1016/j.ijbiomac.2017.11.019
    The current study aimed at developing diethonolamine-modified high-methoxyl pectin (DMP)-alginate (ALG) based core-shell composites for controlled intragastric delivery of metformin HCl (MFM) by combined approach of floating and bioadhesion. DMP with degree of amidation of 48.72% was initially accomplished and characterized by FTIR, DSC and XRD analyses. MFM-loaded core matrices were then fabricated by ionotropic gelation technique employing zinc acetate as cross-linker. The core matrices were further coated by fenugreek gum (FG)-ALG gel membrane via diffusion-controlled interfacial complexation method. Various formulations demonstrated excellent drug encapsulation efficiency (DEE, 51-70%) and sustained drug eluting behavior (Q8h, 72-96%), which were extremely influenced by polymer-blend (ALG:DMP) ratios, low density additives (olive oil/magnesium stearate) and FG-ALG coating inclusion. The drug release profile of the core-shell matrices (F-7) was best fitted in zero-order kinetic model with case-II transport driven mechanism. It also portrayed outstanding gastroretentive characteristics. Moreover, the composites were analyzed for surface morphology, drug-excipients compatibility, thermal behavior and drug crystallinity. Thus, the developed composites are appropriate for controlled stomach-specific delivery of MFM for type 2 diabetes management.
    Matched MeSH terms: Drug Liberation
  18. Malviya R, Raj S, Fuloria S, Subramaniyan V, Sathasivam K, Kumari U, et al.
    Int J Nanomedicine, 2021;16:2533-2553.
    PMID: 33824590 DOI: 10.2147/IJN.S300991
    PURPOSE: The present study was intended to fabricate chitosan (Ch)-tamarind gum polysaccharide (TGP) polyelectrolyte complex stabilized cubic nanoparticles of simvastatin and evaluate their potential against human breast cancer cell lines.

    MATERIALS AND METHODS: The antisolvent precipitation method was used for formulation of nanoparticles. Factorial design (32) was utilized as a tool to analyze the effect of Ch and TGP concentration on particle size and entrapment efficiency of nanoparticles.

    RESULTS: Formulated nanoparticles showed high entrapment efficiency (67.19±0.42-83.36±0.23%) and small size (53.3-383.1 nm). The present investigation involved utilization of two biological membranes (egg and tomato) as biological barriers for drug release. The study revealed that drug release from tomato membranes was retarded (as compared to egg membranes) but the release pattern matched that of egg membranes. All formulations followed the Baker-Lansdale model of drug release irrespective of the two different biological barriers. Stability studies were carried out for 45 days and exhibited less variation in particle size as well as a reduction in entrapment efficiency. Simvastatin loaded PEC stabilized nanoparticles exhibited better control on growth of human breast cancer cell lines than simple simvastatin. An unusual anticancer effect of simvastatin nanoparticles is also supported by several other research studies.

    CONCLUSION: The present study involves first-time synthesis of Ch-TGP polyelectrolyte complex stabilized nanoparticles of simvastatin against MCF-7 cells. It recommends that, in future, theoretical modeling and IVIVC should be carried out for perfect designing of delivery systems.

    Matched MeSH terms: Drug Liberation
  19. Shah SA, Sohail M, Minhas MU, Nisar-Ur-Rehman, Khan S, Hussain Z, et al.
    Drug Deliv Transl Res, 2019 Apr;9(2):555-577.
    PMID: 29450805 DOI: 10.1007/s13346-018-0486-8
    Cellulose acetate phthalate-based pH-responsive hydrogel was synthesized for fabrication of polymeric matrix tablets for gastro-protective delivery of loxoprofen sodium. Cellulose acetate phthalate (CAP) was cross-linked with methacrylic acid (MAA) using free radical polymerization technique. Fourier transform infrared (FTIR) spectra confirmed the formation of cross-linked structure of CAP-co-poly(methacrylic acid). Thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC) confirmed the thermal stability of polymeric networks, and scanning electron microscopy (SEM) and energy-dispersive X-ray spectrum (EDS) images unveiled that the prepared formulations were porous in nature and thus the developed formulations had shown better diffusibility. Swelling and in vitro drug release was performed at various pHs and maximum swelling and release was obtained at pH 7.4, while swelling and release rate was very low at pH 1.2 which confirmed the pH-responsive behavior of CAP-co-poly(MAA). CAP-co-poly(MAA) copolymer prevents the release of loxoprofen sodium into the stomach due to reduced swelling at gastric pH while showing significant swelling and drug release in the colon. Cytotoxicity studies revealed higher biocompatibility of fabricated hydrogel. Acute oral toxicity studies were performed for the evaluation and preliminary screening of safety profile of the developed hydrogels. Matrix tablets were evaluated for release behavior at simulated body pH. The investigations performed for analysis of hydrogels and fabricated matrix tablets indicated the controlled drug release and gastro-protective drug delivery of CAP-co-poly(MAA) hydrogels and pH-sensitive matrix tablets for targeted delivery of gastro-sensitive/irritative agents. Graphical abstract.
    Matched MeSH terms: Drug Liberation
  20. Ali HS, Khan S, York P, Shah SM, Khan J, Hussain Z, et al.
    Pak J Pharm Sci, 2017 Sep;30(5):1635-1643.
    PMID: 29084684
    Drug nanosuspensions have gained tremendous attraction as a platform in drug delivery. In the present work, a nanosuspension was prepared by a wet milling approach in order to increase saturation solubility and dissolution of the water insoluble drug, hydrocortisone. Size of the generated particeles was 290 nm ± 9 nm having a zeta potential of -1.9 mV ± 0.6 mV. Nanosized particles were found to have a rod shape with a narrow particle size distribution (PDI =0.17). Results of differential scanning calorimetry and X-ray diffraction analyses revealed minor modifications of crystallinity of hydrocortisone following the milling process. Solubility of hydrocortisone was enhanced by nanonization to 875µg/ml ±2.5, an almost 2.9-fold compared to the raw hydrocortisone. Moreover, the nanosuspension formulation substabtially enhanced the dissolution rate of hydrocortisone where >97% of the hydrocortisone was dissolved within 10 minutes opposed to 22.3% for the raw 50% for the raw hydrocortisone and the commercial tablet, respectively. The bioavailability study resulted in AUC 0-9h for HC nanosuspensions (31.50±2.50), which is significantly (p<0.05) higher compared to the AUC 0-9h (14.85±3.25) resulted for HC solution. The nanosuspension was physically stable at room temperature for 24 months.
    Matched MeSH terms: Drug Liberation
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