Displaying publications 1 - 20 of 199 in total

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  1. Sabbagh HAK, Hussein-Al-Ali SH, Hussein MZ, Abudayeh Z, Ayoub R, Abudoleh SM
    Polymers (Basel), 2020 Apr 01;12(4).
    PMID: 32244671 DOI: 10.3390/polym12040772
    The goal of this study was to develop and statistically optimize the metronidazole (MET), chitosan (CS) and alginate (Alg) nanoparticles (NP) nanocomposites (MET-CS-AlgNPs) using a (21 × 31 × 21) × 3 = 36 full factorial design (FFD) to investigate the effect of chitosan and alginate polymer concentrations and calcium chloride (CaCl2) concentration ondrug loading efficiency(LE), particle size and zeta potential. The concentration of CS, Alg and CaCl2 were taken as independent variables, while drug loading, particle size and zeta potential were taken as dependent variables. The study showed that the loading efficiency and particle size depend on the CS, Alg and CaCl2 concentrations, whereas zeta potential depends only on the Alg and CaCl2 concentrations. The MET-CS-AlgNPs nanocomposites were characterized by X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), thermal gravimetric analysis (TGA), scanning electron microscopy (SEM) and in vitro drug release studies. XRD datashowed that the crystalline properties of MET changed to an amorphous-like pattern when the nanocomposites were formed.The XRD pattern of MET-CS-AlgNPs showed reflections at 2θ = 14.2° and 22.1°, indicating that the formation of the nanocompositesprepared at the optimum conditions havea mean diameter of (165±20) nm, with a MET loading of (46.0 ± 2.1)% and a zeta potential of (-9.2 ± 0.5) mV.The FTIR data of MET-CS-AlgNPs showed some bands of MET, such as 3283, 1585 and 1413 cm-1, confirming the presence of the drug in the MET-CS-AlgNPs nanocomposites. The TGA for the optimized sample of MET-CS-AlgNPs showed a 70.2% weight loss compared to 55.3% for CS-AlgNPs, and the difference is due to the incorporation of MET in the CS-AlgNPs for the formation of MET-CS-AlgNPs nanocomposites. The release of MET from the nanocomposite showed sustained-release properties, indicating the presence of an interaction between MET and the polymer. The nanocomposite shows a smooth surface and spherical shape. The release profile of MET from its MET-CS-AlgNPs nanocomposites was found to be governed by the second kinetic model (R2 between 0.956-0.990) with more than 90% release during the first 50 h, which suggests that the release of the MET drug can be extended or prolonged via the nanocomposite formulation.
    Matched MeSH terms: Drug Liberation
  2. Dabbagh A, Abdullah BJ, Abu Kasim NH, Abdullah H, Hamdi M
    Int J Hyperthermia, 2015 Jun;31(4):375-85.
    PMID: 25716769 DOI: 10.3109/02656736.2015.1006268
    The aim of this paper was to introduce a new mechanism of thermal sensitivity in nanocarriers that results in a relatively low drug release at physiological temperature and rapid release of the encapsulated drug at hyperthermia and thermal ablation temperature range (40-60 °C).
    Matched MeSH terms: Drug Liberation*
  3. Irfan SA, Razali R, KuShaari K, Mansor N, Azeem B, Ford Versypt AN
    J Control Release, 2018 02 10;271:45-54.
    PMID: 29274697 DOI: 10.1016/j.jconrel.2017.12.017
    Nutrients released into soils from uncoated fertilizer granules are lost continuously due to volatilization, leaching, denitrification, and surface run-off. These issues have caused economic loss due to low nutrient absorption efficiency and environmental pollution due to hazardous emissions and water eutrophication. Controlled-release fertilizers (CRFs) can change the release kinetics of the fertilizer nutrients through an abatement strategy to offset these issues by providing the fertilizer content in synchrony with the metabolic needs of the plants. Parametric analysis of release characteristics of CRFs is of paramount importance for the design and development of new CRFs. However, the experimental approaches are not only time consuming, but they are also cumbersome and expensive. Scientists have introduced mathematical modeling techniques to predict the release of nutrients from the CRFs to elucidate fundamental understanding of the dynamics of the release processes and to design new CRFs in a shorter time and with relatively lower cost. This paper reviews and critically analyzes the latest developments in the mathematical modeling and simulation techniques that have been reported for the characteristics and mechanisms of nutrient release from CRFs. The scope of this review includes the modeling and simulations techniques used for coated, controlled-release fertilizers.
    Matched MeSH terms: Drug Liberation*
  4. 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
  5. Rida Tajau, Siti Farhana Fathy, Mek Zah Salleh, Nor Azowa Ibrahim, Maznah Ismail, Kamaruddin Hashim
    MyJurnal
    The acrylated palm oil (APO) nanoparticle is a potential product that can be used as carriers in
    medical field. The main focus of the present study was to study the potential of the APO
    nanoparticles for used in a controlled drug delivery system. The microemulsion system is used as a
    medium to incorporate an active substance such as Thymoquinone (TQ) into the APO polymeric
    micelle and then the radiation technique is used as a tool for the synthesis of TQ-loaded APO
    nanoparticle. The nano-size TQ-loaded APO particles resulted the particle size of less than 150 nm
    with spherical in shape. The TQ release profile was carried out in potassium buffer saline (PBS)
    solutions (pH 7.4) at 37
    oC. And, the zero-order model has been used to determine the mechanism
    of the drug release from the corresponding nanoparticles, respectively. The TQ release was found
    to be sustained and controlled in pH 7.4. At pH 7.4, the release of TQ followed the zero-order
    model. The in-vitro drug release study showed a good prospect of the APO nanoparticle on being a
    potential drug carrier as there are toxic against colon cancer cells and not toxic towards normal
    cells. This suggested that the APO product produce using this radiation technique can be
    developed into different type of carrier systems for controlled drug release applications.
    Matched MeSH terms: Drug Liberation
  6. 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
  7. Hasnain MS, Nayak AK, Singh M, Tabish M, Ansari MT, Ara TJ
    Int J Biol Macromol, 2016 Feb;83:71-7.
    PMID: 26608007 DOI: 10.1016/j.ijbiomac.2015.11.044
    Alginate-based bipolymeric-nanobioceramic composite matrices for sustained drug release were developed through incorporation of nano-hydroxyapatite [nHAp] powders within ionotropically-gelled calcium ion-induced alginate-poly (vinyl pyrrolidone) blends polymeric systems. nHAp powders were synthesized by precipitation technique using calcium hydroxide [Ca(OH)2] and orthophosphoric acid [H3PO4] as raw materials. The average particle size of these was synthesized. nHAp powders was found as 19.04 nm and used to prepare nHAp-alginate-PVP beads containing DS. These beads exhibited drug entrapment efficiency (%) of 65.82±1.88 to 94.45±3.72% and average bead sizes of 0.98±0.07 to 1.23±0.15 mm. These beads were characterized by scanning electron microscopy (SEM) and Fourier transform-infra red (FTIR) spectroscopy analyses. Various nHAp-alginate-PVP beads containing DS exhibited prolonged sustained drug release and followed the Koresmeyer-Peppas model of drug release (R2=0.9908-0.9978) with non-Fickian release (anomalous transport) mechanism (n=0.73-0.84) for drug release over 8 h.
    Matched MeSH terms: Drug Liberation/drug effects
  8. 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
  9. Kumar GP, Sanganal JS, Phani AR, Manohara C, Tripathi SM, Raghavendra HL, et al.
    Pharmacol Res, 2015 Oct;100:47-57.
    PMID: 26232590 DOI: 10.1016/j.phrs.2015.07.025
    6-Mercaptopurine is a cytotoxic and immunosuppressant drug. The use of this drug is limited due to its poor bioavailability and short plasma half-life. In order to nullify these drawbacks, 6-mercaptopurine-chitosan nanoparticles (6-MP-CNPs) were prepared and evaluated to study the influence of preparation conditions on the physicochemical properties by using DLS, SEM, XRD and FTIR. The in vitro drug release profile at pH 4.8 and 7.4 revealed sustained release patterns for a period of 2 days. The nanoformulations showed enhanced in vitro anti-cancer activities (MTT assay, apoptosis assay, cell cycle arrest and ROS indices) on HT-1080 and MCF-7 cells. In vivo pharmacokinetics profiles of 6-MP-CNPs showed improved bioavailability. Thus, the results of the present study revealed that, the prepared 6-MP-CNPs have a significant role in increasing anti-cancer efficacy, bioavailability and in vivo pharmacokinetics profiles.
    Matched MeSH terms: Drug Liberation
  10. Abrami M, Golob S, Pontelli F, Chiarappa G, Grassi G, Perissutti B, et al.
    Int J Pharm, 2019 Mar 25;559:373-381.
    PMID: 30716402 DOI: 10.1016/j.ijpharm.2019.01.055
    Bacterial infections represent an important drawback in the orthopaedic field, as they can develop either immediately after surgery procedures or after some years. Specifically, in case of implants, they are alleged to be troublesome as their elimination often compels a surgical removal of the infected implant. A possible solution strategy could involve a local coating of the implant by an antibacterial system, which requires to be easily applicable, biocompatible and able to provide the desired release kinetics for the selected antibacterial drug. Thus, this work focusses on a biphasic system made up by a thermo-reversible gel matrix (Poloxamer 407/water system) hosting a dispersed phase (PLGA micro-particles), containing a model antibacterial drug (vancomycin hydrochloride). In order to understand the key parameters ruling the performance of this delivery system, we developed a mathematical model able to discriminate the drug diffusion inside micro-particles and within the gel phase, eventually providing to predict the drug release kinetics. The model reliability was confirmed by fitting to experimental data, proposing as a powerful theoretical approach to design and optimize such in situ delivery systems.
    Matched MeSH terms: Drug Liberation/drug effects
  11. Nor Hazliana Harun, Rabiatul Basria S.M.N. Mydin, Khairul Anuar Shariff, Nur Adila Rosdi, Davamunisvari Rames
    MyJurnal
    Introduction: This study aims to investigate different residue sizes of β-tricalcium phosphate (β-TCP) micro-granules as carriers to assess antibacterial activity and drug-control release behavior of ampicillin (AMP-) and antimycotic (AMC-). Incorporation of antibiotic into the β-TCP micro-granules and it sustain release behavior could be used as alternative solution to reduce the risk of osteomyelitis and bone infections risks. Methods: Three different residue sizes (less than 300 µm, 300 µm and 600 µm) were prepared and coated with antibiotics solution (20 µg/µl of ampi- cillin and 100X antimycotic solution) by using two methods; dip and stream coating. After 72 h, 1.5 mL of distilled water was added to the treated (β-TCP) micro-granules at two different pH value (5.0 and 7.4). The extracted solution was further analyzed by Kirby Bauer disc diffusion test and spectrophotometer assay. Results: The solution con- taining AMC-(β-TCP) micro-granules with the size of 300 µm residue produced the largest inhibition zones against Escherichia coli (E. coli). All residue sizes coated with AMP- showed no antibacterial activity against both strains; Staphylococcus aureus (S. aureus) and E.coli. Additionally, the release behavior of AMC-(β-TCP) micro-granules was found not depending on the pH, but on the size of residue. Complete drug release was rapidly observed within 48
    h. Conclusion: Based on this findings, it showed AMC-(β-TCP) micro-granules had an antibacterial activity against Gram-negative strain. Specifically, it can reduced the growth rate of E. coli and the rapid release behavior of AMC- (β-TCP) micro-granules help in minimizing the risk-infections in early stage of implantation.
    Matched MeSH terms: Drug Liberation
  12. Mohd Cairul Iqbal Mohd Amin, Abadi Gumah Abadi, Naveed Ahmad, Haliza Katas, Jamia Azdina Jamal
    Sains Malaysiana, 2012;41:561-568.
    There has been an increasing interest in the use of natural materials as drug delivery vehicles due to their biodegradability, biocompatibility and ready availability. These properties make bacterial cellulose (BC), from nata de coco, a promising biopolymer for drug delivery applications. The aim of this study was to investigate the film-coating and drug release properties of this biopolymer. Physicochemical, morphological and thermal properties of BC films were studied. Model tablets were film coated with BC, using a spray coating technique, and in vitro drug release studies of these tablets were investigated. It was found that BC exhibited excellent ability to form soft, flexible and foldable films without the addition
    of any plasticizer. They were comparable to Aquacoat ECD (with plasticizer) in tensile strength, percentage elongation and elasticity modulus. Differential scanning calorimetry (DSC) BC showed a high Tg value indicating thermally stability of films. These results suggest that BC can be used as novel aqueous film-coating agent with lower cost and better film forming properties than existing film-coating agents.
    Matched MeSH terms: Drug Liberation
  13. Sahibzada MUK, Sadiq A, Faidah HS, Khurram M, Amin MU, Haseeb A, et al.
    Drug Des Devel Ther, 2018;12:303-312.
    PMID: 29491706 DOI: 10.2147/DDDT.S156123
    BACKGROUND: Berberine is an isoquinoline alkaloid widely used in Ayurveda and traditional Chinese medicine to treat illnesses such as hypertension and inflammatory conditions, and as an anticancer and hepato-protective agent. Berberine has low oral bioavailability due to poor aqueous solubility and insufficient dissolution rate, which can reduce the efficacy of drugs taken orally. In this study, evaporative precipitation of nanosuspension (EPN) and anti-solvent precipitation with a syringe pump (APSP) were used to address the problems of solubility, dissolution rate and bioavailability of berberine.

    METHODS: Semi-crystalline nanoparticles (NPs) of 90-110 nm diameter for APSP and 65-75 nm diameter for EPN were prepared and then characterized using differential scanning calorimetry (DSC) and X-ray powder diffractometry (XRD). Thereafter, drug content solubility and dissolution studies were undertaken. Berberine and its NPs were evaluated for their antibacterial activity.

    RESULTS: The results indicate that the NPs have significantly increased solubility and dissolution rate due to conversion of the crystalline structure to a semi-crystalline form.

    CONCLUSION: Berberine NPs produced by both APSP and EPN methods have shown promising activities against Gram-positive and Gram-negative bacteria, and yeasts, with NPs prepared through the EPN method showing superior results compared to those made with the APSP method and the unprocessed drug.

    Matched MeSH terms: Drug Liberation
  14. Tan KX, Danquah MK, Pan S, Yon LS
    J Pharm Sci, 2019 09;108(9):2934-2941.
    PMID: 31002808 DOI: 10.1016/j.xphs.2019.03.037
    Efficient delivery of adequate active ingredients to targeted malignant cells is critical, attributing to recurrent biophysical and biochemical challenges associated with conventional pharmaceutical delivery systems. These challenges include drug leakage, low targeting capability, high systemic cytotoxicity, and poor pharmacokinetics and pharmacodynamics. Targeted delivery system is a promising development to deliver sufficient amounts of drug molecules to target cells in a controlled release pattern mode. Aptameric ligands possess unique affinity targeting capabilities which can be exploited in the design of high pay-load drug formulations to navigate active molecules to the malignant sites. This study focuses on the development of a copolymeric and multifunctional drug-loaded aptamer-conjugated poly(lactide-co-glycolic acid)-polyethylenimine (PLGA-PEI) (DPAP) delivery system, via a layer-by-layer synthesis method, using a water-in-oil-in-water double emulsion approach. The binding characteristics, targeting capability, biophysical properties, encapsulation efficiency, and drug release profile of the DPAP system were investigated under varying conditions of ionic strength, polymer composition and molecular weight (MW), and degree of PEGylation of the synthetic core. Experimental results showed increased drug release rate with increasing buffer ionic strength. DPAP particulate system obtained the highest drug release of 50% at day 9 at 1 M NaCl ionic strength. DPAP formulation, using PLGA 65:35 and PEI MW of ∼800 Da, demonstrated an encapsulation efficiency of 78.93%, and a loading capacity of 0.1605 mg bovine serum albumin per mg PLGA. DPAP (PLGA 65:35, PEI MW∼25 kDa) formulation showed a high release rate with a biphasic release profile. Experimental data depicted a lower targeting power and reduced drug release rate for the PEGylated DPAP formulations. The outcomes from the present study lay the foundation to optimize the performance of DPAP system as an effective synthetic drug carrier for targeted delivery.
    Matched MeSH terms: Drug Liberation
  15. Ezhilarasu H, Ramalingam R, Dhand C, Lakshminarayanan R, Sadiq A, Gandhimathi C, et al.
    Int J Mol Sci, 2019 Oct 18;20(20).
    PMID: 31635374 DOI: 10.3390/ijms20205174
    Aloe vera (AV) and tetracycline hydrochloride (TCH) exhibit significant properties such as anti-inflammatory, antioxidant and anti-bacterial activities to facilitate skin tissue engineering. The present study aims to develop poly-ε-caprolactone (PCL)/ AV containing curcumin (CUR), and TCH loaded hybrid nanofibrous scaffolds to validate the synergistic effect on the fibroblast proliferation and antimicrobial activity against Gram-positive and Gram-negative bacteria for wound healing. PCL/AV, PCL/CUR, PCL/AV/CUR and PCL/AV/TCH hybrid nanofibrous mats were fabricated using an electrospinning technique and were characterized for surface morphology, the successful incorporation of active compounds, hydrophilicity and the mechanical property of nanofibers. SEM revealed that there was a decrease in the fiber diameter (ranging from 360 to 770 nm) upon the addition of AV, CUR and TCH in PCL nanofibers, which were randomly oriented with bead free morphology. FTIR spectra of various electrospun samples confirmed the successful incorporation of AV, CUR and TCH into the PCL nanofibers. The fabricated nanofibrous scaffolds possessed mechanical properties within the range of human skin. The biocompatibility of electrospun nanofibrous scaffolds were evaluated on primary human dermal fibroblasts (hDF) by MTS assay, CMFDA, Sirius red and F-actin stainings. The results showed that the fabricated PCL/AV/CUR and PCL/AV/TCH nanofibrous scaffolds were non-toxic and had the potential for wound healing applications. The disc diffusion assay confirmed that the electrospun nanofibrous scaffolds possessed antibacterial activity and provided an effective wound dressing for skin tissue engineering.
    Matched MeSH terms: Drug Liberation
  16. 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
  17. Pandey M, Choudhury H, D/O Segar Singh SK, Chetty Annan N, Bhattamisra SK, Gorain B, et al.
    Molecules, 2021 May 05;26(9).
    PMID: 34062995 DOI: 10.3390/molecules26092704
    A single ulcerative colitis (UC) is a chronic inflammatory bowel disease (IBD) that causes inflammation of the colonic mucosa at the distal colon and rectum. The mainstay therapy involves anti-inflammatory immunosuppression based on the disease location and severity. The disadvantages of using systemic corticosteroids for UC treatment is the amplified risk of malignancies and infections. Therefore, topical treatments are safer as they have fewer systemic side effects due to less systemic exposure. In this context, pH sensitive and enzymatically triggered hydrogel of pectin (PC) and polyacrylamide (PAM) has been developed to facilitate colon-targeted delivery of budesonide (BUD) for the treatment of UC. The hydrogels were characterized by Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), swelling ratio, and drug release. FT-IR spectroscopy confirmed the grafting as well loading of BUD in hydrogel. XRD showed the amorphous nature of hydrogel and increment in crystallinity after drug loading. On the other hand, SEM showed that the hydrogels exhibited a highly porous morphology, which is suitable for drug loading and also demonstrated a pH-responsive swelling behaviour, with decreased swelling in acidic media. The in-vitro release of BUD from the hydrogel exhibited a sustained release behaviour with non-ficken diffusion mechanism. The model that fitted best for BUD released was the Higuchi kinetic model. It was concluded that enzyme/pH dual-sensitive hydrogels are an effective colon-targeted delivery system for UC.
    Matched MeSH terms: Drug Liberation*
  18. 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
  19. 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
  20. Bera H, Mothe S, Maiti S, Vanga S
    Int J Biol Macromol, 2018 Feb;107(Pt A):604-614.
    PMID: 28916379 DOI: 10.1016/j.ijbiomac.2017.09.027
    Novel carboxymethyl fenugreek galactomannan (CFG)-gellan gum (GG)-calcium silicate (CS) composite beads were developed for controlled glimepiride (GLI) delivery. CFG having degree of carboxymethylation of 0.71 was synthesized and characterized by FTIR, DSC and XRD analyses. Subsequently, GLI-loaded hybrids were accomplished by ionotropic gelation technique employing Ca+2/Zn+2/Al+3 ions as cross-linkers. All the formulations demonstrated excellent drug encapsulation efficiency (DEE, 48-97%) and sustained drug release behaviour (Q8h, 62-94%). These quality attributes were remarkably influenced by polymer-blend (GG:CFG) ratios, cross-linker types and CS inclusion. The drug release profile of the optimized formulation (F-6) was best fitted in zero-order model with anomalous diffusion driven mechanism. It also conferred excellent ex vivo mucoadhesive property and considerable hypoglycemic effect in streptozotocin-induced diabetic rats. Furthermore, the beads were characterized for drug-excipients compatibility, drug crystallinity, thermal behaviour and surface morphology. Thus, the developed hybrid matrices are appropriate for controlled delivery of GLI for Type 2 diabetes management.
    Matched MeSH terms: Drug Liberation
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