Displaying publications 21 - 40 of 199 in total

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  1. Razavi M, Nyamathulla S, Karimian H, Noordin MI
    Drug Des Devel Ther, 2014;8:1315-29.
    PMID: 25246773 DOI: 10.2147/DDDT.S68517
    This study aimed to develop hydrophilic, gastroretentive matrix tablets of famotidine with good floating and swelling properties. A novel gastroretentive drug delivery formulation was designed using salep, also known as salepi, a flour obtained from grinding dried palmate tubers of Orchis morio var mascula (Orchidaceae family). The main polysaccharide content of salep is glucomannan, highly soluble in cold and hot water, which forms a viscous solution. Salep was characterized for physicochemical properties, thermal stability, chemical interaction, and surface morphology using X-ray diffraction analysis, differential scanning calorimetry, Fourier transform infrared spectroscopy, and scanning electron microscopy. Ten different formulations (S1-S10) were prepared using famotidine to salep ratios from 1:0.5 to 1:5. Results demonstrated that all formulations were able to sustain the drug release for more than 24 hours. The S5 formulation, with a famotidine to salep ratio of 1:2.5, had the shortest floating lag time of 35 seconds and 100% drug release within 24 hours. The dissolution data were fitted into popular mathematical models to assess the mechanism of drug release. S5 showed Zero order release (R=0.9746) with Higuchi diffusion (R=0.9428). We conclude that salep, a novel polymer, can be used in controlled release formulations to sustain release for 24 hours, due to inherent swelling and gelling properties.
    Matched MeSH terms: Drug Liberation
  2. Rahman MR, Rahman MM, Wan Khadijah WE, Abdullah RB
    Asian-Australas J Anim Sci, 2014 Sep;27(9):1270-4.
    PMID: 25178370 DOI: 10.5713/ajas.2013.13786
    An experiment was conducted to evaluate the efficacy of porcine follicle stimulating hormone (pFSH) dosage based on body weight (BW) on ovarian responses of crossbred does. Thirty donor does were divided into 3 groups getting pFSH dosages of 3, 5, and 8 mg pFSH per kg BW, respectively, and were named as pFSH-3, pFSH-5 and pFSH-8, respectively. Estrus was synchronized by inserting a controlled internal drug release (CIDR) device and a single injection of prostaglandin F2α (PGF2α). The pFSH treatments were administered twice a day through 6 decreasing dosages (25, 25, 15, 15, 10, and 10% of total pFSH amount; decreasing daily). Ovarian responses were evaluated on Day 7 after CIDR removal. After CIDR removal, estrus was observed 3 times in a day and pFSH treatments were initiated at 2 days before the CIDR removal. All does in pFSH-5 and pFSH-8 showed estrus signs while half of the does in pFSH-3 showed estrus signs. No differences (p>0.05) were observed on the corpus luteum and total ovarian stimulation among the treatment groups, while total and transferable embryos were higher (p<0.05) in pFSH-5 (7.00 and 6.71) than pFSH-3 (3.00 and 2.80) and pFSH-8 (2.00 and 1.50), respectively. In conclusion, 5 mg pFSH per kg BW dosage gave a higher number of embryos than 3 and 8 mg pFSH per kg BW dosages. The results indicated that the dosage of pFSH based on BW is an important consideration for superovulation in goats.
    Matched MeSH terms: Drug Liberation
  3. Halib N, Mohd Amin MC, Ahmad I, Abrami M, Fiorentino S, Farra R, et al.
    Eur J Pharm Sci, 2014 Oct 1;62:326-33.
    PMID: 24932712 DOI: 10.1016/j.ejps.2014.06.004
    This paper focuses on the micro- and nano-topological organization of a hydrogel, constituted by a mixture of bacterial cellulose and acrylic acid, and intended for biomedical applications. The presence of acrylic acid promotes the formation of two interpenetrated continuous phases: the primary "pores phase" (PP) containing only water and the secondary "polymeric network phase" (PNP) constituted by the polymeric network swollen by the water. Low field Nuclear Magnetic Resonance (LF NMR), rheology, Scanning Electron Microscopy (SEM) and release tests were used to determine the characteristics of the two phases. In particular, we found that this system is a strong hydrogel constituted by 81% (v/v) of PP phase the remaining part being occupied by the PNP phase. Pores diameters span in the range 10-100 μm, the majority of them (85%) falling in the range 30-90 μm. The high PP phase tortuosity indicates that big pores are not directly connected to each other, but their connection is realized by a series of interconnected small pores that rend the drug path tortuous. The PNP is characterized by a polymer volume fraction around 0.73 while mesh size is around 3 nm. The theoretical interpretation of the experimental data coming from the techniques panel adopted, yielded to the micro- and nano-organization of our hydrogel.
    Matched MeSH terms: Drug Liberation
  4. Bose A, Wong TW, Singh N
    Saudi Pharm J, 2013 Apr;21(2):201-13.
    PMID: 23960836 DOI: 10.1016/j.jsps.2012.03.006
    The objective of this present investigation was to develop and formulate sustained release (SR) matrix tablets of Itopride HCl, by using different polymer combinations and fillers, to optimize by Central Composite Design response surface methodology for different drug release variables and to evaluate drug release pattern of the optimized product. Sustained release matrix tablets of various combinations were prepared with cellulose-based polymers: hydroxy propyl methyl cellulose (HPMC) and polyvinyl pyrolidine (pvp) and lactose as fillers. Study of pre-compression and post-compression parameters facilitated the screening of a formulation with best characteristics that underwent here optimization study by response surface methodology (Central Composite Design). The optimized tablet was further subjected to scanning electron microscopy to reveal its release pattern. The in vitro study revealed that combining of HPMC K100M (24.65 MG) with pvp(20 mg)and use of LACTOSE as filler sustained the action more than 12 h. The developed sustained release matrix tablet of improved efficacy can perform therapeutically better than a conventional tablet.
    Matched MeSH terms: Drug Liberation
  5. Koh PT, Chuah JN, Talekar M, Gorajana A, Garg S
    Indian J Pharm Sci, 2013 May;75(3):291-301.
    PMID: 24082345 DOI: 10.4103/0250-474X.117434
    The aim of this study was to enhance the dissolution rate of efavirenz using solid dispersion systems (binary and ternary). A comparison between solvent and fusion method was also investigated. Solid dispersions of efavirenz were prepared using polyethylene glycol 8000, polyvinylpyrrolidone K30 alone and combination of both. Tween 80 was incorporated to obtain a ternary solid dispersion system. Dissolution tests were conducted and evaluated on the basis of cumulative percentage drug release and dissolution efficiency. Physicochemical characterizations of the solid dispersions were carried out using differential scanning calorimetric, powder X-ray diffraction, Fourier transform infrared spectroscopy, and scanning electron microscopy. Dissolution was remarkably improved in both systems compared to pure efavirenz (P<0.05). An optimum ratio was identified at a drug:polymer of 1:10. Incorporation of Tween 80 to 1:10 formulations formed using solvent method showed further improvement in the dissolution rate. Physicochemical characterization results suggested that efavirenz existed in the amorphous form in all the solid dispersion systems providing evidence of improvement in dissolution. No statistically significant difference (P>0.05) in dissolution was observed between the two methods. Binary and ternary solid dispersion systems both have showed a significant improvement in the dissolution rate of efavirenz. Formulations with only polyvinylpyrrolidone K30 showed best dissolution profile and 1:10 was identified as an optimum drug-polymer weight ratio.
    Matched MeSH terms: Drug Liberation
  6. Pandurangan DK, Bodagala P, Palanirajan VK, Govindaraj S
    Int J Pharm Investig, 2016 Jan-Mar;6(1):56-62.
    PMID: 27014620 DOI: 10.4103/2230-973X.176488
    In the present investigation, solid lipid nanoparticles (SLNs)-loaded in situ gel with voriconazole drug was formulated. Further, the formulation was characterized for pH, gelling capacity, entrapment efficiency, in vitro drug release, drug content, and viscosity. Voriconazole is an antifungal drug used to treat various infections caused by yeast or other types of fungi. Film hydration technique was used to prepared SLNs from lecithin and cholesterol. Based on the entrapment efficiency 67.2-97.3% and drug release, the optimized formulation NF1 of SLNs was incorporated into in situ gels. The in situ gels were prepared using viscosity-enhancing polymers such as Carbopol and (hydroxypropyl)methyl cellulose (HPMC). Formulated SLN in situ gel formulations were characterized, which showed pH 4.9-7.1, drug content 65.69-96.3%, and viscosity (100 rpm) 120-620 cps. From the characterizations given above, F6 was optimized and evaluated for microbial assay and ocular irritation studies. Microbial assay was conducted by the cup-plate method using Candida albicans as the test organism. An ocular irritation study was conducted on albino rabbits. The results revealed that there was no ocular damage to the cornea, conjunctiva, or iris. Stability studies were carried out on the F6 formulation for 3 months, which showed that the formulation had good stability. These results indicate that the studied SLNs-loaded in situ gel is a promising vehicle for ocular delivery.
    Matched MeSH terms: Drug Liberation
  7. Haniza Hassan, Ahmad Fuad Shamsuddin, Ekram Alias, Meor Mohd Redzuan Meor Mohd Affandi, Siti Khadijah Adam, Rusliza Basir
    MyJurnal
    Introduction:Acyclovir, a widely marketed antiviral drug is used for the treatment of Herpes Simplex infection. High doses of acyclovir are prescribed to patients to attain its maximum therapeutic effect due to its poor absorption and low oral bioavailability. The current therapeutics regiment of acyclovir are known to cause unwarranted adverse effects, thus prompted the need for a suitable drug carrier to improve the pharmacokinetic limitations. Develop-ment of solid lipid nanoparticles for oral delivery of acyclovir proposed in this study aimed to enhance acyclovir oral bioavailability. Methods: Comprehensive experiments and a series of optimization process were carried out to ensure reproducibility and assurance of product quality. The physicochemical characteristics of the solid lipid nanoparticles developed from plant-based solid lipid, Biogapress Vegetal 297 ATO with polysorbate 80 as an emul-sifying agent were also evaluated. Results: The spherical-shaped nanoparticles had an average size of 123 nm with good drug entrapment efficiency, up to 80%. The in vitro drug release study showed that solid lipid nanoparticles had prolonged acyclovir release in simulated intestinal fluid for 24 hours. The nanoparticles formulation was con-sidered stable during storage at refrigerated temperature for at least three months. In vivo oral bioavailability study showed that acyclovir-loaded solid lipid nanoparticles possessed superior oral bioavailability when compared with the commercial acyclovir suspension. Conclusion: In conclusion, this study exhibited the feasibility of solid lipid nanoparticles as an oral delivery vehicle for acyclovir and therefore represent a new promising therapeutic concept of nanoparticulate delivery system.
    Matched MeSH terms: Drug Liberation
  8. 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
  9. 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
  10. Alrimawi BH, Chan MY, Ooi XY, Chan SY, Goh CF
    Polymers (Basel), 2021 Feb 15;13(4).
    PMID: 33671895 DOI: 10.3390/polym13040578
    Rice starch is a promising biomaterial for thin film development in buccal drug delivery, but the plasticisation and antiplasticisation phenomena from both plasticisers and drugs on the performance of rice starch films are not well understood. This study aims to elucidate the competing effects of sorbitol (plasticiser) and drug (antiplasticiser) on the physicochemical characteristics of rice starch films containing low paracetamol content. Rice starch films were prepared with different sorbitol (10, 20 and 30% w/w) and paracetamol contents (0, 1 and 2% w/w) using the film casting method and were characterised especially for drug release, swelling and mechanical properties. Sorbitol showed a typical plasticising effect on the control rice starch films by increasing film flexibility and by reducing swelling behaviour. The presence of drugs, however, modified both the mechanical and swelling properties by exerting an antiplasticisation effect. This antiplasticisation action was found to be significant at a low sorbitol level or a high drug content. FTIR investigations supported the antiplasticisation action of paracetamol through the disturbance of sorbitol-starch interactions. Despite this difference, an immediate drug release was generally obtained. This study highlights the interplay between plasticiser and drug in influencing the mechanical and swelling characteristics of rice starch films at varying concentrations.
    Matched MeSH terms: Drug Liberation
  11. Shaedi N, Naharudin I, Choo CY, Wong TW
    Carbohydr Polym, 2021 Feb 15;254:117312.
    PMID: 33357875 DOI: 10.1016/j.carbpol.2020.117312
    Vitexin of Ficus deltoidea exhibits intestinal α-glucosidase inhibitory and blood glucose lowering effects. This study designs oral intestinal-specific alginate nanoparticulate system of vitexin. Nanospray-dried alginate, alginate/stearic acid and alginate-C18 conjugate nanoparticles were prepared. Stearic acid was adopted to hydrophobize the matrix and minimize premature vitexin release in stomach, whereas C-18 conjugate as immobilized fatty acid to sustain hydrophobic effect and drug release. Nanoparticles were compacted with polyethylene glycol (PEG 3000, 10,000 and 20,000). The physicochemical, drug release, in vivo blood glucose lowering and intestinal vitexin content of nanoparticles and compact were determined. Hydrophobization of alginate nanoparticles promoted premature vitexin release. Compaction of nanoparticles with PEG minimized vitexin release in the stomach, with stearic acid loaded nanoparticles exhibiting a higher vitexin release in the intestine. The introduction of stearic acid reduced vitexin-alginate interaction, conferred alginate-stearic acid mismatch, and dispersive stearic acid-induced particle breakdown with intestinal vitexin release. Use of PEG 10,000 in compaction brought about PEG-nanoparticles interaction that negated initial vitexin release. The PEG dissolution in intestinal phase subsequently enabled particle breakdown and vitexin release. The PEG compacted nanoparticles exhibited oral intestinal-specific vitexin release, with positive blood glucose lowering and enhanced intestinal vitexin content in vivo.
    Matched MeSH terms: Drug Liberation
  12. Ebadi M, Bullo S, Buskaran K, Hussein MZ, Fakurazi S, Pastorin G
    Polymers (Basel), 2021 Mar 10;13(6).
    PMID: 33802205 DOI: 10.3390/polym13060855
    Iron oxide nanoparticles are suitable for biomedical applications owing to their ability to anchor to various active agents and drugs, unique magnetic properties, nontoxicity, and biocompatibility. In this work, the physico-chemical and magnetic properties, as well as the cytotoxicity, of Fe3O4 nanoparticles coated with a polymeric carrier and loaded with a 5-fluorouracil (5-FU) anti-cancer drug are discussed. The synthesized Fe3O4 nanoparticles were coated with polyvinyl alcohol and Zn/Al-layered double hydroxide as the drug host. The XRD, DTA/TG, and FTIR analyzes confirmed the presence of the coating layer on the surface of nanoparticles. The results showed a decrease in saturation magnetization of bare Fe3O4 nanoparticles after coating with the PVA/5FU/Zn/Al-LDH layer. In addition, the presence of the coating prevented the agglomeration of nanoparticles. Furthermore, the pseudo-second-order equation governed the kinetics of drug release. Finally, the coated nanoparticles showed stronger activity against liver cancer cells (HepG2) compared to that of the naked 5-FU drug, and displayed no cytotoxicity towards 3T3 fibroblast cell lines. The results of the present study demonstrate the potential of a nano delivery system for cancer treatment.
    Matched MeSH terms: Drug Liberation
  13. 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
  14. Noor NM, Abdul-Aziz A, Sheikh K, Somavarapu S, Taylor KMG
    Pharmaceutics, 2020 Oct 20;12(10).
    PMID: 33092119 DOI: 10.3390/pharmaceutics12100994
    Dutasteride, licensed as an oral medicine for the treatment of benign prostatic hypoplasia, has been investigated as a treatment for androgenic alopecia. In this study, the potential for dustasteride to be delivered topically in order to reduce systemic exposure, irritation of the skin, and also cytotoxicity was explored. Chitosan oligomer (CSO) was successfully synthesised with lauric acid as a coating for a dutasteride-loaded nanostructured lipid carriers (DST-NLCs) system. DST-NLCs were prepared using a combination of melt-dispersion and ultrasonication. These negatively charged NLCs (-18.0 mV) had a mean particle size of ~184 nm, which was not significantly increased (p > 0.05) when coated with lauric acid-chitosan oligomer (CSO-LA), whilst the surface charge changed to positive (+24.8 mV). The entrapment efficiency of DST-NLCs was 97%, and coated and uncoated preparations were physically stable for up to 180 days at 4-8 °C. The drug release was slower from DST-NLCs coated with CSO-LA than from uncoated NLCs, with no detectable drug permeation through full-thickness pig ear skin from either preparation. Considering the cytotoxicity, the IC50 values for the DST-NLCs, coated and uncoated with CSO-LA were greater than for dutasteride alone (p < 0.05). DST-NLCs and empty NLCs coated with CSO-LA at 25 µM increased the cell proliferation compared to the control, and no skin irritation was observed when the DST-NLC formulations were tested using EpiDerm™. The cell and skin uptake studies of coated and uncoated NLCs incorporating the fluorescent marker Coumarin-6 showed the time-dependent uptake of Coumarin-6. Overall, the findings suggest that DST-NLCs coated with CSO-LA represent a promising formulation strategy for dutasteride delivery for the treatment of androgenic alopecia, with a reduced cytotoxicity compared to that of the drug alone and lower irritancy than an ethanolic solution of dutasteride.
    Matched MeSH terms: Drug Liberation
  15. Sheshala R, Anuar NK, Abu Samah NH, Wong TW
    AAPS PharmSciTech, 2019 Apr 15;20(5):164.
    PMID: 30993407 DOI: 10.1208/s12249-019-1362-7
    This review highlights in vitro drug dissolution/permeation methods available for topical and transdermal nanocarriers that have been designed to modulate the propensity of drug release, drug penetration into skin, and permeation into systemic circulation. Presently, a few of USFDA-approved in vitro dissolution/permeation methods are available for skin product testing with no specific application to nanocarriers. Researchers are largely utilizing the in-house dissolution/permeation testing methods of nanocarriers. These drug release and permeation methods are pending to be standardized. Their biorelevance with reference to in vivo plasma concentration-time profiles requires further exploration to enable translation of in vitro data for in vivo or clinical performance prediction.
    Matched MeSH terms: Drug Liberation
  16. Surjit Singh CK, Lim HP, Tey BT, Chan ES
    Carbohydr Polym, 2021 Jan 01;251:117110.
    PMID: 33142647 DOI: 10.1016/j.carbpol.2020.117110
    The commercial application of liquid-state Pickering emulsions in food systems remains a major challenge. In this study, we developed a spray-dried Pickering emulsion powder using chitosan as a Pickering emulsifier and alginate as a coating material. The functionality of the powder was evaluated in terms of its oxidative stability, pH-responsiveness, mucoadhesivity, and lipid digestibility. The Pickering emulsion powder was oxidatively more stable than the conventional emulsion powder stabilized by gum Arabic. The powder exhibited pH-responsiveness, whereby it remained intact in acidic pH, but dissolved to release the emulsion in 'Pickering form' at near-neutral pH. The Pickering emulsion powder was also mucoadhesive and could be digested by lipase in a controlled manner. These findings suggested that the multi-functional Pickering emulsion powder could be a potential delivery system for applications in the food industry.
    Matched MeSH terms: Drug Liberation
  17. 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
  18. Yusefi M, Shameli K, Jahangirian H, Teow SY, Umakoshi H, Saleh B, et al.
    Int J Nanomedicine, 2020;15:5417-5432.
    PMID: 32801697 DOI: 10.2147/IJN.S250047
    Introduction: Green-based materials have been increasingly studied to circumvent off-target cytotoxicity and other side-effects from conventional chemotherapy.

    Materials and Methods: Here, cellulose fibers (CF) were isolated from rice straw (RS) waste by using an eco-friendly alkali treatment. The CF network served as an anticancer drug carrier for 5-fluorouracil (5-FU). The physicochemical and thermal properties of CF, pure 5-FU drug, and the 5-FU-loaded CF (CF/5-FU) samples were evaluated. The samples were assessed for in vitro cytotoxicity assays using human colorectal cancer (HCT116) and normal (CCD112) cell lines, along with human nasopharyngeal cancer (HONE-1) and normal (NP 460) cell lines after 72-hours of treatment.

    Results: XRD and FTIR revealed the successful alkali treatment of RS to isolate CF with high purity and crystallinity. Compared to RS, the alkali-treated CF showed an almost fourfold increase in surface area and zeta potential of up to -33.61 mV. SEM images illustrated the CF network with a rod-shaped structure and comprised of ordered aggregated cellulose. TGA results proved that the thermal stability of 5-FU increased within the drug carrier. Based on UV-spectroscopy measurements for 5-FU loading into CF, drug loading encapsulation efficiency was estimated to be 83 ±0.8%. The release media at pH 7.4 and pH 1.2 showed a maximum drug release of 79% and 46%, respectively, over 24 hours. In cytotoxicity assays, CF showed almost no damage, while pure 5-FU killed most of the both normal and cancer cells. Impressively, the drug-loaded sample of CF/5-FU at a 250 µg/mL concentration demonstrated a 58% inhibition against colorectal cancer cells, but only a 23% inhibition against normal colorectal cells. Further, a 62.50 µg/mL concentration of CF/5FU eliminated 71% and 39% of nasopharyngeal carcinoma and normal nasopharyngeal cells, respectively.

    Discussion: This study, therefore, showed the strong potential anticancer activity of the novel CF/5-FU formulations, warranting their further investigation.

    Matched MeSH terms: Drug Liberation
  19. Ng LC, Gupta M
    Asian J Pharm Sci, 2020 Jan;15(1):13-25.
    PMID: 32175015 DOI: 10.1016/j.ajps.2019.04.006
    Diabetes mellitus is a chronic disease in which there is an insufficient production of insulin by the pancreas, or the insulin produced is unable to be utilized effectively by the body. Diabetes affects more than 415 million people globally and is estimated to strike about 642 million people in 2040. The WHO reported that diabetes will become the seventh biggest cause of mortality in 2030. Insulin injection and oral hypoglycemic agents remain the primary treatments in diabetes management. These often present with poor patient compliance. However, over the last decade, transdermal systems in diabetes management have gained increasing attention and emerged as a potential hope in diabetes management owing to the advantages that they offer as compared to invasive injection and oral dosage forms. This review presents the recent advances and developments in transdermal research to achieve better diabetes management. Different technologies and approaches have been explored and applied to the transdermal systems to optimize diabetes management. Studies have shown that these transdermal systems demonstrate higher bioavailability compared to oral administration due to the avoidance of first-pass hepatic metabolism and a sustained drug release pattern. Besides that, transdermal systems have the advantage of reducing dosing frequency as drugs are released at a predetermined rate and control blood glucose level over a prolonged time, contributing to better patient compliance. In summary, the transdermal system is a field worth exploring due to its significant advantages over oral route in administration of antidiabetic drugs and biosensing of blood glucose level to ensure better clinical outcomes in diabetes management.
    Matched MeSH terms: Drug Liberation
  20. 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
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