Displaying publications 1 - 20 of 215 in total

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  1. 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*
  2. Nur Fatin Nazurah R, Noranizan MA, Nor-Khaizura MAR, Nur Hanani ZA
    Int J Biol Macromol, 2024 Jul;273(Pt 2):132972.
    PMID: 38876241 DOI: 10.1016/j.ijbiomac.2024.132972
    The use of essential oils as natural antioxidant, antimicrobial and insect repellent agent was limited by the loss of bioactive components especially volatile compounds. This study aimed to improve biological properties of curry leaf essential oil (CLEO) by producing nanometer sized particles through two different synthesis techniques; nanoencapsulation and nanoprecipitation. The methods produced different nanostructures; nanocapsules and nanospheres distinguished by the morphological structure (TEM analysis). Successful loading of CLEO into chitosan nanocarrier was proven by FTIR spectra. Zeta potential values for both nanostructures were more than +30 mV implying their stability against aggregation. CLEO loaded nanocapsules exhibited highest antibacterial properties against Gram-positive bacteria compared to nanospheres. Meanwhile, CLEO loaded nanospheres recorded up until 90.44 % DPPH radical scavenging properties, higher compared to nanocapsules. Both nanostructures demonstrated further improvement in antioxidant and antibacterial activities with the incorporation of higher chitosan concentration. In vitro release analysis indicated that CLEO undergo two-stage discharge mechanism where fast discharge occurred up until 12 h followed by sustained released afterwards. The two synthesis methods applied synergistically with greater chitosan concentration successfully produced nanostructures with >60 % encapsulation efficiency (EE). This concluded that both techniques were reliable to protect the bioactive constituents of CLEO for further used.
    Matched MeSH terms: Drug Liberation*
  3. Sammour RMF, Chatterjee B, Taher M, Saleh MSM, Shahiwala A
    Curr Drug Deliv, 2021;18(9):1272-1279.
    PMID: 33605859 DOI: 10.2174/1567201818666210219105509
    BACKGROUND: Improved bioavailability of Aceclofenac (ACE) may be achieved through proniosomes, which are considered as one of the most effective drug delivery systems and are expected to represent a valuable approach for the development of better oral dosage form as compared to the existing product. However, the carrier in this system plays a vital role in controlling the drug release and modulating drug dissolution. Accordingly, a comparative study on different carriers can give a clear idea about the selection of carriers to prepare ACE proniosomes.

    OBJECTIVE: This study aims to evaluate the role of maltodextrin, glucose, and mannitol as carriers for in vitro and in vivo performance of Aceclofenac (ACE) proniosomes.

    METHODS: Three formulations of proniosomes were prepared by the slurry method using the 100 mg ACE, 500 mg span 60, 250 mg cholesterol with 1300mg of different carriers, i.e., glucose (FN1), maltodextrin (FN2), and mannitol (FN3). In vitro drug release studies were conducted by the USP paddle method, while in vivo studies were performed in albino rats. Pure ACE was used as a reference in all the tests. Lastly, the results were analyzed using the High-Pressure Liquid Chromatography (HPLC) method, and data were evaluated using further kinetic and statistical tools.

    RESULTS: No significant differences (p > 0.05) in entrapment efficiency (%EE) of FN1, FN2, and FN3 (82 ± 0.5%, 84 ± 0.66%, and 84 ± 0.34% respectively) were observed and formulations were used for further in vitro and in vivo evaluations. During in vitro drug release studies, the dissolved drug was found to be 42% for the pure drug, while 70%, 17%, and 30% for FN1, FN2, and FN3, respectively, at 15 min. After 24 hrs, the pure drug showed a maximum of 50% release while 94%, 80%, and 79% drug release were observed after 24 hr for FN1, FN2, and FN3, respectively. The in vivo study conducted on albino rats showed a higher Cmax and AUC of FN1 and FN2 in comparison with the pure ACE. Moreover, the relative oral bioavailability of proniosomes with maltodextrin and glucose as carriers compared to the pure drug was 183% and 112%, respectively. Mannitol- based formulation exhibited low bioavailability (53.7%) that may be attributed to its osmotic behavior.

    CONCLUSION: These findings confirm that a carrier plays a significant role in determining in vitro and in vivo performance of proniosomes and careful selection of carrier is an important aspect of proniosomes optimization.

    Matched MeSH terms: Drug Liberation
  4. Suteris NN, Yasin A, Misnon II, Roslan R, Zulkifli FH, Rahim MHA, et al.
    Int J Biol Macromol, 2022 Feb 15;198:147-156.
    PMID: 34971642 DOI: 10.1016/j.ijbiomac.2021.12.006
    This article demonstrates the development of nanofibrous cloths by electrospinning of renewable materials, i.e., curcumin-loaded 90% cellulose acetate (CA)/10% poly(ε-caprolactone) (PCL), for applications in regenerative medicine. The CA is derived from the biomass waste of the oil palm plantation (empty fruit bunch). The nanofiber scaffolds are characterized for the fiber morphology, microstructure, thermal properties, and wettability. The optimized smooth and bead-free electrospun fiber cloth contains 90% CA and 10% PCL in two curcumin compositions (0.5 and 1 wt%). The role of curcumin is shown to be two-fold: the first is its function as a drug and the second is its role in lowering the water contact angle and increasing the hydrophilicity. The hydrophilicity enhancements are related to the hydrogen bonding between the components. The enhanced hydrophilicity contributed to improve the swelling behavior of the scaffolds; the CA/PCL/Cur (0.5%) and the CA/PCL/Cur (1.0%) showed swelling of ~700 and 950%, respectively, in phosphate-buffered saline (PBS). The drug-release studies revealed the highest cumulative drug release of 60% and 78% for CA/PCL/Cur (0.5%) and CA/PCL/Cur (1.0%) nanofibers, respectively. The in-vitro studies showed that CA/PCL/Cur (0.5 wt%) and CA/PCL/Cur (1.0 wt%) nanofiber scaffolds facilitate a higher proliferation and expression of actin in fibroblasts than those scaffolds without curcumin for wound healing applications.
    Matched MeSH terms: Drug Liberation
  5. Malik MK, Kumar V, Kumarasamy V, Singh OP, Kumar M, Dixit R, et al.
    Molecules, 2024 Jul 05;29(13).
    PMID: 38999160 DOI: 10.3390/molecules29133208
    Chemically modified mandua starch was successfully synthesized and applied to coat mesalamine-loaded matrix tablets. The coating material was an aqueous dispersion of mandua starch modified by sodium trimetaphosphate and sodium tripolyphosphate. To investigate the colon-targeting release competence, chemically modified mandua starch film-coated mesalamine tablets were produced using the wet granulation method followed by dip coating. The effect of the coating on the colon-targeted release of the resultant delivery system was inspected in healthy human volunteers and rabbits using roentgenography. The results show that drug release was controlled when the coating level was 10% w/w. The release percentage in the upper gastric phase (pH 1.2, simulated gastric fluid) was less than 6% and reached up to 59.51% w/w after 14 h in simulated colonic fluid. In addition to in vivo roentgenographic studies in healthy rabbits, human volunteer studies proved the colon targeting efficiency of the formulation. These results clearly demonstrated that chemically modified mandua starch has high effectiveness as a novel aqueous coating material for controlled release or colon targeting.
    Matched MeSH terms: Drug Liberation*
  6. Che Zain MS, Danish M, Shaari K, Fakurazi S
    Daru, 2024 Dec;32(2):689-703.
    PMID: 39340725 DOI: 10.1007/s40199-024-00540-z
    BACKGROUND: Amorphous hydrogel is a strategic wound healing dressings that comprised of water, polymers and excipients with no shape. The dense cross-linked network of polymer is interspersed by the immobilized water component could rehydrate and promote healing in wound tissue.

    OBJECTIVE: In this work, various polysaccharide/gelatin amorphous hydrogels with the impregnation of oil palm leaf derived total flavonoid enriched extract (OPL-TFEE) were fabricated via one-pot synthesis method to provide multiple crosslinking networks.

    METHOD: The bioflavonoids (OPL-TFEE) were derived from Elaeis guineensis leaf using an integrated green extraction and enrichment process. Amorphous hydrogels with good wound healing properties were developed by incorporating 0.3% antioxidant agent into the hybrid polymeric gelling system.

    RESULT: The formulations appeared as a semi-solid dark yellow translucent hydrogel with good spreading and consistency characteristics and satisfying aesthetic properties. The FTIR analysis indicated that the bioflavonoid was compatible with the matrix, and the hydrogels showed porous morphological structures when observed under SEM. Furthermore, the hydrogels possessed shear thinning, pseudoplastic, and elastic properties. Bioflavonoids-impregnated polysaccharide/gelatin hydrogel release 95-98% bioflavonoids within 24 h, while the drug release profile followed the Korsmeyer-Peppas kinetic model. The hydrogels showed antioxidant and wound healing properties with no sign of cytotoxicity.

    CONCLUSION: Overall, the results revealed bioflavonoid-loaded hydrogels exhibited good physicochemical and biological properties, thus could serve as new innovative formulation in the sustainable advancement of wound care product for promoting wound healing.

    Matched MeSH terms: Drug Liberation*
  7. Salma H, Melha YM, Sonia L, Hamza H, Salim N
    J Pharm Sci, 2021 06;110(6):2531-2543.
    PMID: 33548245 DOI: 10.1016/j.xphs.2021.01.032
    The purpose of this study was to simultaneously predict the drug release and skin permeation of Piroxicam (PX) topical films based on Chitosan (CTS), Xanthan gum (XG) and its Carboxymethyl derivatives (CMXs) as matrix systems. These films were prepared by the solvent casting method, using Tween 80 (T80) as a permeation enhancer. All of the prepared films were assessed for their physicochemical parameters, their in vitro drug release and ex vivo skin permeation studies. Moreover, deep learning models and machine learning models were applied to predict the drug release and permeation rates. The results indicated that all of the films exhibited good consistency and physicochemical properties. Furthermore, it was noticed that when T80 was used in the optimal formulation (F8) based on CTS-CMX3, a satisfactory drug release pattern was found where 99.97% of PX was released and an amount of 1.18 mg/cm2 was permeated after 48 h. Moreover, Generative Adversarial Network (GAN) efficiently enhanced the performance of deep learning models and DNN was chosen as the best predictive approach with MSE values equal to 0.00098 and 0.00182 for the drug release and permeation kinetics, respectively. DNN precisely predicted PX dissolution profiles with f2 values equal to 99.99 for all the formulations.
    Matched MeSH terms: Drug Liberation
  8. Setapa A, Ahmad N, Mohd Mahali S, Mohd Amin MCI
    Polymers (Basel), 2020 Dec 05;12(12).
    PMID: 33291495 DOI: 10.3390/polym12122921
    Various swelling drug delivery devices are promising materials for control drug delivery because of their ability to swell and release entrapped therapeutics, in response to physiological stimuli. Previously, many mathematical models have been developed to predict the mechanism of drug release from a swelling device. However, some of these models do not consider the changes in diffusion behaviour as the device swells. Therefore, we used a two-phase approach to simplify the mathematical model considering the effect of swelling on the diffusion coefficient. We began by defining a moving boundary problem to consider the swelling process. Landau transformation was used for mitigating the moving boundary problem. The transformed problem was analytically solved using the separation of variables method. Further, the analytical solution was extended to include the drug release in two phases where each phase has distinct diffusion coefficient and continuity condition was applied. The newly developed model was validated by the experimental data of bacterial cellulose hydrogels using the LSQCURVEFIT function in MATLAB. The numerical test showed that the new model exhibited notable improvement in curve fitting, and it was observed that the initial effective diffusion coefficient of the swelling device was lower than the later effective diffusion coefficient.
    Matched MeSH terms: Drug Liberation
  9. Musa N, Wong TW
    Carbohydr Polym, 2020 Nov 01;247:116673.
    PMID: 32829801 DOI: 10.1016/j.carbpol.2020.116673
    Microencapsulation of polysaccharidic nanoparticles is met with nanoscale and biological performance changes. This study designs soft agglomerates as nanoparticle vehicle without nanoparticles undergoing physical processes that alter their geometry. The nanoparticles were made of high molecular weight chitosan/pectin with covalent 5-fluorouracil/folate. Nanoparticle aggregation vehicle was prepared from low molecular weight chitosan. The nanoparticles and aggregation vehicle were blended in specific weight ratios to produce soft agglomerates. Nanoparticles alone are unable to agglomerate. Adding aggregation vehicle (< 2 μm) promoted soft agglomeration with nanoparticles deposited onto its surfaces with minimal binary coalescence. The large and rough-surfaced aggregation vehicle promoted nanoparticles deposition and agglomeration. A rounder vehicle allowed assembly of nanoparticles-on-aggregation vehicle into agglomerates through interspersing smaller between larger populations. Soft agglomeration reduced early drug release, and was responsive to intracapsular sodium alginate coat to further sustain drug release. The soft agglomerates can serve as a primary oral colon-specific vehicle.
    Matched MeSH terms: Drug Liberation
  10. Wan Md Zin Wan Yunus, Tajau, Rida, Khairul Zaman Mohd Dahlan, Mohd Hilmi Mahmood, Kamaruddin Hashim, Mohd Yusof Hamzah
    MyJurnal
    The use of microemulsion in the development of nanoparticle based on acrylated palm oil product is demonstrated. Acr ylated palm oil microemulsions were prepared using ionic surfactant. Combination methods of emulsion polymerization and radiation crosslinking were applied to the microemulsion system for synthesizing nanoparticle. The ionizing radiat ion technique was introduced to generate a crosslinking reaction in the development of nanoparticle. The nanoparticle was evaluated in terms of particle diameter, surface charge, pH and conductance. Their image was captured using Tra nsmission electron microscopy (TEM). Results show that the size, charge and shape of the particles are influenced by c oncentration of surfactants, monomer concentration, radiation dose and time of storage. The study showed a promising method to produced nanoparticle. This nano-sized product has the potential to be utilized as controlled-drug-release-carrier.
    Matched MeSH terms: Drug Liberation
  11. 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
  12. Abdul Khodir WKW, Abdul Razak AH, Ng MH, Guarino V, Susanti D
    J Funct Biomater, 2018 May 18;9(2).
    PMID: 29783681 DOI: 10.3390/jfb9020036
    In the current practice, the clinical use of conventional skin substitutes such as autogenous skin grafts have shown several problems, mainly with respect to limited sources and donor site morbidity. In order to overcome these limitations, the use of smart synthetic biomaterials is tremendously diffusing as skin substitutes. Indeed, engineered skin grafts or analogues frequently play an important role in the treatment of chronic skin wounds, by supporting the regeneration of newly formed tissue, and at the same time preventing infections during the long-term treatment. In this context, natural proteins such as collagen-natively present in the skin tissue-embedded in synthetic polymers (i.e., PCL) allow the development of micro-structured matrices able to mimic the functions and to structure of the surrounding extracellular matrix. Moreover, the encapsulation of drugs, such as gentamicin sulfate, also improves the bioactivity of nanofibers, due to the efficient loading and a controlled drug release towards the site of interest. Herein, we have done a preliminary investigation on the capability of gentamicin sulfate, loaded into collagen-added nanofibers, for the controlled release in local infection treatments. Experimental studies have demonstrated that collagen added fibers can be efficaciously used to administrate gentamicin for 72 h without any toxic in vitro response, thus emerging as a valid candidate for the therapeutic treatment of infected wounds.
    Matched MeSH terms: Drug Liberation
  13. Uyen NTT, Hamid ZAA, Tram NXT, Ahmad N
    Int J Biol Macromol, 2020 Jun 15;153:1035-1046.
    PMID: 31794824 DOI: 10.1016/j.ijbiomac.2019.10.233
    Alginate microspheres (AMs) have received much attention as a novel drug delivery system owing to various advantages of alginate such as inexpensiveness, nontoxicity, biocompatibility and biodegradability. The well-designed fabrication method is essential to achieve desired AMs suitable for specific drug delivery system. Reports on AMs preparation techniques have increased rapidly in the last decade. A number of synthesis parameters have been investigated for the improvement of physical, chemical and biological properties of AMs. Hence, this review summarizes the work to date on the fabrication techniques of AMs for drug delivery system, including spray-drying, extrusion and emulsification/gelation technique. Besides, the influence of various factors such as alginate concentration, oil phase, surfactant, cross-linker concentrations, cross-linking time, stirring speed, model drug and drug content on the morphologies, properties and encapsulation efficiency (EE) of AMs via extrusion and emulsification/gelation technique are summarized. Before embarking on the development of any drug delivery system, a thorough understanding of drug release mechanism and factors that impact the drug release profile are essential, which are also covered in this review.
    Matched MeSH terms: Drug Liberation
  14. 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
  15. Almurisi SH, Doolaanea AA, Akkawi ME, Chatterjee B, Ahmed Saeed Aljapairai K, Islam Sarker MZ
    Drug Dev Ind Pharm, 2020 Aug;46(8):1373-1383.
    PMID: 32619118 DOI: 10.1080/03639045.2020.1791165
    OBJECTIVE: Paracetamol is a common antipyretic and analgesic medicine used in childhood illness by parents and physicians worldwide. Paracetamol has a bitter taste that is considered as a significant barrier for drug administration. This study aimed to develop an oral dosage form that is palatable and easy to swallow by pediatric patients as well as to overcome the shortcomings of liquid formulations.

    METHODS: The paracetamol was encapsulated in beads, which were prepared mainly from alginate and chitosan through electrospray technique. The paracetamol beads were sprinkled on the instant jelly prepared from glycine, ι-carrageenan and calcium lactate gluconate. The paracetamol instant jelly characteristics, in terms of physical appearance, texture, rheology, in vitro drug release and palatability were assessed on a human volunteer.

    RESULTS: The paracetamol instant jelly was easily reconstituted in 20 mL of water within 2 min to form jelly with acceptable consistency and texture. The jelly must be ingested within 30 min after reconstitution to avoid the bitter taste. The palatability assessment carried out on 12 human subjects established the similar palatability and texture of the paracetamol instant jelly dosage comparable to the commercial paracetamol suspension and was found to be even better in overcoming the aftertaste of paracetamol.

    CONCLUSION: Such findings indicate that paracetamol instant jelly will compensate for the use of sweetening and flavoring agents as well as develop pediatric dosage forms with limited undesired excipients.

    Matched MeSH terms: Drug Liberation
  16. Sreeharsha N, Prasanthi S, Mahalakshmi SVVNS, Goudanavar PS, Naveen NR, Gowthami B, et al.
    Molecules, 2022 Nov 16;27(22).
    PMID: 36432014 DOI: 10.3390/molecules27227914
    A brand-new nano-crystal (NC) version of the hydrophobic drug Paclitaxel (PT) were formulated for cancer treatment. A stable NC formulation for the administration of PT was created using the triblock co-polymer Pluronic F127. To achieve maximum entrapment effectiveness and minimal particle size, the formulation was improved using the central composite design by considering agitation speed and vacuum pressure at five levels (coded as +1.414, +1, 0, -1, and -1.414). According to the Design Expert software's predictions, 13 runs were created and evaluated for the chosen responses. The formulation prepared with an agitation speed of 1260 RPM and a vacuum pressure of 77.53 mbar can meet the requirements of the ideal formulation in order to achieve 142.56 nm of PS and 75.18% EE, according to the level of desirability (D = 0.959). Folic acid was conjugated to Pluronic F127 to create folate receptor-targeted NC. The drug release profile of the nano-crystals in vitro demonstrated sustained release over an extended period. Folate receptor (FR)-targeted NC (O-PT-NC-Folate) has also been prepared by conjugating folic acid to Pluronic F127. MTT test is used to validate the targeting efficacy on the FR-positive human oral cancer cell line (KB). At pharmacologically relevant concentrations, the PT nano-crystal formulation did not cause hemolysis. Compared to non-targeted NC of PT, the O-PT-NC-Folate showed a comparable but more sustained anti-cancer effect, according to an in vivo anti-tumor investigation in NCI/ADR-RES cell lines. The remarkable anti-tumor effectiveness, minimal toxicity, and simplicity of scale-up manufacturing of the NC formulations indicate their potential for clinical development. Other hydrophobic medications that are formulated into nano-systems for improved therapy may benefit from the formulation approach.
    Matched MeSH terms: Drug Liberation
  17. 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
  18. Veronica N, Lee ESM, Heng PWS, Liew CV
    Int J Pharm, 2024 Aug 15;661:124467.
    PMID: 39004293 DOI: 10.1016/j.ijpharm.2024.124467
    Tablet disintegration is crucial for drug release and subsequent systemic absorption. Although factors affecting the disintegrant's functionality have been extensively studied, the impact of wet granulation on the performance of disintegrants in a poorly water-soluble matrix has received much less attention. In this study, the disintegrants, crospovidone (XPVP), croscarmellose sodium (CCS) and sodium starch glycolate (SSG), were wet-granulated with dibasic calcium phosphate dihydrate as the poorly water-soluble matrix and polyvinylpyrrolidone as the binder. The effect of wet granulation was studied by evaluating tablet tensile strength and disintegratability. Comparison between tablets with granulated or ungranulated disintegrants as well those without disintegrants were also made. Different formulations showed different degrees of sensitivity to changes in tablet tensile strength and disintegratability post-wet granulation. Tablet tensile strength decreased for tablets with granulated disintegrant XPVP or CCS, but to a smaller extent for SSG. While tablets with granulated XPVP or CCS had increased disintegration time, the increment was lesser than for SSG, suggesting that wet granulation impacted a swelling disintegrant more. The findings showed that tablets with wet-granulated disintegrant had altered the disintegrant's functionality. These findings could provide better insights into changes in the disintegrant's functionality after wet granulation.
    Matched MeSH terms: Drug Liberation
  19. Mulenga G, Alahmed TAA, Sami F, Majeed S, Ali MS, Le JLJ, et al.
    AAPS PharmSciTech, 2024 Jun 11;25(5):134.
    PMID: 38862663 DOI: 10.1208/s12249-024-02845-3
    Inclusion complexes require higher concentration of Beta cyclodextrins (βCD) resulting in increased formulation bulk, toxicity, and production costs. This systematic review offers a comprehensive analysis using Quality by design (QbD) as a tool to predict potential applications of Polyvinylpyrrolidone (PVP) as a ternary substance to address issues of inclusion complexes. We reviewed 623 documents from 2013 to 2023 and Eighteen (18) research papers were selected for statistical and meta-analysis using the QbD concept to identify the most critical factors for selecting drugs and effect of PVP on inclusion complexes. The QbD analysis revealed that Molecular weight (MW), Partition coefficient (Log P), and the auxiliary substance ratio directly affected complexation efficiency (CE), thermodynamic stability in terms of Gibbs free energy (ΔG), and percent drug release. However, Stability constant (Ks) remained unaffected by any of these parameters. The results showed that low MW (250), median Log P (6), and a βCD: PVP ratio of 2:3 would result in higher CE, lower G, and improved drug release. PVP improves drug solubility, enhances delivery and therapeutic outcomes, and counteracts increased drug ionization due to decreased pH. In certain cases, its bulky nature and hydrogen bonding with CD molecules can form non-inclusion complexes. The findings of the study shows that there is potential molecular interaction between PVP and β-cyclodextrins, which possibly enhances the stability of inclusion complexes for drug with low MW and log P values less than 9. The systematic review shows a comprehensive methodology based on QbD offers a replicable template for future investigations into drug formulation research.
    Matched MeSH terms: Drug Liberation
  20. 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*
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