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Journal ArticleDOI: 10.1080/03639045.2021.1892738

Synthesis of PEG-4000-co-poly (AMPS) nanogels by cross-linking polymerization as highly responsive networks for enhancement in meloxicam solubility.

02 Mar 2021-Drug Development and Industrial Pharmacy (Taylor & Francis)-Vol. 47, Iss: 3, pp 465-476
Abstract: Poor solubility is an ongoing issue and the graph of poorly soluble drugs has increased markedly which critically affect their dissolution, bioavailability, and clinical effects. This common issue ...

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Topics: Solubility (53%)
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9 results found


Open accessJournal ArticleDOI: 10.3390/GELS7020068
09 Jun 2021-Gels
Abstract: Different combinations of polymers, aspartic acid (ASP), alginic acid (AL), and monomer acrylic acid (AA) were crosslinked in the presence of an initiator ammonium peroxodisulfate (APS) and cross-linker ethylene glycol dimethacrylate (EGDMA) to develop aspartic acid/alginic acid-co-poly(acrylic acid) (ASP/ALPAA) (semi-interpenetrating polymer network (SIPN)) hydrogels by the free radical polymerization technique for the controlled delivery of ibuprofen (IBP). Various studies such as dynamic swelling studies, drug loading, in vitro drug release and sol−gel analysis were carried out for the hydrogels. Higher swelling was observed at higher pH 7.4 as compared to lower pH 1.2, due to the presence of carboxylic groups of polymers and the monomer. Hence, pH-dependent swelling was exhibited by the developed hydrogels which led to a pH-dependent drug release and vice versa. The structural properties of the hydrogels were assessed by FTIR, PXRD, TGA, DSC, and SEM which confirmed the fabrication and stability of the developed structure. FTIR analysis revealed the reaction of both polymers with the monomer during the polymerization process and confirmed the overlapping of the monomer on the backbone of the both polymers. The disappearance of high intense crystalline peaks and the encapsulation of the drug by the hydrogel network was confirmed by PXRD. TGA and DSC showed that the developed hydrogels were thermally more stable than their basic ingredients. Similarly, the surface morphology of the hydrogels was analyzed by SEM and showed a smooth surface with few pores. Conclusively, ASP/ALPAA hydrogels have the potential to deliver IBP for a long period of time in a controlled way.

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Topics: Self-healing hydrogels (61%), Radical polymerization (55%), Acrylic acid (54%) ... show more

4 Citations


Open accessJournal ArticleDOI: 10.3390/GELS7030110
05 Aug 2021-Gels
Abstract: The purpose of the current investigation was to develop chondroitin sulfate/carbopol-co-poly(acrylic acid) (CS/CBP-co-PAA) hydrogels for controlled delivery of diclofenac sodium (DS). Different concentrations of polymers chondroitin sulfate (CS), carbopol 934 (CBP), and monomer acrylic acid (AA) were cross-linked by ethylene glycol dimethylacrylate (EGDMA) in the presence of ammonium peroxodisulfate (APS) (initiator). The fabricated hydrogels were characterized for further experiments. Characterizations such as Scanning electron microscopy (SEM), Thermogravimetric analysis (TGA), Differential scanning calorimetry (DSC), Powder X-ray diffractometry (PXRD), and Fourier transform infrared spectroscopy (FTIR) were conducted to understand the surface morphology, thermodynamic stability, crystallinity of the drug, ingredients, and developed hydrogels. The swelling and drug release studies were conducted at two different pH mediums (pH 1.2 and 7.4), and pH-dependent swelling and drug release was shown due to the presence of functional groups of both polymers and monomers; hence, greater swelling and drug release was observed at the higher pH (pH 7.4). The percent drug release of the developed system and commercially available product cataflam was compared and high controlled release of the drug from the developed system was observed at both low and high pH. The mechanism of drug release from the hydrogels followed Korsmeyer–Peppas model. Conclusively, the current research work demonstrated that the prepared hydrogel could be considered as a suitable candidate for controlled delivery of diclofenac sodium.

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2 Citations


Journal ArticleDOI: 10.1208/S12249-021-02054-2
15 Jun 2021-Aaps Pharmscitech
Abstract: In this study, two hydrophilic polymers hydroxypropyl methyl cellulose and beta-cyclodextrin (β-CD) are used to synthesize highly responsive and spongy polymeric matrices. Porous and stimulus-responsive polymeric network was developed to improve the solubility of acyclovir (ACV) at significant level. Grafting was successfully carried out by free radical polymerization technique. Spongy matrices were characterized by percentage entrapment efficiency, drug loading, solubility studies, FTIR, powder X-ray diffraction, TGA, DSC, XRD, SEM, swelling studies, and in vitro studies. Acute oral toxicity studies were conducted to determine the safety of oral administration of prepared HPMC-βCD-g-poly(AMPS) formulation. Porous and spongy structures were depicted in SEM images. Complex formation and thermal stability of constituents and drug (ACV) were analyzed by FTIR, TGA, and DSC spectra. XRD analysis revealed reduction in acyclovir crystallinity in spongy matrices. Particle size of optimized formulation was found in the range of 197 ± 2.55 nm. The momentous difference with reference product committed that drug solubility and release characteristics were markedly enhanced by the developed spongy matrices. Toxicity studies endorsed that developed spongy matrices were non-toxic and compatible to biological system. The efficient method of preparation, enhanced solubility, excellent physico-chemical characteristics, high dissolution, and non-toxic HPMC-βCD-g-poly(AMPS) spongy matrices may be a promising approach for oral delivery of poorly soluble drugs.

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Topics: Solubility (52%)

1 Citations


Journal ArticleDOI: 10.1080/25740881.2021.1934019
Sana Tanveer1, Mahmood Ahmad1, Muhammad Usman Minhas2, Aousaf Ahmad1  +1 moreInstitutions (2)
15 Jun 2021-
Abstract: Current study aimed to develop and evaluate interpenetrating polymer network (IPN) nanogels for transdermal delivery of ondansetron (OND) using combination of natural and synthetic polymers. Owing ...

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Open accessJournal ArticleDOI: 10.1016/J.JDDST.2021.102952
Abstract: Herein, we report highly porous and amorphous nanomatrices developed by cross-linking polymerization with subsequent condensation technique for solubility, dissolution and ultimately bioavailability enhancement of poorly soluble drug olanzapine (OLN). β-cyclodextrin was chemically cross-linked with monomer 2-acrylamido 2-methylpropane sulfonic acid (AMPS) by using methylene bis acrylamide (MBA) as cross-linking agent. Developed nanomatrices were characterized by zetasizer, FTIR, XRD, SEM, DSC, swelling, sol-gel, drug loading, stability, porosity (%), solubility, and in-vitro dissolution analysis. The developed porous nanomatrices are intended for oral administration of poorly soluble drugs therefore, to determine the biocompatibility of the system to the biological environment, in-vivo cytotoxicity study was also conducted using rabbit model which endorsed the safety of the nanomatrices with biological system. The particle size of nanomatrices were found 152.30 ± 07.46 d.nm. XRD analysis depicted the highly amorphous nature of nanomatrices while. To evaluate the pharmacokinetic profile of olanzapine, in-vivo studies were also conducted. The in-vivo and dissolution experiments revealed that drug release characteristics were significantly improved by nanomatrices as compared with the reference product (OLANZIA®). The solubility of olanzapine by the developed nanomatrices was enhanced noticeably up to 40.11 times which is higher than previously reported β-cyclodextrin formulations. The efficient method of preparation, improved solubility, rapid and high dissolution and non-toxic βCD-co-poly (AMPS) nanomatrices may be a promising approach for oral delivery of poorly soluble drugs.

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Topics: Solubility (50%)

References
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68 results found


Journal ArticleDOI: 10.1016/S0169-409X(00)00129-0
Abstract: Experimental and computational approaches to estimate solubility and permeability in discovery and development settings are described In the discovery setting 'the rule of 5' predicts that poor absorption or permeation is more likely when there are more than 5 H-bond donors, 10 H-bond acceptors, the molecular weight (MWT) is greater than 500 and the calculated Log P (CLogP) is greater than 5 (or MlogP > 415) Computational methodology for the rule-based Moriguchi Log P (MLogP) calculation is described Turbidimetric solubility measurement is described and applied to known drugs High throughput screening (HTS) leads tend to have higher MWT and Log P and lower turbidimetric solubility than leads in the pre-HTS era In the development setting, solubility calculations focus on exact value prediction and are difficult because of polymorphism Recent work on linear free energy relationships and Log P approaches are critically reviewed Useful predictions are possible in closely related analog series when coupled with experimental thermodynamic solubility measurements

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12,161 Citations


Journal ArticleDOI: 10.1023/A:1007516718048
Bruno C. Hancock1, Michael Parks2Institutions (2)
Abstract: Purpose To evaluate the magnitude of the solubility advantage foramorphous pharmaceutical materials when compared to their crystallinecounterpartsMethods The thermal properties of several drugs in their amorphousand crystalline states were determined using differential scanningcalorimetry From these properties the solubility advantage for theamorphous form was predicted as a function of temperature using a simplethermodynamic analysis These predictions were compared to theresults of experimental measurements of the aqueous solubilities of theamorphous and crystalline forms of the drugs at several temperaturesResults By treating each amorphous drug as either an equilibriumsupercooled liquid or a pseudo-equilibrium glass, the solubilityadvantage compared to the most stable crystalline form was predicted to bebetween 10 and 1600 fold The measured solubility advantage wasusually considerably less than this, and for one compound studied indetail its temperature dependence was also less than predicted It wascalculated that even for partially amorphous materials the apparentsolubility enhancement (theoretical or measured) is likely to influencein-vitro and in-vivo dissolution behaviorConclusions Amorphous pharmaceuticals are markedly more solublethan their crystalline counterparts, however, their experimental solubility advantage is typically less than that predicted from simplethermodynamic considerations This appears to be the result of difficulties indetermining the solubility of amorphous materials under trueequilibrium conditions Simple thermodynamic predictions can provide a useful indication of the theoretical maximum solubility advantage foramorphous pharmaceuticals, which directly reflects the driving forcefor their initial dissolution

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Topics: Solubility (58%), Dissolution (53%), Amorphous solid (53%)

1,227 Citations


Open accessJournal ArticleDOI: 10.1016/J.AJPS.2014.08.005
Abstract: Nanocrystals, a carrier-free colloidal delivery system in nano-sized range, is an interesting approach for poorly soluble drugs. Nanocrystals provide special features including enhancement of saturation solubility, dissolution velocity and adhesiveness to surface/cell membranes. Several strategies are applied for nanocrystals production including precipi- tation, milling, high pressure homogenization and combination methods such as Nano- Edge™, SmartCrystal and Precipitation-lyophilization-homogenization (PLH) technology. For oral administration, many publications reported useful advantages of nanocrystals to improve in vivo performances i.e. pharmacokinetics, pharmacodynamics, safety and tar- geted delivery which were discussed in this review. Additionally, transformation of nanocrystals to final formulations and future trends of nanocrystals were also described. © 2015 Shenyang Pharmaceutical University. Production and hosting by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/ licenses/by-nc-nd/4.0/).

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252 Citations


Journal ArticleDOI: 10.1016/J.BIOMATERIALS.2006.11.008
Lichen Yin1, Likun Fei1, Fuying Cui1, Cui Tang1  +1 moreInstitutions (1)
01 Feb 2007-Biomaterials
Abstract: Superporous hydrogels containing poly(acrylic acid-co-acrylamide)/O-carboxymethyl chitosan interpenetrating polymer networks (SPH-IPNs) were prepared by cross-linking O-carboxymethyl chitosan (O-CMC) with glutaraldehyde (GA) after superporous hydrogel (SPH) was synthesized. The structures of the SPH-IPNs were characterized with FT-IR, 13C-NMR and DSC. SEM, CLSM and light images revealed that the SPH-IPNs possessed both the IPN network and large numbers of pores and the cross-linked O-CMC molecules were located on the peripheries of these pores. The swelling behavior of SPH-IPNs was dependent on the O-CMC content, GA amount and cross-linking time. Due to the cross-linked O-CMC network, in vitro muco-adhesive force and mechanical properties, including compression and tensile modulus, of the SPH-IPN were greatly improved when compared with the CSPH. An enhanced loading capacity for insulin could be obtained by the SPH-IPNs as compared to non-porous hydrogel and CSPH, and more than 90% of the insulin was released within 1 h. With the improved mechanical properties, in vitro muco-adhesive force and loading capacities, the SPH-IPN may be used as a potential muco-adhesive system for peroral delivery of peptide and protein drugs.

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Topics: Self-healing hydrogels (59%), Chitosan (50%)

235 Citations


Journal ArticleDOI: 10.1016/J.IJPHARM.2004.09.007
Abstract: In this first of two articles, we discuss some issues surrounding the dissolution rate enhancement of poorly-soluble active ingredients micronized into nano-particles using several supercritical fluid particle design processes including rapid expansion of supercritical solutions (RESS), supercritical anti-solvent (SAS) and particles from gas-saturated solutions/suspensions (PGSS). Experimental results confirm that dissolution rates do not only depend on the surface area and particle size of the processed powder, but are greatly affected by other physico-chemical characteristics such as crystal morphology and wettability that may reduce the benefit of micronization.

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Topics: Supercritical fluid (62%), Micronization (62%), Particle size (52%) ... show more

206 Citations