scholarly journals Nanoencapsulation of Nimodipine in Novel Biocompatible Poly(propylene-co-butylene succinate) Aliphatic Copolyesters for Sustained Release

2009 ◽  
Vol 2009 ◽  
pp. 1-11 ◽  
Author(s):  
Sofia Papadimitriou ◽  
George Z. Papageorgiou ◽  
Feras I. Kanaze ◽  
Manolis Georgarakis ◽  
Dimitrios N. Bikiaris
Keyword(s):  
Chemical Interaction ◽  
Spherical Shape ◽  
Water Soluble ◽  
Degree Of Crystallinity ◽  
Butylene Succinate ◽  
Melt Polycondensation ◽  
Water Soluble Drug ◽  
The Matrix ◽  
Model Drug ◽  
Poly Propylene

Biocompatible poly(propylene-co-butylene succinate) (PPBSu) copolyesters, containing up to 50 mol% butylene succinate units, were synthesized by the two-stage melt polycondensation method (esterification and polycondensation). The copolymers were fully characterized and biocompatibility studies were also performed. They were proved to be biocompatible and they were used as polymer matrices for the preparation of drug loaded nanoparticles. Nimodipine was selected as a model hydrophobic poorly water soluble drug. From the results obtained by dynamic light scattering (DLS) and scanning electron microscopy (SEM), drug loaded copolymer nanoparticles were found to exhibit a spherical shape and their mean diameter appeared in the range of 180–200 nm. Fourier Transformation-Infrared Spectroscopy (FTIR) spectra indicated that no chemical interaction between the drug and the matrix could be justified, while Wide-Angle X-Ray Diffraction (WAXD) patterns proved a low degree of crystallinity of Nimodipine in the nanoparticles. The release behavior of the model drug from nanoparticles was also investigated in order to identify modifications and find out any possible correlation between the chemical composition of the polymer matrix and the drug release rates.

Controlled Release of Resveratrol and Lignan by Matrix Tableting

2013 ◽  
Vol 746 ◽  
pp. 330-336
Author(s):  
Mont Kumpugdee-Vollrath ◽  
Mario Helmis
Keyword(s):  
Controlled Release ◽  
Release Kinetics ◽  
Research Work ◽  
Magnesium Stearate ◽  
Water Soluble ◽  
Matrix Tablets ◽  
Water Soluble Drug ◽  
The Matrix ◽  
Best Fitting ◽  
Model Drug

The aim of this research work was to develop the controlled release of two model drugs i.e. water insoluble drug - resveratrol and water soluble drug - lignan by matrix tableting with an eccentric tablet machine. For this purpose different kinds of polymers i.e. Metolose 90 SH-4000® (HMPC), Fetocel RT-N-100® (EC) and Eudragit RLPO® (polymethacrylate) were used. The matrix tablets containing 2 %wt of a model drug which were mixed with 5, 10, 20, 30 and 50 %wt of the polymers mentioned above. In addition, a glidant composed of 1 %wt talc and 1 %wt magnesium stearate as well as a filler Ludipress® were processed. Different physical properties of the powder mixtures (e.g. flowability) and of the tablets (e.g. hardness, uniformity of mass or drug content, drug release, etc.) were determined. Most of the tablets met the physical requirements. If the polymer content got higher the release was slower, which can be confirmed by the lower values of k. The release kinetics were described by three typical mathematic models i.e. biphasic, Noyes-Whitney and KorsmeyerPeppas. The best fitting results were ordered as follows: biphasic > Noyes-Witney > KorsmeyerPeppas.

scholarly journals Novel Biodegradable Polyester Poly(Propylene Succinate): Synthesis and Application in the Preparation of Solid Dispersions and Nanoparticles of a Water-Soluble Drug

2009 ◽  
Vol 10 (1) ◽  
pp. 138-146 ◽  
Author(s):  
Dimitrios N. Bikiaris ◽  
George Z. Papageorgiou ◽  
Sofia A. Papadimitriou ◽  
Evangelos Karavas ◽  
Konstantinos Avgoustakis
Keyword(s):  
Solid Dispersions ◽  
Water Soluble ◽  
Biodegradable Polyester ◽  
Water Soluble Drug ◽  
Poly Propylene

scholarly journals Biobased Engineering Thermoplastics: Poly(butylene 2,5-furandicarboxylate) Blends

Polymers ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 937 ◽  
Author(s):  
Niki Poulopoulou ◽  
George Kantoutsis ◽  
Dimitrios N. Bikiaris ◽  
Dimitris S. Achilias ◽  
Maria Kapnisti ◽  
...  
Keyword(s):  
Renewable Resources ◽  
Degree Of Crystallinity ◽  
X Ray Diffraction ◽  
Reactive Blending ◽  
Scanning Calorimetry ◽  
Melt Polycondensation ◽  
Poly Ethylene Terephthalate ◽  
Furandicarboxylic Acid ◽  
Poly Ethylene ◽  
Poly Propylene

Poly(butylene 2,5-furandicarboxylate) (PBF) constitutes a new engineering polyester produced from renewable resources, as it is synthesized from 2,5-furandicarboxylic acid (2,5-FDCA) and 1,4-butanediol (1,4-BD), both formed from sugars coming from biomass. In this research, initially high-molecular-weight PBF was synthesized by applying the melt polycondensation method and using the dimethylester of FDCA as the monomer. Furthermore, five different series of PBF blends were prepared, namely poly(l-lactic acid)–poly(butylene 2,5-furandicarboxylate) (PLA–PBF), poly(ethylene terephthalate)–poly(butylene 2,5-furandicarboxylate) (PET–PBF), poly(propylene terephthalate)–poly(butylene 2,5-furandicarboxylate) (PPT–PBF), poly(butylene 2,6-naphthalenedicarboxylate)-poly(butylene 2,5-furandicarboxylate) (PBN–PBF), and polycarbonate–poly(butylene 2,5-furandicarboxylate) (PC–PBF), by dissolving the polyesters in a trifluoroacetic acid/chloroform mixture (1/4 v/v) followed by coprecipitation as a result of adding the solutions into excess of cold methanol. The wide-angle X-ray diffraction (WAXD) patterns of the as-prepared blends showed that mixtures of crystals of the blend components were formed, except for PC which did not crystallize. In general, a lower degree of crystallinity was observed at intermediate compositions. The differential scanning calorimetry (DSC) heating scans for the melt-quenched samples proved homogeneity in the case of PET–PBF blends. In the remaining cases, the blend components showed distinct Tgs. In PPT–PBF blends, there was a shift of the Tgs to intermediate values, showing some partial miscibility. Reactive blending proved to improve compatibility of the PBN–PBF blends.

scholarly journals Novel application of mixed solvency concept in the development of oral liquisolid system of a poorly soluble drug, cefixime and its evaluation

2018 ◽  
Vol 8 (6-s) ◽  
pp. 5-8 ◽  
Author(s):  
Rinshi Agrawal ◽  
RK Maheshwari
Keyword(s):  
Drug Loading ◽  
Research Work ◽  
Water Soluble ◽  
Dsc Studies ◽  
Water Soluble Drug ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
Poorly Soluble Drug ◽  
Model Drug ◽  
Poorly Water Soluble Drug

Application of mixed solvency has been employed in the present research work to develop a liquisolid system (Powder formulation) of poorly water soluble drug, cefixime (as model drug). Material and Methods: For poorly water soluble drug cefixime, combination of solubilizers such as sodium acetate, sodium caprylate and propylene glycol as mixed solvent systems were used to decrease the overall concentration of solubilizers required to produce substantial increase in solubility and thereby resulting in enhanced drug loading capacity of cefixime. The procured sample of cefixime was characterized by melting point, IR, UV and DSC studies. Stability studies of liquisolid system of cefixime were performed for two months at room temperature, 30˚C and 40˚C. All the formulations were physically, chemically, and microbiologically stable. Conclusion: Mixed solvency concept has been successfully employed for enhancing the drug loading of poorly water soluble drug, cefixime. Keywords: Solubility, cefixime, liquisolid system, mixed solvency concept.

scholarly journals The Effect of Drug Heterogeneous Distributions within Core-Sheath Nanostructures on Its Sustained Release Profiles

Biomolecules ◽  
2021 ◽  
Vol 11 (9) ◽  
pp. 1330 ◽  
Author(s):  
Haixia Xu ◽  
Xizi Xu ◽  
Siyu Li ◽  
Wen-Liang Song ◽  
Deng-Guang Yu ◽  
...  
Keyword(s):  
Sustained Release ◽  
Extended Release ◽  
Water Soluble ◽  
Metformin Hydrochloride ◽  
The Core ◽  
Water Soluble Drug ◽  
Time Period ◽  
Drug Sustained Release ◽  
Water Soluble Drugs ◽  
Model Drug

The sustained release of a water-soluble drug is always a key and important issue in pharmaceutics. In this study, using cellulose acetate (CA) as a biomacromolecular matrix, core-sheath nanofibers were developed for providing a sustained release of a model drug—metformin hydrochloride (MET). The core–sheath nanofibers were fabricated using modified tri-axial electrospinning, in which a detachable homemade spinneret was explored. A process—nanostructure–performance relationship was demonstrated through a series of characterizations. The prepared nanofibers F2 could release 95% of the loaded MET through a time period of 23.4 h and had no initial burst effect. The successful sustained release performances of MET can be attributed to the following factors: (1) the reasonable application of insoluble CA as the filament-forming carrier, which determined that the drug was released through a diffusion manner; (2) the core–sheath nanostructure provided the possibility of both encapsulating the drug completely and realizing the heterogeneous distributions of MET in the nanofibers with a higher drug load core than the sheath; (3) the thickness of the sheath sections were able to be exploited for further manipulating a better drug extended release performance. The mechanisms for manipulating the drug sustained release behaviors are proposed. The present proof-of-concept protocols can pave a new way to develop many novel biomolecule-based nanostructures for extending the release of water-soluble drugs.

scholarly journals Solubility Enhancement of Ibuprofen by Adsorption onto Spherical Porous Calcium Silicate

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 767
Author(s):  
Yayoi Kawano ◽  
Shiyang Chen ◽  
Takehisa Hanawa
Keyword(s):  
Calcium Silicate ◽  
Spherical Shape ◽  
Water Soluble ◽  
Dissolution Behavior ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Dsc Measurements ◽  
Water Soluble Drug ◽  
Main Component ◽  
Poorly Water Soluble Drug

The solubility of a drug is higher when it is in an amorphous form than when it is in a crystalline form. To enhance the solubility of ibuprofen (IBU), a poorly water-soluble drug, we attempted to adsorb IBU onto spherical porous calcium silicate (Florite® PS300, PS300) in two ways: the evaporation (EV) and sealed heating (SH) methods. The crystallinity of the samples was evaluated using powder X-ray diffraction analysis (PXRD) and differential scanning calorimetry (DSC). The molecular interaction between IBU and PS300 was evaluated with FTIR. In addition, the dissolution behavior of IBU in the samples was assessed by the dissolution test. Based on the results of the PXRD and DSC measurements, both methods allowed adsorption of IBU onto PS300, and IBU was amorphized. Based on the FTIR observations, in the SH or EV mixtures containing 10% and 30% IBU, respectively, it seemed that the IBU molecules intermolecularly interacted with calcium molecules as the main component of PS300. Improvement in the solubility of IBU was observed with both methods; however, the dissolution rate of IBU from samples prepared via SH was higher than that from EV, or of IBU crystals. Collectively, our findings indicate that the petal-like structure of PS300, which has a spherical shape and good flowability, is an effective tool for adsorbing IBU onto PS300 via SH.

scholarly journals Formulating a poorly water soluble drug into an oral solution suitable for paediatric patients; lorazepam as a model drug

2017 ◽  
Vol 100 ◽  
pp. 205-210 ◽  
Author(s):  
A.C. van der Vossen ◽  
I. van der Velde ◽  
O.S.N.M. Smeets ◽  
D.J. Postma ◽  
M. Eckhardt ◽  
...  
Keyword(s):  
Oral Solution ◽  
Water Soluble ◽  
Paediatric Patients ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Model Drug ◽  
Poorly Water Soluble Drug

Ionically cross-linked chitosan–halloysite composite microparticles for sustained drug release

Clay Minerals ◽  
2017 ◽  
Vol 52 (4) ◽  
pp. 413-426 ◽  
Author(s):  
Bojan Čalija ◽  
Jela Milić ◽  
Jelena Janićijević ◽  
Aleksandra Daković ◽  
Danina Krajišnik
Keyword(s):  
Drug Release ◽  
Ftir Spectroscopy ◽  
Encapsulation Efficiency ◽  
Spherical Shape ◽  
Halloysite Nanotubes ◽  
Water Soluble ◽  
Composite Particles ◽  
Sustained Drug Release ◽  
Model Drug ◽  
Dta And Tg

AbstractThis study investigated the potential of halloysite nanotubes (HNTs) to improve the sustained release properties of chitosan (CS) microparticles cross-linked ionically with tripolyphosphate (TPP). Composite CS-HNTs microparticles were obtained by a simple and eco-friendly procedure based on a coaxial extrusion technique. Prior to encapsulation, a water-soluble model drug, verapamil hydrochloride (VH), was adsorbed successfully on HNTs. The microparticles were characterized by optical microscopy, Fourier transform infrared (FTIR) spectroscopy, differential thermal analysis/ thermogravimetric analysis (DTA/TG) and evaluated for encapsulation efficiency and drug-release properties. The composite particles had a slightly deformed spherical shape and micrometric size with average perimeters ranging from 485.4 ± 13.3 to 492.4 ± 11.9 μm. The results of FTIR spectroscopy confirmed non-covalent interactions between CS and HNTs within composite particle structures. The DTA and TG studies revealed increased thermal stability of the composite particles in comparison to the CS-TPP particles. Drug adsorption on HNTs prior to encapsulation led to an increase in encapsulation efficiency from 19.6 ± 2.9 to 84.3 ± 1.9%. In contrast to the rapid release of encapsulated model drug from CS-TPP microparticles, the composite CS-HNTs microparticles released drug in a sustained manner, showing the best fit to the Bhaskar model. The results presented here imply that HNTs could be used to improve morphology, encapsulation efficiency and sustained drug-release properties of CS microparticles cross-linked ionically with TPP.

scholarly journals Microneedle-Assisted Percutaneous Delivery of Paeoniflorin-Loaded Ethosomes

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3371 ◽  
Author(s):  
Yahua Cui ◽  
Yujia Mo ◽  
Qi Zhang ◽  
Wanwan Tian ◽  
Yutao Xue ◽  
...  
Keyword(s):  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Topical Administration ◽  
Water Soluble ◽  
Orthogonal Experimental Design ◽  
Therapeutic Effects ◽  
Transdermal Drug Delivery System ◽  
Water Soluble Drug ◽  
Transmission Electron ◽  
Main Component

Paeoniflorin, the main component of total glucosides of paeony (TGP), shows good therapeutic effects in arthritis, but has low bioavailability when administered orally. Avoiding such a deficiency for topical administration would expand its clinical application. This study aimed to avoid these limitations by using nanotechnology (ethosomes) and a physical approach (microneedles). Paeoniflorin-loaded ethosomal formulation (TGP-E) was optimized and evaluated in terms of entrapment efficiency (EE), particle size (PS), zeta potential (ZP), polydispersity index (PDI) and morphology. TGP-E was prepared by the hot injection method and optimized by single-factor tests and an orthogonal experimental design. The optimized paeoniflorin-loaded ethosomes had EE of 27.82 ± 1.56%, PS of 137.9 ± 7.57 nm with PDI of 0.120 ± 0.005, ZP of −0.74 ± 0.43 mV. Ethosomes showed a nearly spherical shape under the transmission electron microscope (TEM). The optimal microneedle-assisted (MN-assisted) conditions were obtained at a microneedle length of 500 μm, a pressure of 3 N and an action time of 3 min. The cumulative penetration amounts (Qn) of TGP solution transdermal (ST) and MN-assisted TGP solution transdermal (MST) were 24.42 ± 8.35 μg/cm2 and 548.11 ± 10.49 μg/cm2, respectively. Qn of TGP-E transdermal (PT) and MN-assisted TGP-E transdermal (MPT) were 54.97 ± 4.72 μg/cm2 and 307.17 ± 26.36 μg/cm2, respectively. These findings indicate that use of ethosomes and microneedles can both enhance the penetration ofpaeoniflorin, but for the water-soluble drug, there is no obvious synergism between nanotechnology and microneedles for enhancing penetration in a transdermal drug delivery system.

scholarly journals SOLUBILITY AND DISSOLUTION ENHANCEMENT OF PIOGLITAZONE USING SOLID DISPERSION TECHNIQUE

2017 ◽  
pp. 186-193
Author(s):  
Bhushan A. Bhairav ◽  
Lalit R. Jagtap ◽  
R. B. Saudagar
Keyword(s):  
Solid Dispersion ◽  
Chemical Interaction ◽  
Physicochemical Characteristics ◽  
Water Soluble ◽  
Dissolution Enhancement ◽  
Hydrophobic Drug ◽  
Water Soluble Drug ◽  
Poorly Water Soluble ◽  
Dispersion Technique ◽  
Poorly Water Soluble Drug

Objective: To design the study to improve the solubility and hence enhance the dissolution of hydrophobic drug Pioglitazone in order to increase its bioavailability.Methods: Solid dispersion of Pioglitazone using carriers Poloxomer 188 and HPβCD was formulated in different ratios by microwave induced fusion method. In particular, the Microwave technology has been considered in order to prepare an enhanced release dosage form for poorly water soluble drug Pioglitazone. Statistical Analysis: Their physicochemical characteristics and solubility were compared to the corresponding dispersions and marketed drug. Drug and polymer were further characterized by FTIR.Results: The results of FTIR revealed that no chemical interaction between the drug and the polymer exist.Conclusion: All the formulations showed a marked increase in drug release with the increase in the concentration of Poloxomer 188 and HPβCD. 

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