scholarly journals Enhanced Nanoencapsulation of Sepiapterin within PEG-PCL Nanoparticles by Complexation with Triacetyl-Beta Cyclodextrin

Molecules ◽  
2019 ◽  
Vol 24 (15) ◽  
pp. 2715 ◽  
Author(s):  
Nataliya Kuplennik ◽  
Alejandro Sosnik
Keyword(s):  
Spray Drying ◽  
Encapsulation Efficiency ◽  
Water Solubility ◽  
Hydrophobic Interactions ◽  
Drug Loading ◽  
Weight Ratio ◽  
Sem Analysis ◽  
Molar Ratio ◽  
Scanning Calorimetry ◽  
Dry Powders

In this work, we aimed to improve the encapsulation efficiency of sepiapterin (SP), the natural precursor of the essential cofactor tetrahydrobiopterin (BH4) that displays mild water-solubility and a short biological half-life, within methoxy-poly(ethylene-glycol)-poly(epsilon-caprolactone)(mPEG-PCL) nanoparticles (NPs) by means of its complexation and hydrophobization with 2,3,6-triacetyl-β-cyclodextrin (TAβCD). For this, SP/TAβCD complexes were produced by spray-drying of SP/TAβCD binary solutions in ethanol using the Nano Spray Dryer B-90 HP. Dry powders were characterized by differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), and transmission and scanning electron microscopy (TEM and SEM, respectively) and compared to the pristine components and their physical mixtures (PMs). Next, SP was encapsulated within mPEG-PCL NPs by nano-precipitation of an SP/TAβCD complex/mPEG-PCL solution. In addition to the nano-encapsulation of a preformed complex within the polymeric NPs, we assessed an alternative encapsulation approach called drying with copolymer (DWC) in which pristine SP, TAβCD, and mPEG-PCL were co-dissolved in a mixture of acetone and methanol at the desired weight ratio, dried under vacuum, re-dissolved, and nano-precipitated in water. The dissolution-drying step was aimed to promote the formation of molecular hydrophobic interactions between SP, TAβCD, and the PCL blocks in the copolymer. SP-loaded mPEG-PCL NPs were characterized by dynamic light scattering (DLS) and SEM. NPs with a size of 74–75 nm and standard deviation (S.D., a measure of the peak width) of 21–22 nm were obtained when an SP:TAβCD (1:1 molar ratio) spray-dried complex was used for the nano-encapsulation and SEM analysis revealed the absence of free SP crystals. The encapsulation efficiency (%EE) and drug loading (%DL) were 85% and 2.6%, respectively, as opposed to the much lower values (14% and 0.6%, respectively) achieved with pristine SP. Moreover, the NPs sustained the SP release with relatively low burst effect of 20%. Overall, our results confirmed that spray-drying of SP/TAβCD solutions at the appropriate molar ratio leads to the hydrophobization of the relatively hydrophilic SP molecule, enabling its encapsulation within mPEG-PCL NPs and paves the way for the use of this strategy in the development of novel drug delivery systems of this vital biological precursor.

scholarly journals SPRAY DRYING APPROACH IN PREPARATION AND CHARACTERIZATION OF SOLID DISPERSION OF EPROSARTAN MESYLATE

2021 ◽  
Vol 10 (3) ◽  
pp. 2929-2932
Author(s):  
Sachin N Kothawade
Keyword(s):  
Spray Drying ◽  
Solid Dispersion ◽  
Water Solubility ◽  
Solid Dispersions ◽  
Weight Ratio ◽  
Water Soluble ◽  
Drying Methods ◽  
Scanning Calorimetry ◽  
Dispersion Systems ◽  
Physicochemical Features

Spray drying methods were used to make solid dispersions of the medication Eprosartan Mesylate, which is poorly water-soluble. X-ray Powder diffraction, Fourier transform infrared spectroscopy, and differential scanning calorimetry were used to characterize the products' physicochemical features as well as drug-polymer interactions. Eprosartan Mesylate was shown to be dispersed amorphously in both solid dispersion systems, with a drug to polymer weight ratio of 1:4.The drug and polymer created hydrogen bonds, according to the spectrum data. Both techniques utilized in this investigation enhanced Eprosartan Mesylate solubility. Solid dispersions, on the other hand, performed significantly better, dissolving completely in 5 minutes and at a rate that was about 20 times faster than API within the first 15 minutes. Spray drying is a good way to boost the bioavailability of drugs that are poor water solubility.

scholarly journals EVALUATION OF ORALLY DISINTEGRATING TABLET OF IBUPROFEN-β-CYCLODEXTRIN INCLUSION COMPLEX

2020 ◽  
pp. 60-64
Author(s):  
NUR AINI DEWI PURNAMASARI ◽  
PRATAMA ANGGI SAPUTRA
Keyword(s):  
Inclusion Complex ◽  
Dissolution Rate ◽  
Spray Drying ◽  
Water Solubility ◽  
The Other ◽  
Molar Ratio ◽  
Taste Masking ◽  
Scanning Calorimetry ◽  
Orally Disintegrating Tablet ◽  
Dissolution Efficiency

Objective: This study aims to determine the effect of the inclusion complex formation of ibuprofen (IB) with β-cyclodextrin (β-CD) in improving water solubility and taste masking as well as to study the effect of the combined use of super disintegrants in IB-β-CD ODT (Orally disintegrating tablet). Methods: IB-β-CD inclusion complex was prepared by spray drying technique with a 1:1 molar ratio. ODTs were prepared by the direct compression method using various ratios of Ac-Di-Sol® and Kollidon® CL as super disintegrant. The inclusion complex was characterized using spectroscopy FT-IR (Fourier-transform infrared) and DSC (Differential Scanning Calorimetry). The physical properties and dissolution rate of ODTs were evaluated. Dissolved drug concentration at 60 min (Q60) and Dissolution Efficiency (DE60) was calculated using the dissolution test result. Results: The unpleasant taste of IB had been successfully masked by IB-β-CD. Formula 1 was observed having 14.5 sec of disintegration, fastest compared to the other formulas. Moreover DE60 value of formula I was higher than the other formulas (113.45). Conclusion: IB-β-CD Inclusion complex prepared by spray drying method (1: 1) increased the water solubility and masked the unpleasant taste compared to IB moreover combination of Ac-Di-Sol® and Kollidon® CL increased ODT dissolution rate.

scholarly journals Nanopolyphenols: a review of their encapsulation and anti-diabetic effects

2020 ◽  
Vol 2 (8) ◽  
Author(s):  
Theresa F. Rambaran
Keyword(s):  
Functional Food ◽  
Encapsulation Efficiency ◽  
Water Solubility ◽  
Drug Loading ◽  
Therapeutic Agents ◽  
Low Ph ◽  
Free Form ◽  
Pharmaceutical Development ◽  
Curcumin Nanoparticles ◽  
Treatment Of Diabetes

AbstractPolyphenols are believed to possess numerous health benefits and can be grouped as phenolic acids, flavonoids or non-flavonoids. Research involving the synthesis of nanopolyphenols has attracted interest in the areas of functional food, nutraceutical and pharmaceutical development. This is in an effort to overcome current challenges which limit the application of polyphenols such as their rapid elimination, low water-solubility, instability at low pH, and their particle size. In the synthesis of nanopolyphenols, the type of nanocarrier used, the nanoencapsulation technique employed and the type of polymers that constitute the drug delivery system are crucial. For this review, all mentioned factors which can influence the therapeutic efficacy of nanopolyphenols were assessed. Their efficacy as anti-diabetic agents was also evaluated in 33 publications. Among these were phenolic acid (1), flavonoids (13), non-flavonoids (17) and polyphenol-rich extracts (2). The most researched polyphenols were quercetin and curcumin. Nanoparticles were the main nanocarrier and the size of the nanopolyphenols ranged from 15 to 333 nm with encapsulation efficiency and drug loading capacities of 56–97.7% and 4.2–53.2%, respectively. The quantity of nanomaterial administered orally ranged from 1 to 300 mg/kg/day with study durations of 1–70 days. Most studies compared the effect of the nanopolyphenol to its free-form and, in all but three cases, significantly greater effects of the former were reported. Assessment of the polyphenol to understand its properties and the subsequent synthesis of its nanoencapsulated form using suitable nanocarriers, polymers and encapsulation techniques can result in effective therapeutic agents for the treatment of diabetes.

scholarly journals Optimization and characterization of poly(lactic-co-glycolic acid) nanoparticles loaded with astaxanthin and evaluation of anti-photodamage effect in vitro

2019 ◽  
Vol 6 (10) ◽  
pp. 191184 ◽  
Author(s):  
Fangbin Hu ◽  
Weikang Liu ◽  
Liuliu Yan ◽  
Fanhui Kong ◽  
Kun Wei
Keyword(s):  
Electron Microscopy ◽  
Glycolic Acid ◽  
Water Solubility ◽  
Skin Diseases ◽  
Biological Activities ◽  
Drug Loading ◽  
Synthesis Method ◽  
Hacat Cells ◽  
Scanning Calorimetry

Astaxanthin is a xanthophyll carotenoid with high beneficial biological activities, such as antioxidant function and scavenging oxygen free radicals, but its application is limited because of poor water solubility and low bioavailability. Here, we prepared and optimized poly(lactic-co-glycolic acid) (PLGA) nanoparticles loaded with astaxanthin using the emulsion solvent evaporation technique and investigated the anti-photodamage effect in HaCaT cells. The four-factor three-stage Box–Behnken design was used to optimize the nanoparticle formulation. The experimental determination of the optimal nanoparticle size was 154.4 ± 0.35 nm, the zeta potential was 22.07 ± 0.93 mV, encapsulation efficiency was 96.42 ± 0.73% and drug loading capacity was 7.19 ± 0.12%. The physico-chemical properties of the optimized nanoparticles were characterized by dynamic light scattering, scanning electron microscopy, transmission electron microscopy, Fourier-transform infrared spectroscopy, X-ray diffraction, differential scanning calorimetry and thermo-gravimetric analyser. In vitro study exhibited the excellent cell viability and cellular uptake of optimized nanoparticles on HaCaT cells. The anti-photodamage studies (cytotoxicity assay, reactive oxygen species content and JC-1 assessment) demonstrated that the optimized nanoparticles were more effective and safer than pure astaxanthin in HaCaT cells. These results suggest that our PLGA-coated astaxanthin nanoparticles synthesis method was highly feasible and can be used in cosmetics or the treatment of skin diseases.

scholarly journals Synthesis of thermoplastic poly(ester-olefin) elastomers

2004 ◽  
Vol 58 (10) ◽  
pp. 444-449
Author(s):  
Branka Tanasijevic ◽  
Salem Elkhaseh ◽  
Marija Nikolic ◽  
Jasna Djonlagic
Keyword(s):  
Soft Segment ◽  
Weight Ratio ◽  
Soxhlet Extraction ◽  
Thermoplastic Elastomers ◽  
Molecular Structures ◽  
Degree Of Crystallinity ◽  
Molar Ratio ◽  
Mechanical Spectroscopy ◽  
Scanning Calorimetry ◽  
High Boiling Solvent

A series of thermoplastic poly(ester-olefin) elastomers, based on poly(ethylene-stat-butylene), HO-PEB-OH, as the soft segment and poly (butylene terephthalate), PBT, as the hard segment, were synthesized by a catalyzed transesterification reaction in solution. The incorporation of soft hydrogenated poly(butadiene) segments into the copolyester backbone was accomplished by the polycondensation of ?, ?-dihydroxyl telechelic HO-PEB-OH, (PEB Mn = 3092 g/mol) with 1,4-butanediol (BD) and dimethyl terephthalate (DMT) in the presence of a 50 wt-% high boiling solvent i.e., 1,2,4-trichlorobenzene. The molar ratio of the starting comonomers was selected to result in a constant hard to soft weight ratio of 60:40. The synthesis was optimized in terms of both the concentration of catalyst, tetra-n-butyl-titanate (Ti(OBu)4), and stabilizer, N,N'-diphenyl-p-phenylenediamine (DPPD), as well as the reaction time. It was found that the optimal catalyst concentration (Ti(OBu)4) for the synthesis of these thermoplastic elastomers was 1.0 mmol/mol ester and the optimal DPPD concentration was 1.0 wt-%. The extent of the reaction was followed by measuring the inherent viscosity of the reaction mixture. The effectiveness of the incorporation of the soft segments into the copolymer chains was proved by Soxhlet extraction with chloroform. The molecular structures, composition and the size of the synthesized poly(ester-butylene)s were verified by 1H NMR spectroscopy, viscometry of dilute solutions and the complex dynamic melt viscosity. The thermal properties of poly(ester-olefin)s were investigated by differential scanning calorimetry (DSC). The degree of crystallinity was also determined by DSC. The thermal and thermo-oxidative stability were investigated by thermogravimetric analysis (TGA). The rheological properties of poly(ester-olefin)s were investigated by dynamic mechanical spectroscopy in the melt and solid state.

scholarly journals A Micellar Mitotane Formulation with High Drug Loading and Solubility: Physico-Chemical Characterization and Cytotoxicity Studies in 2D and 3D in Vitro Tumor Models.

2019 ◽  
Author(s):  
Malik Salman Haider ◽  
Jochen Schreiner ◽  
Sabine Kendl ◽  
Matthias Kroiß ◽  
Robert Luxenhofer
Keyword(s):  
Water Solubility ◽  
Drug Loading ◽  
Plasma Concentrations ◽  
Ethanol Solution ◽  
Comparable Efficacy ◽  
Scanning Calorimetry ◽  
High Drug ◽  
Cytotoxicity Studies ◽  
High Drug Loading

Adrenocortical carcinoma (ACC) is a rare tumor and prognosis is overall poor but heterogeneous. Mitotane (MT) has been used for treatment of ACC for decades, either alone or in combination with cytotoxic chemotherapy. Even at doses up to 6 g per day, more than half of the patients do not achieve targeted plasma concentration (14-20 mg/L) even after many months of treatment which is caused by low water solubility and unfavorable pharmacokinetic properties such as poor bioavailability and high volume of distribution of MT. The clinical need and previously reported extraordinary high drug loading of poly(2-methyl-2-oxazoline)-block-poly(2-butyl-2-oxazoline)-block-poly(2-methyl-2-oxazoline) (A-pBuOx-A) based micelles for paclitaxel (PTX), led us to develop MT loaded micelles which may enable an injectable formulation. We successfully solubilized up to 6 g/L of MT in an aqueous formulation. The MT loaded nanoformulations were characterized by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and powder X-ray<br> <p>diffraction (XRD), confirmed the amorphous nature of drug in the formulations. The polymer itself did not show cytotoxicity in adrenal and liver cell lines. By using the ACC model cell line NCI-H295 both in monolayers and tumor cell spheroids, we demonstrated micellar MT to exhibit comparable efficacy to its ethanol solution. We postulate that this formulation would be suitable for i.v. application and more rapid attainment of therapeutic plasma concentrations. In conclusion, we consider our micellar formulation a promising tool to alleviate major drawbacks of current MT treatment while retaining bioactivity towards ACC in vitro.</p>

scholarly journals A Micellar Mitotane Formulation with High Drug Loading and Solubility: Physico-Chemical Characterization and Cytotoxicity Studies in 2D and 3D in Vitro Tumor Models.

2019 ◽  
Author(s):  
Malik Salman Haider ◽  
Jochen Schreiner ◽  
Sabine Kendl ◽  
Matthias Kroiß ◽  
Robert Luxenhofer
Keyword(s):  
Water Solubility ◽  
Drug Loading ◽  
Plasma Concentrations ◽  
Ethanol Solution ◽  
Comparable Efficacy ◽  
Scanning Calorimetry ◽  
High Drug ◽  
Cytotoxicity Studies ◽  
High Drug Loading

Adrenocortical carcinoma (ACC) is a rare tumor and prognosis is overall poor but heterogeneous. Mitotane (MT) has been used for treatment of ACC for decades, either alone or in combination with cytotoxic chemotherapy. Even at doses up to 6 g per day, more than half of the patients do not achieve targeted plasma concentration (14-20 mg/L) even after many months of treatment which is caused by low water solubility and unfavorable pharmacokinetic properties such as poor bioavailability and high volume of distribution of MT. The clinical need and previously reported extraordinary high drug loading of poly(2-methyl-2-oxazoline)-block-poly(2-butyl-2-oxazoline)-block-poly(2-methyl-2-oxazoline) (A-pBuOx-A) based micelles for paclitaxel (PTX), led us to develop MT loaded micelles which may enable an injectable formulation. We successfully solubilized up to 6 g/L of MT in an aqueous formulation. The MT loaded nanoformulations were characterized by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and powder X-ray<br> <p>diffraction (XRD), confirmed the amorphous nature of drug in the formulations. The polymer itself did not show cytotoxicity in adrenal and liver cell lines. By using the ACC model cell line NCI-H295 both in monolayers and tumor cell spheroids, we demonstrated micellar MT to exhibit comparable efficacy to its ethanol solution. We postulate that this formulation would be suitable for i.v. application and more rapid attainment of therapeutic plasma concentrations. In conclusion, we consider our micellar formulation a promising tool to alleviate major drawbacks of current MT treatment while retaining bioactivity towards ACC in vitro.</p>

scholarly journals Effect of Spray Drying on the Microencapsulation of Blueberry Natural Antioxidants

Proceedings ◽  
2020 ◽  
Vol 70 (1) ◽  
pp. 26
Author(s):  
Mariana S. Lingua ◽  
Virginia Salomón ◽  
María V. Baroni ◽  
Jesica E. Blajman ◽  
Luis María Maldonado ◽  
...  
Keyword(s):  
Phenolic Compounds ◽  
Moisture Content ◽  
Spray Drying ◽  
Encapsulation Efficiency ◽  
Water Solubility ◽  
Phenolic Content ◽  
Natural Antioxidants ◽  
Total Phenolic ◽  
Inlet Temperature ◽  
Food Ingredients

Phenolic compounds obtained from blueberries have gained great attention due to their more effective bioactive roles in human health than those of whole berries. However, they are sensitive to environmental conditions and are therefore susceptible to degradation affecting their effectiveness. The microencapsulation of these compounds by spray drying provides a solution to these problems. This work aimed to study the effect of spray drying on the microencapsulation of the blueberry phenolic compounds to optimize the production of a powder rich in stable polyphenols. The phenolic extract from blueberries was spray dried under different conditions of inlet air temperatures (140 and 160 °C) and encapsulating agent concentrations (20 and 30% w/v), using maltodextrin (14.7 dextrose equivalent). The drying yield, moisture content, water-solubility, total and surface phenolic content, and encapsulation efficiency of total phenolic were investigated. The results obtained showed that the different conditions evaluated influenced the drying yield, moisture content, surface phenolic content, and encapsulation efficiency of phenolic compounds. In this sense, the powders with the best characteristics were obtained with 30% w/v of maltodextrin at 160 °C inlet temperature. These powders, rich in blueberry polyphenols stabilized by microencapsulation, are easier to handle for application, so they could be used as functional food ingredients.

scholarly journals CHARACTERIZATION OF DRUGS ENCAPSULATED INTO MESOPOROUS SILICA

2019 ◽  
pp. 7-11
Author(s):  
ARIF BUDIMAN
Keyword(s):  
Water Solubility ◽  
Drug Loading ◽  
Physicochemical Characterization ◽  
Amorphous State ◽  
Molecular State ◽  
Water Soluble ◽  
Crystal Nucleation ◽  
Formulation Development ◽  
Scanning Calorimetry

Solubility of the drug has a strong influence to achieve higher bioavailability of the drug in systemic circulation. More than 70% NCEs (new chemical entities) are hydrophobic, and practically difficult into solid formulation due to their poor water solubility. Mesoporous silicas (MSP) have been used for drug delivery system, especially for poorly water-soluble drugs. Encapsulation and interaction of drugs in MSP can enhance the delivery and maintain the stability of the drug. However, the characterization of the drug in MSP is necessary to confirm its molecular state. In this review, we present an overview of reports related to the characterization of drug encapsulated into MSP. Encapsulation of drugs in MSP can prevent recrystallization of drugs due to its inhibition of crystal nucleation. A porous material in MSP can maintain the drug in a physically stable amorphous state. The preventing of drug crystallization in MSP can enhance the solubility and the dissolution rate of drug. Therefore, in this work, attempts have been made to understand the molecular state of the drug in MSP. The physicochemical characterization of drug by transmission electron microscopy (TEM), scanning electron microscope (SEM), differential scanning calorimetry (DSC), fourier-transform infrared spectroscopy (FTIR), powder x-ray diffraction (PXRD) and thermogravimetric analysis (TGA) were discussed. The effect of solvent and methods of drug loading and the effect of the shape of MSP on release profiles are also presented. Overall, this review provides information about the characterization of drug encapsulated into MSP which will be useful in pharmaceutical formulation development.

Preparation and Characterisation of Phase Change Material-Loaded Polyurea Microcapsules Several Hundred Micrometres in Diameter

2009 ◽  
Vol 17 (6) ◽  
pp. 365-369 ◽  
Author(s):  
Takayuki Takei ◽  
Masahiro Yoshida ◽  
Tomonori Nagayoshi ◽  
Yasuo Hatate ◽  
Kouichiro Shiomori ◽  
...  
Keyword(s):  
Phase Change ◽  
Phase Change Material ◽  
Weight Ratio ◽  
Phenyl Isocyanate ◽  
Toluene Diisocyanate ◽  
Molar Ratio ◽  
Agitation Rate ◽  
Scanning Calorimetry ◽  
Water Emulsion ◽  
Change Material

In the present study, we attempted to prepare phase-change material (PCM)-loaded polyurea microcapsules several hundred micrometres in diameter via oil-in-water emulsion polymerisation. An oil phase with two types of isocyanate monomers (2,4-toluene diisocyanate (TDI) and phenyl isocyanate (PI)) and tetradecane as PCM was dispersed in an aqueous phase with hexamethylene diamine (HMD). The polyurea shell of microcapsules was formed by reaction of the isocyanate monomers with the amine groups derived from HMD and hydrolysed isocyanate monomers. A suitably adjusted agitation rate made it possible to prepare the required microcapsules. An increased molar ratio of TDI to PI in oil phase resulted in improvement of microcapsule morphology. Increased weight ratio of tetradecane to the two isocyanate monomers (TDI and PI) led to an increase in the PCM content in the microcapsules, which is preferable for practical applications. An examination using differential scanning calorimetry analyser demonstrated that the polyurea shell of the microcapsules scarcely influenced the thermal properties of encapsulated tetradecane.

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