Preparation and Characterization of Danazol Nanoparticles for Dissolution Improvement

2018 ◽  
Vol 9 (SPL1) ◽  
Author(s):  
Luma Safa el-din Al-Hassnaui
Keyword(s):  
Particle Size ◽  
Phosphate Buffer ◽  
Phosphate Buffer Solution ◽  
Amorphous State ◽  
Volume Ratio ◽  
In Vitro Dissolution ◽  
Buffer Solution ◽  
Solution Ph ◽  
Freeze Dried

Danazol is a synthetic steroid used for endometriosis treatment, haslow bioavailability as it is practically insoluble in water. This study has been carried out to prepare and characterize danazol nanoparticles by nanoprecipitation method at a different polymer to drug ratios of 0.5:1,1:1,2:1 and 3:1 using different polymers of CMC-30 and various grades of HPMC and PVP,as stabilizers. Variables that might affect the particle size as polymer type,polymer to drug ratio,temperature of precipitation,addition rate of danazol solution,volume ratio,time of stirring,concentrationof drug,have been investigated. The particle size of the prepared formulas has been in the nano-sized except those using CMC and the best formula has beenF20 at a polymer to drug ratio of0.5:1 which has given the smallest particle sizeof 33nm.The investigations of the drug–stabilizer compatibility havebeen studied by FTIR and DSC,crystalline state by XRD,size,and shape of nanoparticles by FESEM and the results showed that there has been no interaction between the danazol and stabilizer and there has been a partial conversion of danazol from crystalline to an amorphous state with a size below 100nm. Most of the studied factors havebeen found affect the particle size of the nanoparticles.The Entrapment efficiency has been (91.3% ± 0.4) in the (F20). The solubility study revealed that 6.75,4.97 and 5.1 folds increased of solubility of danazol for nanoparticles than that for raw in distilled water,0.1N HCl and in phosphate buffer of pH 6.8.The simple capsule has been prepared by incorporation of freeze-dried of F20 with lactose as a filler and the in vitro dissolution study has been conducted using 0.1N HCl (pH 1.2) with 2% w/v Brij-35,phosphate buffer solution(pH 6.8) with 2% w/v Brij-35as dissolution media. Within 30 minutes,100% of the danazol has been released from the nanoparticle capsule in both dissolution media compared to the raw and physical blend capsules as controls havebeen nearly complete in 120 minutes.One can conclude that Antisolvent method is an easy,efficient method to prepare danazol nanoparticles with an intense effect on solubility and faster in vitro dissolution rate than raw drug and its physical blend with stabilizer.

scholarly journals Encapsulation of Polyphenols from Lycium barbarum Leaves into Liposomes as a Strategy to Improve Their Delivery

Nanomaterials ◽  
2021 ◽  
Vol 11 (8) ◽  
pp. 1938
Author(s):  
Ramona-Daniela Păvăloiu ◽  
Fawzia Sha’at ◽  
Georgeta Neagu ◽  
Mihaela Deaconu ◽  
Corina Bubueanu ◽  
...  
Keyword(s):  
Particle Size ◽  
Phosphate Buffer ◽  
Phosphate Buffer Solution ◽  
Entrapment Efficiency ◽  
Cytoprotective Effect ◽  
Buffer Solution ◽  
Lycium Barbarum ◽  
Burst Effect ◽  
Pharmaceutical Applications

This study is focused on the encapsulation of polyphenols from Lycium barbarum leaves into liposomes as a strategy to improve their delivery. Liposomes loaded with Lycium barbarum leaves extract were obtained and characterized for particle size, polydispersity, entrapment efficiency, and stability. Liposomes presented entrapment efficiency higher than 75%, nanometric particle size, narrow polydispersity, and good stability over three months at 4 °C. The liposomes containing Lycium barbarum offered a slower release of polyphenols with attenuated burst effect compared with the dissolution of free Lycium barbarum extract in phosphate buffer solution at pH 7.4. Moreover, an in vitro pretreatment of 24 h with loaded liposomes showed a cytoprotective effect against H2O2-induced cytotoxicity on L-929 mouse fibroblasts cells. These preliminary findings imply that liposomes could be successfully employed as carriers for polyphenols in pharmaceutical applications.

The Study of Albumin Release from Silica/Albumin as a Potential Drug Delivery Carrier

2014 ◽  
Vol 69 (5) ◽  
Author(s):  
Shafiyah Pondi ◽  
Jon Efendi ◽  
Ho Chin Siong ◽  
Lai Sin Yuan ◽  
Sheela Chandren ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Fumed Silica ◽  
In Vitro Release ◽  
Phosphate Buffer Solution ◽  
Buffer Solution ◽  
Solution Ph ◽  
Drug Delivery Carrier ◽  
High Interaction ◽  
Uv Visible

The drug-delivery field has been an attractive as well as challenging area for research. With the emerging of new formulated drugs and pharmaceutical compounds, development of good drug-delivery system (DDS) is crucially required. This study aims to utilize albumin as the drug template in silica/albumin/drug (S/A/D) system. Prior to designing this system, the interaction between silica and albumin was investigated. It is hypothesized that high interaction between silica and albumin may result in slower drug release over time, which is preferred for a good DDS. Silica and albumin (S/A) materials were prepared by using fumed silica and tetraethyl orthosilicate (TEOS) as the silica precursors. Three different S/A samples were prepared; fumed silica with albumin (FS/A), fumed silica with pre-treated albumin by sodium borohydrate (FS/A-N), and silica sol (TEOS) with albumin (SS/A). In-vitro release of albumin in phosphate buffer solution (pH 7) was carried out to examine the interaction between albumin and silica. The concentration of albumin was detected at 280 nm by UV-visible spectrophotometer. All samples were characterized by diffuse reflectance-UV-visible spectrophotometer (DR-UV), Fourier transform infrared spectrophotometer (FTIR) dan thermogravimetric-differential thermal analysis (TG-DTA). DR-UV results show that SS/A exhibited the lowest absorption intensity at 280 nm, which indicates better interaction between silica and albumin. This result was supported by the presence of Si-O stretching band of silanol at 952 cm-1 from the FTIR spectrum. Release study of albumin demonstrated that the release of albumin from SS/A was slowest compared to those of FS/A and FS/A-N. 

scholarly journals Color Stability of Phycoerythrin Crude Extract (PECE) from Rhodomonas Salina Toward Physicochemical Factors

2019 ◽  
Vol 14 (1) ◽  
pp. 21
Author(s):  
Endar Marraskuranto ◽  
Tri Joko Raharjo ◽  
Rina Sri Kasiamdari ◽  
Tri Rini Nuringtyas
Keyword(s):  
Phosphate Buffer Solution ◽  
Color Stability ◽  
Ethanol Solution ◽  
Future Application ◽  
Buffer Solution ◽  
Solution Ph ◽  
Rhodomonas Salina ◽  
Freeze Dried ◽  
Physicochemical Factors ◽  
The Stability

Rhodomonas salina produces Cr-phycoerythrin545 as its designated phycoerythrin (PE) with an absorption maximum at 545 nm and a shoulder 564 nm. PE has potential to be applied as colorants, pharmaceutical agents, and fluorescent dye tags. The stability of the PE color is influenced by the physicochemical factors of the solution. This study aimed to analyze the color stability of PECE against chemical (ethanol and pH) and physical (light and temperature) factors. PECE was prepared from freeze-dried biomass of R. salina and was extracted in phosphate buffer solution (pH = 6.0) using a freeze-thaw method in -25 oC (2 hours) and 4 oC (24 hours). The resulting extract was concentrated and dried in a freeze-dryer. Analyses were conducted using UV-visible and fluorescence spectrophotometer. PECE showed color stability against light of white fluorescent lamp exposure up to 8 hours, temperature exposure up to 40 oC, ethanol solution up to concentration of 20 % (v/v), and pH range 3.9-8.42. Results from this study can be useful for extraction, purification, and future application of Cr-PE545.

scholarly journals Enhancement of Solubility and Improvement of Dissolution Rate of Atorvastatin Calcium Prepared as Nanosuspension

2019 ◽  
Vol 28 (2) ◽  
pp. 46-57
Author(s):  
Ahmed H. Ali ◽  
Shaimaa N. Abd-Alhammid
Keyword(s):  
Particle Size ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Precipitation Method ◽  
Size Analysis ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Atorvastatin Calcium ◽  
Freeze Dried

       Atorvastatin have problem of very slightly aqueous solubility (0.1-1 mg/ml). Nano-suspension is used to enhance it’s of solubility and dissolution profile. The aim of this study is to formulate Atorvastatin as a nano-suspension to enhance its solubility due to increased surface area of exposed for dissolution medium, according to Noyes-Whitney equation.         Thirty one formulae were prepared to evaluate the effect of ; Type of polymer, polymer: drug ratio, speed of homogenization, temperature of preparation and inclusion of co-stabilizer in addition to the primary one; using solvent-anti-solvent precipitation method under high power of ultra-sonication. In this study five types of stabilizers (TPGS, PVP K30, HPMC E5, HPMC E15, and Tween80) were used in three different concentrations 1:1, 1:0.75 and 1:0.5 for preparing of formulations. At the same time, tween80 and sodium lauryl sulphate have been added as a co-stabilizer.          Atorvastatin nano-suspensions were evaluated for particle size, PDI, zeta potential, crystal form and surface morphology. Finally, results of particle size analysis revealed reduced nano-particulate size to 81nm for optimized formula F18 with the enhancement of in-vitro dissolution profile up to 90% compared to 44% percentage cumulative release for the reference Atorvastatin calcium powder in 6.8 phosphate buffer media. Furthermore, saturation solubility of freeze dried Nano suspension showed 3.3, 3.8, and 3.7 folds increments in distilled water, 0.1N Hcl and 6.8 phosphate buffers, respectively. Later, freeze dried powder formulated as hard gelatin capsules and evaluated according to the USP specifications of the drug content and the disintegration time.        As a conclusion; formulation of poorly water soluble Atorvastatin calcium as nano suspension significantly improved the dissolution of the drug and enhances its solubility.

scholarly journals In vitro dissolution and in vivo gamma scintigraphic evaluation of press-coated salbutamol sulfate tablets

2013 ◽  
Vol 63 (4) ◽  
pp. 545-551 ◽  
Author(s):  
Wei Li ◽  
Cai-Hong Shi ◽  
Yi-Ling Sheng ◽  
Ping Cui ◽  
Yu-Qing Zhao ◽  
...  
Keyword(s):  
In Vitro Release ◽  
Phosphate Buffer Solution ◽  
Gamma Scintigraphy ◽  
In Vitro Dissolution ◽  
Salbutamol Sulfate ◽  
Buffer Solution ◽  
Delayed Release ◽  
Vitro Release

Abstract The aim of this study was to investigate the in vitro and in vivo performance of salbutamol sulfate press-coated tablets for delayed release. The in vitro release behavior of press-coated tablets with the outer layer of PEG 6000/ Eudragit S100 blends (2:1) in pH 1.2 (0.1 mol L-1 HCl) and then pH 6.8 buffer solution was examined. Morphological change of the press-coated tablet during in vitro release was recorded with a digital camera. Release of salbutamol sulfate from press-coated tablets was less than 5 % before 3 h and was completed after 8 h in pH 6.8 phosphate buffer solution. In vivo gamma scintigraphy study carried out on healthy men indicated that the designed system released the drug in lower parts of the GI tract after a lag time of 5 hours. The results showed the capability of the system of achieving delayed release of the drug in both in vitro and in vivo gamma scintigraphy studies.

Synthesis, characterization, and drug delivery property of 2-N-carboxymethyl-6-O-diethylaminoethyl-chitosan

e-Polymers ◽  
2013 ◽  
Vol 13 (1) ◽  
Author(s):  
Aidi Zhang ◽  
Derun Ding ◽  
Jicun Ren ◽  
Xiangli Zhu ◽  
Youhong Yao
Keyword(s):  
Phosphate Buffer ◽  
Phosphate Buffer Solution ◽  
Controlled Delivery ◽  
Protective Agent ◽  
Buffer Solution ◽  
Solution Ph ◽  
H Nmr ◽  
Structure Morphology ◽  
Ft Ir ◽  
Model Drug

Abstract A novel route is demonstrated for the synthesis of 2-N-carboxymethyl-6- O-diethylaminoethyl-chitosan (DEAE-CMC) by incorporation of carboxymethyl groups as hydrophilic moieties to the C2-NH2, and diethylaminoethyl groups as hydrophobic moieties to the C6-CH2OH of the structural unit of chitosan, via a protection-graft-deprotection procedure with benzaldehyde as protective agent. The structure, morphology, and thermal properties of the chitosan graft copolymers were characterized by means of FT-IR, 1H NMR, SEM, TGA and DSC. Chitosan and its derivatives were used as carrier of model drug-Vitamin B12 (VB12), and their controlled delivery behaviour in phosphate buffer solution (pH 7.4) were studied. The results show that the release rate of VB12 from the carrier of DEAE-CMC copolymer becomes much slower than that of chitosan in phosphate buffer solution.

Glucose electro-oxidation on Pt(100) in phosphate buffer solution (pH 7): A mechanistic study

2020 ◽  
Vol 354 ◽  
pp. 136765 ◽  
Author(s):  
Gisele A.B. Mello ◽  
William Cheuquepán ◽  
Valentín Briega-Martos ◽  
Juan M. Feliu
Keyword(s):  
Phosphate Buffer ◽  
Phosphate Buffer Solution ◽  
Mechanistic Study ◽  
Buffer Solution ◽  
Solution Ph ◽  
Electro Oxidation

scholarly journals Olanzapine Loaded Nanostructured Lipid Carriers via High Shear Homogenization and Ultrasonication

2021 ◽  
Vol 89 (2) ◽  
pp. 25
Author(s):  
Adejumoke Lara Ajiboye ◽  
Uttom Nandi ◽  
Martin Galli ◽  
Vivek Trivedi
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Drug Loading ◽  
Particle Diameter ◽  
Phosphate Buffer Solution ◽  
Nanostructured Lipid Carriers ◽  
High Shear ◽  
Buffer Solution ◽  
High Shear Homogenization

The aim of this study was to understand the effect of high shear homogenization (HSH) and ultrasonication (US) on the physicochemical properties of blank and olanzapine loaded nanostructured lipid carriers (NLCs) along with their drug loading potential and drug release profiles from formulated particles. NLCs were prepared with different ratios of Compritol and Miglyol as the solid and liquid lipids, respectively, under changing HSH and US times between 0 to 15 minutes. The surfactants (Poloxamer 188 (P188) and tween 80) and the drug content was kept constant in all formulations. The prepared NLCs were evaluated for particle size, polydispersity index, zeta potential, drug crystallinity and chemical interactions between lipids and OLZ. The in-vitro drug release was performed using dialysis tube method in phosphate buffer solution (PBS) at pH 7.4. The formulated NLCs were negatively charged, spherically shaped and monodisperse, with particle sizes ranging from 112 to 191 nm. There was a significant influence of US time on the preparation of NLCs in comparison to HSH, where a significant reduction in the mean particle diameter was seen after 5 min of sonication. An increase of Miglyol content in NLCs led to an increase in particle size. In general, application of US led to decrease in particle size after HSH but an increase in particle diameter of low Miglyol containing preparation was also observed with longer sonication time. OLZ was successfully encapsulated in the NLCs and a total release of 89% was achieved in 24 hours in PBS at pH 7.4.

Formulation and Evaluation of Ketoprofen Using β-Cyclodextrin Capped Silver Nanoparticles

2021 ◽  
Vol 14 (3) ◽  
pp. 5501-5507
Author(s):  
Kiranmai Mandava ◽  
Kruthika Lalit ◽  
Venu Madhav Katla
Keyword(s):  
Particle Size ◽  
Silver Nanoparticles ◽  
Average Particle Size ◽  
Amorphous State ◽  
Entrapment Efficiency ◽  
In Vitro Dissolution ◽  
Average Particle ◽  
Dissolution Studies ◽  
Drug Entrapment Efficiency

The objective of the study was to develop silver nanoparticles loaded with Ketoprofen (Ag-KP) for increasing the drug solubility and thereby its bioavailability. Ag-KP were prepared by the solvent evaporation method using β-Cyclodextrin as a biodegradable polymer. Different formulations of Ag-KP were characterized for the drug entrapment efficiency, Fourier Transform Infrared Spectroscopy (FTIR), particle size analysis, X-ray diffraction studies (XRD), scanning electron microscopy (SEM) and  in-vitro dissolution studies. The optimized formulation (F6) has shown an average particle size of 167.8 ± 3.46 nm,zeta potential of -23.7 ± 1.46 mV. FTIR revealed that the drug showed good excipient compatibility. XRD studies showed that the drug has changed from crystalline to amorphous state. In all formulations, F6 formulation (optimized) exhibited high drug entrapment efficiency (∼93%). SEM studies indicated the shape of Ag-KP was roughly spherical with smooth surface. In vitro dissolution studies showed that Ag-KP from F6 formulation was 94.3 ± 4.9% but for the marketed formulation, it is only 84.6 ± 3.7% in 12 hours and F6 was found to be found stable for three months at both refrigerated and room temperature (RT).

Synthesis of antimicrobial polymer composition and in vitro drugs release study

e-Polymers ◽  
2008 ◽  
Vol 8 (1) ◽  
Author(s):  
Tudorachi Nita
Keyword(s):  
Diclofenac Sodium ◽  
Phosphate Buffer Solution ◽  
Polymer Composition ◽  
Size Analysis ◽  
Colloidal Silver ◽  
Silver Particles ◽  
Buffer Solution ◽  
Solution Ph ◽  
Oh Groups

AbstractThe study presents a procedure to acquire a colloidal silver-based antimicrobial polymer composition. Carboxymethylstarch (CMS) as polymer matrix, and colloidal silver particles (Ag0) obtained by in situ synthesis with silver nitrate and sodium citrate as reducing agent, were used. In solution, the presence of COOH and OH groups in carboxymethylstarch directs to silver complexation and acquirement of a stable suspension of silver particles. Due to the presence of colloidal silver particles, the composition presents bacteriostatic activity and in association with some drugs (acetylsalicylic acid or diclofenac sodium) pharmaceutical compositions can be obtained, which are useful in the prevention and treatment of some infections or diseases. The compositions were characterized by FTIR spectroscopy, UV-vis spectrophotometry, particle size analysis and zeta potential measurements. Drug release tests were done in vitro in phosphate buffer solution (pH=7.4, at 37°C).

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