scholarly journals Preparation, Characterization, and In Vivo Pharmacoscintigraphy Evaluation of an Intestinal Release Delivery System of Prussian Blue for Decorporation of Cesium and Thallium

2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
Nidhi Sandal ◽  
Gaurav Mittal ◽  
Aseem Bhatnagar ◽  
Dharam Pal Pathak ◽  
Ajay Kumar Singh
Keyword(s):  
Prussian Blue ◽  
Delivery System ◽  
Oral Delivery ◽  
Polymer Concentration ◽  
Particle Size Analysis ◽  
Size Analysis ◽  
Cesium 137 ◽  
Ph Dependent ◽  
Us Fda

Background. Prussian blue (PB, ferric hexacyanoferrate) is approved by US-FDA for internal decorporation of Cesium-137 (137Cs) and Thallium-201 (201Tl). Aim. Since PB is a costly drug, pH-dependent oral delivery system of PB was developed using calcium alginate matrix system. Methods. Alginate (Alg) beads containing PB were optimized by gelation of sodium alginate with calcium ions and effect of varying polymer concentration on encapsulation efficiency and release profile was investigated. Scanning electron microscopy (SEM) was carried out to study surface morphology. Adsorption efficacy of Alg-PB beads for 201Tl was evaluated and compared with native PB. In vivo pH-dependent release of the formulation was studied in humans using gamma scintigraphy. Results. Encapsulation efficiencies of Alg-PB beads with 0.5, 1.0, 1.5, and 2.0% polymer solution were 99.9, 91, 92, and 93%, respectively. SEM and particle size analysis revealed differences between formulations in their appearance and size distribution. No drug release was seen in acidic media (pH of 1-2) while complete release was observed at pH of 6.8. Dissolution data was fitted to various mathematical models and beads were found to follow Hixson-Crowell mechanism of release. The pH-dependent release of beads was confirmed in vivo by pharmacoscintigraphy in humans.

Acyclovir Loaded Solid Lipid Nanoparticle Based Cream: A Novel Drug Delivery System

2017 ◽  
Vol 7 (1) ◽  
Author(s):  
EL- Assal I. A. ◽  
Retnowati .
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Antiviral Agent ◽  
Study Drug ◽  
Particle Size Analysis ◽  
Stability Study ◽  
Size Analysis ◽  
Solid Lipid ◽  
Dermal Delivery

Objective of the present investigation was enthused by the possibility to develop solid lipid nanoparticles (SLNs) of hydrophilic drug acyclovir. Also study vitro and vivo drug delivery. Methods: Drug loaded SLNs (ACV-SLNs) were prepared by high pressure homogenization of aqueous surfactant solutions containing the drug-loaded lipids in the melted or in the solid state with formula optimization study (Different lipid concentration, drug loaded, homogenization / stirring speed and compritol 888ATO: drug ratio). ACV - SLN incorporated in cream base. The pH was evaluated and rheological study. Drug release was evaluated and compared with simple cream- drug, ACV – SLN with compritol 888ATO and marketed cream. The potential of SLN as the carrier for dermal delivery was studied. Results: Particle size analysis of SLNs prove small, smooth, spherical shape particle ranged from 150 to 200 nm for unloaded and from 330 to 444 nm for ACV loaded particles. The EE% for optimal formula is 72% with suitable pH for skin application. Rheological behavior is shear thinning and thixotropic. Release study proved controlled drug release for SLNs especially in formula containing compritol88 ATO. Stability study emphasized an insignificant change in SLNs properties over 6 month. In-vivo study showed significantly higher accumulation of ACV in stratum corneum, dermal layer, and receptor compartment compared with blank skin. Conclusion: AVC-loaded SLNs might be beneficial in controlling drug release, stable and improving dermal delivery of antiviral agent(s).

Formulation, Characterization and In Vivo Evaluation of Self-Nanoemulsifying Drug Delivery System for Oral Delivery of Valsartan

2014 ◽  
Vol 10 (2) ◽  
pp. 263-270 ◽  
Author(s):  
Maulick Chopra ◽  
Usha Y. Nayak ◽  
Aravind Kumar Gurram ◽  
M. Sreenivasa Reddy ◽  
K.B. Koteshwara
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
In Vivo Evaluation

scholarly journals Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation

Nanomaterials ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 2920
Author(s):  
Ameeduzzafar Zafar ◽  
Syed Sarim Imam ◽  
Nabil K. Alruwaili ◽  
Omar Awad Alsaidan ◽  
Mohammed H. Elkomy ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Ex Vivo ◽  
In Vitro Release ◽  
System Optimization ◽  
Globule Size

Hypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and transcutol HP as oil, surfactant, and co-surfactant, respectively. The formulation was optimized by three-factor, three-level Box-Behnken design. PE-SNEDDs were characterized for globule size, emulsification time, stability, in-vitro release, and ex-vivo intestinal permeation study. The optimized PE-SNEDDS (OF3) showed the globule size of 70.34 ± 3.27 nm, percentage transmittance of 99.02 ± 2.02%, and emulsification time of 53 ± 2 s Finally, the formulation OF3 was transformed into solid PE-SNEDDS (S-PE-SNEDDS) using avicel PH-101 as adsorbent. The reconstituted SOF3 showed a globule size of 73.56 ± 3.54 nm, PDI of 0.35 ± 0.03, and zeta potential of −28.12 ± 2.54 mV. SEM image exhibited the PE-SNEDDS completely adsorbed on avicel. Thermal analysis showed the drug was solubilized in oil, surfactant, and co-surfactant. S-PE-SNEDDS formulation showed a more significant (p < 0.05) release (97.87 ± 4.89% in 1 h) than pure PE (27.87 ± 2.65% in 1 h). It also exhibited better antimicrobial activity against S. aureus and P. aeruginosa and antioxidant activity as compared to PE dispersion. The in vivo activity in rats exhibited better (p < 0.05) antihypertensive activity as well as 4.92-fold higher relative bioavailability than pure PE dispersion. Finally, from the results it can be concluded that S-PE-SNEDDS might be a better approach for the oral delivery to improve the absorption and therapeutic activity.

scholarly journals Increased Carrier Peptide Stability through pH Adjustment Improves Insulin and PTH(1-34) Delivery In Vitro and In Vivo Rather than by Enforced Carrier Peptide-Cargo Complexation

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 993
Author(s):  
Mie Kristensen ◽  
Ragna Guldsmed Diedrichsen ◽  
Valeria Vetri ◽  
Vito Foderà ◽  
Hanne Mørck Nielsen
Keyword(s):  
Oral Delivery ◽  
Molecular Size ◽  
Therapeutic Peptide ◽  
Enzymatic Stability ◽  
Therapeutic Peptides ◽  
Ph Dependent ◽  
Pharmacologically Active ◽  
High Degree

Oral delivery of therapeutic peptides is hampered by their large molecular size and labile nature, thus limiting their permeation across the intestinal epithelium. Promising approaches to overcome the latter include co-administration with carrier peptides. In this study, the cell-penetrating peptide penetratin was employed to investigate effects of co-administration with insulin and the pharmacologically active part of parathyroid hormone (PTH(1-34)) at pH 5, 6.5, and 7.4 with respect to complexation, enzymatic stability, and transepithelial permeation of the therapeutic peptide in vitro and in vivo. Complex formation between insulin or PTH(1-34) and penetratin was pH-dependent. Micron-sized complexes dominated in the samples prepared at pH-values at which penetratin interacts electrostatically with the therapeutic peptide. The association efficiency was more pronounced between insulin and penetratin than between PTH(1-34) and penetratin. Despite the high degree of complexation, penetratin retained its membrane activity when applied to liposomal structures. The enzymatic stability of penetratin during incubation on polarized Caco-2 cell monolayers was pH-dependent with a prolonged half-live determined at pH 5 when compared to pH 6.5 and 7.4. Also, the penetratin-mediated transepithelial permeation of insulin and PTH(1-34) was increased in vitro and in vivo upon lowering the sample pH from 7.4 or 6.5 to 5. Thus, the formation of penetratin-cargo complexes with several molecular entities is not prerequisite for penetratin-mediated transepithelial permeation a therapeutic peptide. Rather, a sample pH, which improves the penetratin stability, appears to optimize the penetratin-mediated transepithelial permeation of insulin and PTH(1-34).

scholarly journals Formulation and Pharmacokinetic Evaluation of Phosal Based Zaltoprofen Solid Self-Nanoemulsifying Drug Delivery System

2019 ◽  
Vol 7 (4) ◽  
pp. 328-338
Author(s):  
Rajan Kalamkar ◽  
Shailesh Wadher
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase Diagram ◽  
In Vitro Dissolution ◽  
Size Analysis ◽  
Dissolution Profile ◽  
Globule Size ◽  
Water Insoluble Drug

Background: Phosal based excipients are liquid concentrates containing phospholipids. They are used to solubilize water-insoluble drug and also act as an emulsifier to get the smallest droplet size of the formed emulsion after administration. Objective: The aim is to prepare phosal based self nanoemulsifying drug delivery system (SNEDDS) for water insoluble drug zaltoprofen. Methods: The various parameters like solubility of drug in different vehicles, ternary phase diagram are considered to formulate the stable emulsion which is further characterized by Self emulsification time and globule size analysis to optimize liquid SNEDDS of Zaltoprofen. Optimized L-SNEDDS was converted into free-flowing powder Solid-SNEDDS (S-SNEDDS). S-SNEDDS was evaluated for Globule size analysis after reconstitution, in vitro dissolution study and in vivo pharmacokinetic study in rats. Results: Phosal 53 MCT with highest drug solubility was used as oil along with Tween 80 and PEG 400 as surfactant and cosurfactant respectively to prepare liquid SNEDDS. Neusilin us2 was used as an adsorbent to get free-flowing S-SNEDDS. S-SNEDDS showed improved dissolution profile of the drug as compared to pure drug. In vivo study demonstrated that there is a significant increase in Cmax and AUC of S-SNEDDS compared to zaltoprofen powder. Conclusion: Phosal based SNEDDS formation can be successfully used to improve the dissolution and oral bioavailability of poorly soluble drug zaltoprofen.

In vivo evaluation of an oral delivery system for P-gp substrates based on thiolated chitosan

Biomaterials ◽  
2006 ◽  
Vol 27 (23) ◽  
pp. 4250-4255 ◽  
Author(s):  
Florian Föger ◽  
Thierry Schmitz ◽  
Andreas Bernkop-Schnürch
Keyword(s):  
Delivery System ◽  
Oral Delivery ◽  
In Vivo Evaluation ◽  
Thiolated Chitosan ◽  
Oral Delivery System

scholarly journals Preparation, in vitro and in vivo evaluation of algino-pectinate bioadhesive microspheres: An investigation of the effects of polymers using multiple comparison analysis

2010 ◽  
Vol 60 (3) ◽  
pp. 255-266 ◽  
Author(s):  
Santanu Chakraborty ◽  
Madhusmruti Khandai ◽  
Anuradha Sharma ◽  
Nazia Khanam ◽  
Ch. Patra ◽  
...  
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Drug Carrier ◽  
Polymer Concentration ◽  
Multiple Comparison ◽  
Prolonged Release ◽  
Comparison Analysis ◽  
Significant Difference

Preparation,in vitroandin vivoevaluation of algino-pectinate bioadhesive microspheres: An investigation of the effects of polymers using multiple comparison analysisIonotropic gelation was used to entrap aceclofenac into algino-pectinate bioadhesive microspheres as a potential drug carrier for the oral delivery of this anti-inflammatory drug. Microspheres were investigatedin vitrofor possible sustained drug release and their usein vivoas a gastroprotective system for aceclofenac. Polymer concentration and polymer/drug ratio were analyzed for their influence on microsphere properties. The microspheres exhibited good bioadhesive property and showed high drug entrapment efficiency. Drug release profiles exhibited faster release of aceclofenac from alginate microspheres whereas algino-pectinate microspheres showed prolonged release. Dunnet's multiple comparison analysis suggested a significant difference in percent inhibition of paw edema when the optimized formulation was compared to pure drug. It was concluded that the algino-pectinate bioadhesive formulations exhibit promising properties of a sustained release form for aceclofenac and that they provide distinct tissue protection in the stomach.

Particle Size Analysis of Fe3O4 Nanoparticles Coated by Polyethyleneglycol

2015 ◽  
Vol 820 ◽  
pp. 373-377 ◽  
Author(s):  
Fernanda A. Sampaio da Silva ◽  
Edwin E.G. Rojas ◽  
Marcos Flávio de Campos
Keyword(s):  
Particle Size ◽  
Average Diameter ◽  
Rietveld Analysis ◽  
Particle Size Analysis ◽  
Size Analysis ◽  
Cancer Treatments ◽  
Peg 4000 ◽  
Size Characterization ◽  
Particle Size Characterization

Nanotechnology has been shown as an important tool for developing intelligent devices. In particular, magnetic nanoparticles have been studied due their applications in cancer treatments. However, nanoparticles need to be tightly controlled in relation to size, shape and coating. It makes particles suitable for in vivo applications. In this work, magnetite nanoparticles were used for particle size characterization. Fe3O4 crystals were coated by polyethyleneglycol (PEG 4000). Three different techniques were performed to obtain the nanoparticles average diameter: Rietveld Analysis, Scherrer Equation and Nanosight®. Results indicate good properties.

Chronomodulated Drug Delivery System of Salmeterol Fluticasone Nlcs Loaded Tablets: Preparation, Characterization, Stability and Drug Release Studies for Management of Asthma

2021 ◽  
Vol 11 (2) ◽  
pp. 95-102
Author(s):  
Mohammed Waseem A ◽  
Ajin P Kurian ◽  
Dhanapal Y
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Drug Loading ◽  
Water Soluble ◽  
Size Analysis ◽  
Differential Scanning Calorimetric ◽  
Time Interval

Objective: The purpose of this study was to develop salmeterol, fluticasone nano-lipid carriers to estimate as potentials of oral delivery system for poorly water soluble drugs. Nano-lipid carriers applied to chronomodulated pulsatile drug delivery system maintain the concentration level by releasing the drug at predetermined time interval throughout the management of asthma. Method: The particle size analysis revealed that all the formulations were within the nanometer range of 150.0±2.4nm. Percentage of entrapment efficiency and drug loading were found to be 69.5±4.4 - 85.3±1.3 and 9.358±2.2-10.45±8.1, respectively. The SLM-FCN nano-lipid carrier’s optimized formulation showed spherical morphology with smooth surface under the transmission electron microscope (TEM), the crystalline characterization of drug in NLC was investigated by X-ray diffraction and differential scanning calorimetric (DSC). The ex-vivo permeation study showed many folds increment in the SLM-FCN NLCs compared to powder SLM-FCN 96.0±2.55 and pulsing plugs in-vivo drug released effectively in pre-determine time intervals. Conclusion: The progression concludes that chronomodulated programming pulsatile release was achieved with modified pulsing bilayerd plugged of salmeterol, fluticasone propionate NLCs, formulation remarkably improved oral bioavailability. we promise that finding in this investigations suggest practicability of the dosage form system can be taken after at bedtime then it will be delivered in the early morning which maintains the drug concentration throughout to control asthma.

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