scholarly journals Synergistic Effect of Acetazolamide-(2-hydroxy)propyl β-Cyclodextrin in Timolol Liposomes for Decreasing and Prolonging Intraocular Pressure Levels

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2010
Author(s):  
Carmen M. Arroyo-García ◽  
Daniela Quinteros ◽  
Santiago D. Palma ◽  
Cesáreo J. Jiménez de los Santos ◽  
José R. Moyano ◽  
...  
Keyword(s):  
Intraocular Pressure ◽  
Synergistic Effect ◽  
Lipid Bilayer ◽  
In Vitro Release ◽  
Solubility Parameters ◽  
Binding Ability ◽  
Permeation Studies ◽  
Aqueous Core ◽  
Vitro Release

The purpose of this study was to design, for the first time, a co-loaded liposomal formulation (CLL) for treatment of glaucoma including timolol maleate (TM) in the lipid bilayer and acetazolamide (Acz)-(2-hydroxy)propyl β-cyclodextrin (HPβCD) complexes (AczHP) solubilized in the aqueous core of liposomes. Formulations with TM (TM-L) and AczHP (AczHP-L), separately, were also prepared and characterized. A preliminary study comprising the Acz/HPβCD complexes and their interaction with cholesterol (a component of the lipid bilayer) was realized. Then, a screening study on formulation factors affecting the quality of the product was carried out following the design of the experiment methodology. In addition, in vitro release and permeation studies and in vivo lowering intraocular pressure (IOP) studies were performed. The results of the inclusion complexation behavior, characterization, and binding ability of Acz with HPβCD showed that HPβCD could enhance the water solubility of Acz despite the weak binding ability of the complex. Ch disturbed the stability and solubility parameters of Acz due to the fact of its competence by CD; thus, Chems (steroid derivative) was selected for further liposome formulation studies. The optimization of the lipid bilayer composition (DDAB, 0.0173 mmol and no double loading) and the extrusion as methods to reduce vesicle size were crucial for improving the physico-chemical properties and encapsulation efficiency of both drugs. In vitro release and permeation studies demonstrated that the CLL formulation showed improvement in in vitro drug release and permeation compared to the liposomal formulations with a single drug (TM-L and AczHP-L) and the standard solutions (TM-S and AczHP-S). CLL showed high efficacy in reducing and prolonging IOP, suggesting that the synergistic effect of TM and Acz on aqueous humor retention and the presence of this cyclodextrin and liposomes as permeation enhancers are responsible for the success of this strategy of co-loading for glaucoma therapy.

Nanostructured Lipid Carriers for Intranasal Administration of Olanzapine in the management of Schizophrenia

2021 ◽  
Vol 14 ◽  
Author(s):  
Sarbjot Kaur ◽  
Ujjwal Nautiyal ◽  
Pooja A. Chawla ◽  
Viney Chawla
Keyword(s):  
Drug Delivery ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Nanostructured Lipid Carriers ◽  
Polydispersity Index ◽  
Poloxamer 407 ◽  
Ex Vivo Permeation ◽  
Permeation Studies ◽  
Vitro Release

Background: Background: Olanzapine belongs to a new class of dual spectrum antipsychotic agents. It is known to show promise in managing both the positive and negative symptoms of schizophrenia. Drug delivery systems based on nanostructured lipid carriers (NLC) are expected to provide rapid nose-to-brain transport of this drug and improved distribution into and within the brain. Objective: The present study deals with the preparation and evaluation of olanzapine loaded NLC via the intranasal route for schizophrenia. Methods: Olanzapine-NLC were formulated through the solvent injection method using isopropyl alcohol as the solvent, stearic acid as solid lipid, and oleic acid as liquid lipid, chitosan as a coating agent, and Poloxamer 407 as a surfactant. NLC were characterized for particle size, polydispersity index, entrapment efficiency, pH, viscosity, X-ray diffraction studies, in-vitro mucoadhesion study, in- vitro release and ex-vivo permeation studies. The shape and surface morphology of the prepared NLC was determined through transmission electron microscopy. To detect the interaction of the drug with carriers, compatibility studies were also carried out. Results: Average size and polydispersity index of developed formulation S6 was 227.0±6.3 nm and 0.460 respectively. The encapsulation efficiency of formulation S6 was found to be 87.25 %. The pH, viscosity, in-vitro mucoadhesion study, and in- vitro release of optimized olanzapine loaded NLC were recorded as 5.7 ± 0.05, 78 centipoise, 15±2 min, and 91.96 % respectively. In ex-vivo permeation studies, the percent drug permeated after 210 min was found to be 84.03%. Conclusion: These results reveal potential application of novel olanzapine-NLC in intranasal drug delivery system for treatment of schizophrenia.

In vitro release of protein from poly(butylcyanoacrylate) nanocapsules with an aqueous core

2004 ◽  
Vol 283 (5) ◽  
pp. 480-485 ◽  
Author(s):  
Sai Li ◽  
Yi He ◽  
Cao Li ◽  
Xiaobo Liu
Keyword(s):  
In Vitro Release ◽  
Aqueous Core ◽  
Vitro Release

scholarly journals Synergistic Effect of Ultrasound and Polyethylene Glycol on the Mechanism of the Controlled Drug Release from Polylactide Matrices

Polymers ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 880
Author(s):  
Wenting Bao ◽  
Xianlong Zhang ◽  
Hong Wu ◽  
Rong Chen ◽  
Shaoyun Guo
Keyword(s):  
Polyethylene Glycol ◽  
Controlled Release ◽  
Drug Release ◽  
Synergistic Effect ◽  
In Vitro Release ◽  
Structure And Properties ◽  
Melt Extrusion ◽  
Model Drug ◽  
Vitro Release

In this paper, the synergistic effect of ultrasound and polyethylene glycol (PEG) on the controlled release of a water soluble drug from polylactide (PLA) matrices was studied. When ultrasound was used following the hot melt extrusion (HME) of the PLA/model drug release system, the release of the model drug (Methylene Blue (MB)) from the PLA when immersed in phosphate buffered saline (PBS) was affected by the variation of the parameters of ultrasound. It was found that no more than 2% PLA dissolved during the in-vitro release study, and the release of the MB from the PLA was diffusion controlled and fit well with the Higuchi diffusion model. Polyethylene glycol (PEG), which has high hydrophilicity and rapid dissolution speed, was blended with the PLA during the melt extrusion to enhance the release of the MB. The analysis of the structure and properties of the in-vitro release tablets of PLA/PEG/MB indicated that the ultrasound could improve the dispersion of MB in the PLA/PEG blends and it could also change the structure and properties of the PLA/PEG blends. Due to the dissolution of the PEG in PBS, the release of the MB from the PLA/PEG drug carrier was a combination of diffusion and erosion controlled release. Thus a new mechanism combining of diffusion and erosion models and modified kinetics model was proposed to explain the release behavior.

Study on in vitro release patterns of fentanyl-loaded PLGA microspheres

2003 ◽  
Vol 20 (5) ◽  
pp. 569-579 ◽  
Author(s):  
S.-A. Seo ◽  
G. Khang ◽  
J. M. Rhee ◽  
J. Kim ◽  
H. B. Lee
Keyword(s):  
In Vitro Release ◽  
Plga Microspheres ◽  
Vitro Release

Reliability of a Single β-Thromboglobulin Measurement in a Diabetic Population : Importance of PGE1 in Anticoagulant Mixture

1987 ◽  
Vol 57 (02) ◽  
pp. 201-204 ◽  
Author(s):  
P Y Scarabin ◽  
L Strain ◽  
C A Ludlam ◽  
J Jones ◽  
E M Kohner
Keyword(s):  
In Vitro Release ◽  
Mean Value ◽  
Reliable Estimate ◽  
Diabetic Patients ◽  
Single Measurement ◽  
Diabetic Population ◽  
The Difference ◽  
Vitro Release

SummaryDuring the collection of samples for plasma β-thromboglobulin (β-TG) determination, it is well established that artificially high values can be observed due to in-vitro release. To estimate the reliability of a single β-TG measurement, blood samples were collected simultaneously from both arms on two separate occasions in 56 diabetic patients selected for a clinical trial. From each arm, blood was taken into two tubes containing an anticoagulant mixture with (tube A) and without (tube B) PGE!. The overall mean value of B-TG in tube B was 1.14 times higher than in tube A (p <0.01). The markedly large between-arms variation accounted for the most part of within-subject variation in both tubes and was significantly greater in tube B than in tube A. Based on the difference between B-TG values from both arms, the number of subjects with artifically high B-TG values was significantly higher in tube B than in tube A on each occasion (overall rate: 28% and 14% respectively). Estimate of between-occasions variation showed that B-TG levels were relatively stable for each subject between two occasions in each tube. It is concluded that the use of PGEi decreases falsely high B-TG levels, but a single measurement of B-TG does not provide a reliable estimate of the true B-TG value in vivo.

Preparation and In-vitro Evaluation of Fe3O4 Encapsulated by Chitosan Loaded Capecitabine Nanoparticles for the Treatment of Breast Cancer

2016 ◽  
Vol 6 (3) ◽  
Author(s):  
Shanmuganathan S. ◽  
Nigma S. ◽  
Anbarasan B. ◽  
Harika B.
Keyword(s):  
Fe3o4 Nanoparticles ◽  
Polymer Concentration ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
In Vitro Evaluation ◽  
Sem Image ◽  
Therapeutic Molecules ◽  
Dialysis Method ◽  
Vitro Release

Nanoparticulate Carriers which is biodegradable, biocompatible and bio adhesive have significant feasible applications for administration of therapeutic molecules. The present study was aimed to formulate and optimise Capecitabine loaded Chitosan-Fe3O4 Nanoparticles and to study the in-vitro evaluation by sigma dialysis method. Capecitabine loaded chitosan – Fe3O4 nanoparticles batches with different ratios of drug: polymer (1:1, 1:2, 1:3, 1:4, 1:5, 1:6) were prepared by ionic gelation method. Increase in polymer concentration increases the nanoparticle drug content. Entrapment efficiency was 60.12% with drug to polymer ratio F3 (1:3). In-vitro release was found to be 65.20% for 12 hrs. Capecitabine from chitosanFe3O4 nanoparticles SEM image reveals discrete spherical structure and particles with size range of 100-500nm. FTIR studies represent the functional groups present with no characteristics change in formulations. Samples stored at refrigerator conditions showed better stability compared with samples kept at other conditions during 8 weeks of storage.

Sign in / Sign up

Export Citation Format

Share Document