In Vitro-In Vivo Correlation of Indomethacin Release from Prolonged Release W/O/W Multiple Emulsion System

1993 ◽  
Vol 19 (15) ◽  
pp. 1965-1980 ◽  
Author(s):  
Suranjana Roy ◽  
Bijan K. Gupta
Keyword(s):  
Prolonged Release ◽  
Emulsion System ◽  
Multiple Emulsion

scholarly journals Biochemical, Ameliorative and Cytotoxic Effects of Newly Synthesized Curcumin Microemulsions: Evidence from In Vitro and In Vivo Studies

Nanomaterials ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 817
Author(s):  
Abbas Rahdar ◽  
Mohammad Reza Hajinezhad ◽  
Saman Sargazi ◽  
Maryam Zaboli ◽  
Mahmood Barani ◽  
...  
Keyword(s):  
Hepg2 Cells ◽  
Density Functional ◽  
Liver Enzymes ◽  
Elevated Serum ◽  
Ethyl Butyrate ◽  
Polymeric Chain ◽  
Prolonged Release ◽  
Advanced Therapies

Curcumin is known to exhibit antioxidant and tissue-healing properties and has recently attracted the attention of the biomedical community for potential use in advanced therapies. This work reports the formulation and characterization of oil-in-water F127 microemulsions to enhance the bioavailability of curcumin Microemulsions showed a high encapsulation efficiency and prolonged release. To investigate the interactions of curcumin with one unit of the polymeric chain of surfactant F127, ethyl butyrate, and sodium octanoate, as well as the interaction between ethyl butyrate and one unit of the F127 polymer chain, the Density Functional Theory (DFT) calculations at the M06-2X level of theory, were performed in water solution. The MTT assay was used to assess the cytotoxicity of free and encapsulated curcumin on non-malignant and malignant cell lines. Combination effects were calculated according to Chou-Talalay’s principles. Results of in vitro studies indicated that MCF7 and HepG2 cells were more sensitive to curcumin microemulsions. Moreover, a synergistic relationship was observed between curcumin microemulsions and cisplatin in all affected fractions of MCF7 and HepG2 cells (CI < 0.9). For in vivo investigation, thioacetamide-intoxicated rats received thioacetamide (100 mg/kg Sc) followed by curcumin microemulsions (30 mg/kg Ip). Thioacetamide-intoxicated rats showed elevated serum liver enzymes, blood urea nitrogen (BUN), and creatinine levels, and a significant reduction in liver superoxide dismutase (SOD) and catalase (CAT) activities (p < 0.05). Curcumin microemulsions reduced liver enzymes and serum creatinine and increased the activity of antioxidant enzymes in thioacetamide-treated rats in comparison to the untreated thioacetamide-intoxicated group. Histopathological investigations confirmed the biochemical findings. Overall, the current results showed the desirable hepatoprotective, nephroprotective, and anti-cancer effects of curcumin microemulsions.

scholarly journals Survival and Proliferation under Severely Hypoxic Microenvironments Using Cell-Laden Oxygenating Hydrogels

2021 ◽  
Vol 12 (2) ◽  
pp. 30
Author(s):  
Shabir Hassan ◽  
Berivan Cecen ◽  
Ramon Peña-Garcia ◽  
Fernanda Roberta Marciano ◽  
Amir K. Miri ◽  
...  
Keyword(s):  
Prolonged Release ◽  
Therapeutic Approaches ◽  
Encapsulated Cells ◽  
Hypoxic Conditions ◽  
Skeletal Myoblasts ◽  
Artificial Tissue ◽  
Delivery Platform ◽  
Living Tissues

Different strategies have been employed to provide adequate nutrients for engineered living tissues. These have mainly revolved around providing oxygen to alleviate the effects of chronic hypoxia or anoxia that result in necrosis or weak neovascularization, leading to failure of artificial tissue implants and hence poor clinical outcome. While different biomaterials have been used as oxygen generators for in vitro as well as in vivo applications, certain problems have hampered their wide application. Among these are the generation and the rate at which oxygen is produced together with the production of the reaction intermediates in the form of reactive oxygen species (ROS). Both these factors can be detrimental for cell survival and can severely affect the outcome of such studies. Here we present calcium peroxide (CPO) encapsulated in polycaprolactone as oxygen releasing microparticles (OMPs). While CPO releases oxygen upon hydrolysis, PCL encapsulation ensures that hydrolysis takes place slowly, thereby sustaining prolonged release of oxygen without the stress the bulk release can endow on the encapsulated cells. We used gelatin methacryloyl (GelMA) hydrogels containing these OMPs to stimulate survival and proliferation of encapsulated skeletal myoblasts and optimized the OMP concentration for sustained oxygen delivery over more than a week. The oxygen releasing and delivery platform described in this study opens up opportunities for cell-based therapeutic approaches to treat diseases resulting from ischemic conditions and enhance survival of implants under severe hypoxic conditions for successful clinical translation.

scholarly journals Fabrication, physicochemical characterization and preliminary efficacy evaluation of a W/O/W multiple emulsion loaded with 5% green tea extract

2013 ◽  
Vol 49 (2) ◽  
pp. 341-349 ◽  
Author(s):  
Tariq Mahmood ◽  
Naveed Akhtar ◽  
Barkat Ali Khan ◽  
Akhtar Rasul ◽  
Haji M. Shoaib Khan
Keyword(s):  
Green Tea ◽  
Storage Conditions ◽  
Green Tea Extract ◽  
Viscosity Data ◽  
Skin Protection ◽  
Multiple Emulsion ◽  
Multiple Emulsions ◽  
Tea Extract

Complex multiple emulsions have an excellent ability to fill large volumes of functional cosmetic agents. This study was aimed to encapsulate large volume of green tea in classical multiple emulsion and to compare its stability with a multiple emulsion without green tea extract. Multiple emulsions were developed using Cetyl dimethicone copolyol as lipophilic emulsifier and classic polysorbate-80 as hydrophilic emulsifier. Multiple emulsions were evaluated for various physicochemical aspects like conductivity, pH, microscopic analysis, rheology and these characteristics were followed for a period of 30 days in different storage conditions. In vitro and in vivo skin protection tests were also performed for both kinds of multiple emulsions i.e. with active (MeA) and without active (MeB). Both formulations showed comparable characteristics regarding various physicochemical characteristics in different storage conditions. Rheological analysis showed that formulations showed pseudo plastic behavior upon continuous shear stress. Results of in vitro and in vivo skin protection data have revealed that the active formulation has comparable skin protection effects to that of control formulation. It was presumed that stable multiple emulsions could be a promising choice for topical application of green tea but multiple emulsions presented in this study need improvement in the formula, concluded on the basis of pH, conductivity and apparent viscosity data.

Formulation and Characterization of Transethosomes for Enhanced Transdermal Delivery of Propranolol Hydrochloride

2020 ◽  
Vol 12 (1) ◽  
pp. 38-47 ◽  
Author(s):  
Lalit Kumar ◽  
Puneet Utreja
Keyword(s):  
Plasma Concentration ◽  
Skin Permeation ◽  
Laser Scanning Microscopy ◽  
Prolonged Release ◽  
Propranolol Hydrochloride ◽  
Oral Tablet ◽  
In Vitro Skin Permeation ◽  
Oral Propranolol

Objective: The objective of the present work was to develop transethosomes loaded with propranolol hydrochloride using Lipoid S100 as phospholipid, and oleic acid as permeation enhancer and evaluate them for prolonged release effect, in-vitro skin permeation, and in-vivo plasma concentration. Methods: Transethosomes loaded with propranolol hydrochloride were prepared by homogenization method. Furthermore, they were characterized by using Transmission Electron Microscopy (TEM), zeta sizer, Differential Scanning Calorimetry (DSC), and Confocal Laser Scanning Microscopy (CLSM) for in-vitro skin permeation. Plasma concentration profile of transethosomal gel was determined using Sprague Dawley rats and compared with a marketed oral tablet of propranolol hydrochloride. Results: Developed transethosomes loaded with propranolol hydrochloride showed acceptable size (182.7 ± 5.4 nm), high drug entrapment (81.98 ± 2.9%) and good colloidal characteristics [polydispersity index (PDI) = 0.234 ± 0.039, zeta potential = -21.91 ± 0.65 mV]. Transethosomes showed prolonged in-vitro release of propranolol hydrochloride for 24 h. Results of in-vitro skin permeation studies of transethosomal gel showed 74.34 ± 2.33% permeation of propranolol hydrochloride after 24 h and confocal microscopy revealed accumulation of transethosomes in the stratum basale layer of the skin. Transethosomal gel was capable to prolong the in-vivo release of propranolol hydrochloride upto 24 h. The value of peak plasma concentration (Cmax) of propranolol hydrochloride was found to be 93.8 ± 3.6 ng/mL which was very high compared to the marketed oral tablet of propranolol hydrochloride (45.6 ± 3.1 ng/mL). Conclusion: The results suggested that transethosomal gel of propranolol hydrochloride could be a better alternative to oral propranolol hydrochloride as it can avoid various disadvantages of oral propranolol hydrochloride like high dosing frequency, first pass effect, and organ toxicity.

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.

scholarly journals Preparation and evaluation of chitosan based thermoreversible gels for intraperitoneal delivery of 5-fluorouracil (5-FU)

2013 ◽  
Vol 63 (4) ◽  
pp. 479-491 ◽  
Author(s):  
Bhavesh P. Depani ◽  
Anuja A. Naik ◽  
Hema A. Nair
Keyword(s):  
Antineoplastic Agent ◽  
In Vitro Cytotoxicity ◽  
In Vivo Studies ◽  
Comparable Efficacy ◽  
Prolonged Release ◽  
Fibroblast Cells ◽  
Glycerol Phosphate ◽  
Drug Free

Abstract Sterile thermoreversibly gelling systems based on chitosan- glycerol phosphate were developed for intraperitoneal delivery of the antineoplastic agent 5-FU. The formulation was evaluated for gelling characteristics and in vitro drug release. Drug free gels were evaluated for in vitro cytotoxicity in L-929 mouse fibroblast cells. Drug loaded gels were subjected to acute toxicity studies in Swiss albino mice via intraperitoneal route and efficacy studies via intratumoral injections in subcutaneous colon carcinoma bearing BALB/c mice. The formulations gelled reversibly in 8 min at 37 °C and provided prolonged release of the drug. Drug free systems showed dose dependent cytotoxicity in fibroblast cells, while in vivo studies revealed a 2.8-fold increase in LD50 of 5-FU administered intraperitoneally as the developed system. Tumor volume measurements showed comparable efficacy of 5-FU administered as gel and commercial injection with a greatly improved safety profile of the former as adjudged from mortality and body weight measurements.

In vitro/in vivo correlation of prolonged release dosage forms containing diltiazem HCl

1993 ◽  
Vol 14 (2) ◽  
pp. 143-160 ◽  
Author(s):  
C. Caramella ◽  
F. Ferrari ◽  
M. C. Bonferoni ◽  
M. E. Sangalli ◽  
M. De Bernardi Di Valserra ◽  
...  
Keyword(s):  
Dosage Forms ◽  
Prolonged Release ◽  
Diltiazem Hcl

scholarly journals Preparation of Liposomal Formulations for Ocular Delivery of Thymoquinone: In Vitro Evaluation in HCEC-2 e HConEC Cells

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2093
Author(s):  
Elisa Landucci ◽  
Francesca Bonomolo ◽  
Chiara De Stefani ◽  
Costanza Mazzantini ◽  
Domenico Edoardo Pellegrini-Giampietro ◽  
...  
Keyword(s):  
Epithelial Cells ◽  
Therapeutic Potential ◽  
Nigella Sativa ◽  
Pigment Epithelium ◽  
Retinal Pigment ◽  
Fold Increase ◽  
Prolonged Release ◽  
Liposomal Formulations

Thymoquinone (TQ) is the main constituent of Nigella sativa L. essential oil. In vitro studies have shown its protective effect against H2O2-induced oxidative stress in human retinal pigment epithelium cells, and in vivo experiments have demonstrated its effect in decreasing corneal neovascularization and reducing the inflammation in an experimental dry eye model in mice. Its therapeutic use is limited by poor bioavailability, low solubility, and scarce permeability. In this study, two liposomal formulations have been developed, both of which consist of phosphatidylcholine and Plurol Oleique, a liquid lipid, and one of which is coated with 0.1% w/v hyaluronic acid (HA) to increase both TQ solubility and its ocular therapeutic potential. Each formulation has a size <200 nm and an EE% around 70%, determined by scattering techniques and the HPLC-DAD analytical method, respectively, and they result in a 2-fold increase in TQ solubility. HA-coated liposomes are stable over 2 months at +4 °C, and coated and uncoated liposomes present a gradual and prolonged release of TQ. Two cell lines, human corneal epithelial cells (HCEC-2) and human conjunctival epithelial cells (HConEC) were used to investigate the safety of the liposomal formulations. Uptake studies were also performed using fluorescent liposomes. Both liposomes and, in particular, HA-coated liposomes reduce the TQ toxicity observed at high doses in both HCEC-2 and HConEC cells, and both formulations increase the absorption at the cellular level and especially at the nucleus level, with a more pronounced effect for HA-coated liposomes.

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