scholarly journals In Vitro Intestinal Permeability Studies and Pharmacokinetic Evaluation of Famotidine Microemulsion for Oral Delivery

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Sajal Kumar Jha ◽  
Roopa Karki ◽  
Venkatesh Dinnekere Puttegowda ◽  
D. Harinarayana
Keyword(s):  
Intestinal Permeability ◽  
Oral Delivery ◽  
Tween 80 ◽  
Absolute Bioavailability ◽  
Microemulsion System ◽  
Standard Drug ◽  
Peg 400 ◽  
Permeability Studies ◽  
In Vitro Intestinal Permeability

The absolute bioavailability of famotidine after oral administration is about 40–45% and absorbance only in the initial part of small intestine may be due to low intestinal permeability. Hence, an olive oil based microemulsion formulation with Tween-80 as surfactant and PEG-400 as cosurfactant was developed by using water titration method with the aim of enhancing the intestinal permeability as well as oral bioavailability. In vitro drug permeation in intestine after 8 h for all formulations varied from 30.42% to 78.39% and most of the formulations showed enhanced permeation compared to pure drug (48.92%). Famotidine microemulsion exhibited the higher absorption and Cmax⁡ achieved from the optimized famotidine formulation (456.20 ng·h/ml) was higher than the standard (126.80 ng·h/mL). It was found that AUC0–24 h obtained from the optimized famotidine test formulation (3023.5 ng·h/mL) was significantly higher than the standard famotidine (1663.3 ng·h/mL). F-1 demonstrated a longer (6 h) Tmax⁡ compared with standard drug (2 h) and sustained the release of drug over 24 h. The bioavailability of F-1 formulation was about 1.8-fold higher than that of standard drug. This enhanced bioavailability of famotidine loaded in microemulsion system might be due to increased intestinal permeability.

scholarly journals Pharmacodynamics and Pharmacokinetics Evaluation of Ranitidine Microemulsion on Experimental Animals

2014 ◽  
Vol 2014 ◽  
pp. 1-6
Author(s):  
Sajal Kumar Jha ◽  
Roopa Karki ◽  
Venkatesh Dinnekere Puttegowda ◽  
Amitava Ghosh
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Intestinal Permeability ◽  
Delivery System ◽  
Oral Delivery ◽  
Tween 80 ◽  
Standard Drug ◽  
Alternative Drug ◽  
And Control ◽  
Antiulcer Therapy

Ranitidine microemulsion was investigated for its pharmacodynamic and pharmacokinetic evaluation to find out the suitability of microemulsion as a potential drug delivery system in the treatment of ulcer. The bioavailability of ranitidine after oral administration is about 50% and is absorbed via the small intestine; this may be due to low intestinal permeability. Hence the aim of present investigation was to maximize the therapeutic efficacy of ranitidine by developing microemulsion to increase the intestinal permeability as well as bioavailability. A ground nut oil based microemulsion formulation with Tween-80 as surfactant and PEG-400 as cosurfactant was developed for oral delivery of ranitidine and characterized for physicochemical parameters. In pharmacodynamic studies, significant (P<0.05) variation in parameters estimated was found between the treated and control groups. Ranitidine microemulsion exhibited higher absorption and Cmax (863.20 ng·h/mL) than the standard (442.20 ng/mL). It was found that AUC0–24 hr obtained from the optimized ranitidine test formulation (5426.5 ng·h/mL) was significantly higher than the standard ranitidine (3920.4 ng·h/mL). The bioavailability of optimized formulation was about 1.4-fold higher than that of standard drug. This enhanced bioavailability of ranitidine microemulsion may be used as an effective and alternative drug delivery system for the antiulcer therapy.

scholarly journals DEVELOPMENT OF MICROEMULSION FORMULATION FOR ORAL DELIVERY OF ROSUVASTATIN CALCIUM

2020 ◽  
pp. 35-39
Author(s):  
Himanshu Paliwal ◽  
Ram Singh Solanki ◽  
Chetan Singh Chauhan
Keyword(s):  
Zeta Potential ◽  
Droplet Size ◽  
Oral Delivery ◽  
Water Solubility ◽  
Tween 80 ◽  
In Vitro Dissolution ◽  
Microemulsion Formulation ◽  
Polyethylene Glycol 400 ◽  
Rosuvastatin Calcium

The purpose of conducting this study was to prepare an oral microemulsion formulation of Rosuvastatin calcium (RC) to improve its water solubility. Oil in water microemulsion was formulated using Oleic acid, Tween 80 and Polyethylene Glycol-400(PEG-400) as oil, surfactant and co-surfactant, respectively. The ideal proportion of surfactant: co-surfactant (Smix) was chosen by constructing pseudoternary diagrams. The microemulsion formulations which proved to be stable after thermodynamic stability testing were further evaluated for physical characteristics. Selected formulations were evaluated for droplet size, zeta potential, polydispersity index, viscosity and % drug content. The results were suggestive that optimized microemulsion formulation (F2) was thermodynamically stable and clear having a droplet size of 74.29 nm and zeta potential of -18.44.  In vitro dissolution study for optimized microemulsion was performed using a dialysis bag method and cumulative % drug release was determined. The result from the release study was indicative of improved solubility of Rosuvastatin calcium which may serve to boost up the oral bioavailability of drug.

scholarly journals A PREPARATION, CHARACTERIZATION, AND IN VITRO SKIN PENETRATION OF MORUS ALBA ROOT EXTRACT NANOEMULSION

2019 ◽  
pp. 292-296
Author(s):  
MAZAYA FADHILA ◽  
ABDUL MUN IM ◽  
MAHDI JUFRI
Keyword(s):  
Phase Diagram ◽  
Tween 80 ◽  
Skin Penetration ◽  
Morus Alba ◽  
Root Extract ◽  
Peg 400 ◽  
In Vitro Skin Penetration ◽  
White Mulberry ◽  
Pseudoternary Phase Diagram

Objective: White mulberry (Morus alba) root extract has terpenoid, flavonoid, and stilbene compounds. The stilbenes, oxyresveratrol and resveratrol, have antioxidant and antityrosinase activities. Nanocarriers can help active ingredients to be delivered in a more efficient manner. The advantages of nanoemulsion on products include increased penetration, biocompatibility, and low toxicity due to its non-ionic properties and have the ability to combine the properties of lipophilic and hydrophilic active ingredients. The objective of this study was to prepare, characterize, and evaluate the in vitro skin penetration of M. alba root extract nanoemulsion. Methods: The M. alba root extract was prepared by ionic liquid-based microwave-assisted extraction method. Nanoemulsion was optimized and prepared using virgin coconut oil (VCO), Tween 80, and polyethylene glycol 400 (PEG 400) by aqueous phase-titration method to construct pseudoternary phase diagram. M. alba root extract nanoemulsion was characterized for droplet size, viscosity, zeta potential, and physical stability tests for 12 weeks. In vitro skin penetration of oxyresveratrol from nanoemulsion was determined by the Franz diffusion cell and was compared by macroemulsion preparation, then analyzed by high-performance liquid chromatography method. Results: Based on pseudoternary phase diagram, nanoemulsion of white mulberry root extract contained of 2% VCO and 18% mixture of surfactant Tween 80 and PEG 400 (1:1) was chosen. Nanoemulsion has average globule size of 81.61 nm, with polydispersity index 0.22, and potential zeta −1.56 mV. The cumulative penetration of oxyresveratrol from nanoemulsion was 55.86 μg/cm2 with flux of 6.53 μg/cm2/h, while regular emulsion was 32.45 μg/cm2 with flux of 3.5501 μg/cm2/h. Conclusion: Nanoemulsion of white mulberry root extract was penetrated deeper than regular emulsion.

scholarly journals FORMULATION AND CHARACTERIZATION OF SELF EMULSIFYING DRUG DELIVERY SYSTEM OF SPIRONOLACTONE

1970 ◽  
Vol 7 (1) ◽  
pp. 38-40
Author(s):  
Ankur Gupta ◽  
Arpna Indurkhya ◽  
S.C Chaturvedi ◽  
Ajit Varma
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Absorption ◽  
Tween 80 ◽  
Water Soluble ◽  
Absolute Bioavailability ◽  
Polyethylene Glycol 400

Spironolactone is aldosterone antagonist drug belonging to the category of potassium sparing diuretics administered orally that has absolute bioavailability of only 68% due to the poor aqueous solubility. The main aim of the present work was to develop a self emulsifying drug delivery system (SEDDS) to enhance the oral absorption of spironolactone. The solubility of spironolactone in various oils, surfactants, and co surfactants was determined. Pseudo ternary phase diagrams were constructed using castor oil, Tween 80, and polyethylene glycol 400, and distilled water to identify the efficient self-micro emulsion region. Prepared self emulsifying drug delivery system was further evaluated for its emulsification time, drug content, optical clarity, droplet size, zeta potential, in vitro drug release. The results showed that 96.16% drug was released from the SEDDS formulation in 3 hrs. This demonstrated an enhancement in the drug release and thereby, absorption of the drug through the membrane, this was significantly higher than that of the plain drug suspension. Thus, the above findings support that the utility of SEDDS to enhance solubility and dissolution of poorly water soluble compounds which may result in improved Therapeutic performance.

scholarly journals In Vitro Evaluation of Eudragit Matrices for Oral Delivery of BCG Vaccine to Animals

2019 ◽  
Author(s):  
Imran Saleem ◽  
Allan Coombes ◽  
Mark Chambers
Keyword(s):  
Oral Delivery ◽  
Freeze Drying ◽  
Tween 80 ◽  
Gastric Fluid ◽  
Powder Compaction ◽  
Bcg Vaccine ◽  
Simulated Gastric Fluid ◽  
Physical Damage ◽  
Freeze Dried

Bacillus Calmette-Gu&eacute;rin (BCG) vaccine is the only licensed vaccine against tuberculosis (TB) in humans and animals. It is most commonly administered parenterally but oral delivery is highly advantageous for immunisation of cattle and wildlife hosts of TB in particular. Since BCG is susceptible to inactivation in the gut, vaccine formulations were prepared from suspensions of Eudragit L100 copolymer powder and BCG in PBS, containing Tween 80, with and without the addition of mannitol or trehalose. Samples were frozen at -20oC, freeze-dried and the lyophilised powders were compressed to produce BCG-Eudragit matrices. Production of the dried powders resulted in a reduction in BCG viability. Substantial losses in viability occurred at the initial formulation stage and at the stage of powder compaction. Data indicated that the Eudragit matrix protected BCG against simulated gastric fluid (SGF). The matrices remained intact in SGF and dissolved completely in SIF within three hours. The inclusion of mannitol or trehalose in the matrix provided additional protection to BCG during freeze-drying. Control needs to be exercised over BCG aggregation, freeze-drying and powder compaction conditions to minimise physical damage of the bacterial cell wall and maximise the viability of oral BCG vaccines prepared by dry powder compaction.

scholarly journals Formulation and evaluation of self nano-emulsifying drug delivery system of ezetimibe for dissolution rate enhancement

2020 ◽  
Vol 11 (2) ◽  
pp. 1294-1301
Author(s):  
Geethanjali K ◽  
Vaiyana Rajesh C
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Dissolution Rate ◽  
Delivery System ◽  
Tween 80 ◽  
In Vitro Dissolution ◽  
Cinnamon Oil ◽  
Peg 400 ◽  
Solid Form

The present study was aimed to develop a Self Nano Emulsifying Delivery System of Ezetimibe (EZM) for enhancing its dissolution rate. Ezetimibe is a cholesterol absorption inhibitor, being a lipophilic drug due to its low solubility EZM shows a low dissolution profile. The SNEDDS formulation consisted of excipients Cinnamon oil, Tween 80, PEG 400 as the Oil, Surfactant and Co-surfactant. Twelve formulations with different ratios of Oil, Surfactant and Co-surfactant were prepared. The liquid SNEDDS were then converted into Solid form by adsorption technique using Avicel PH 101 and Aerosil 200 as adsorbents. The liquid SNEDDS was characterised for Particle size, Emulsification time, Dispersibility, percentage transmittance, PCM, Centrifugation, Cloud Point and Freeze thaw cycle. The solid form was characterized for the flow property, SEM, Drug content and in-vitro dissolution. Among the twelve formulations F6 formulation was found to have a particle size of 196 nm and PDI of 0.123. F6 formulation was selected as the best and it was made into solid by adsorption onto solid carriers. The F6 formulation consisted of the 25% Cinnamon oil, 50% tween 80 and 25% PEG 400. The in-vitro dissolution rate of the prepared formulation was compared with the marketed formulation. The in-vitro dissolution data showed that the drug release at the end of 60 mins from marketed formulation was 63.75 % and from SNEDDS formulation was         90.62 %. The dissolution rate of the prepared SNEDDS was increased by 1.42 times than the marketed formulation. The increase in the dissolution rate shows that SNEDDS is a suitable drug delivery system to enhance the rate of dissolution of Ezetimibe.

scholarly journals Formulation and Evaluation of Galantamine Hydrobromide Proniosome Gel for Alzheimer’s disease

2020 ◽  
Vol 10 (2-s) ◽  
pp. 68-74
Author(s):  
Mohammed Sarfaraz ◽  
Tanvi Goel ◽  
H. Doddayya
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Phase Separation ◽  
Oral Delivery ◽  
Tween 80 ◽  
Separation Method ◽  
Tween 20 ◽  
Drug Diffusion ◽  
Diffusion Studies

Galantamine hydrobromide is formulated in tablets and capsules prescribed through oral delivery for the treatment of Alzheimer’s disease. However, oral delivery of drugs can cause severe side effects such as nausea, vomiting, and gastrointestinal disturbance. In the present research work, Galantamine hydrobromide is formulated as proniosome gel by Coacervation phase separation method using different surfactants such as Tweens and Spans. Overall eight formulations were developed and evaluated for various parameters. The prepared gels were viewed by naked eye to observe the colour of gel. Microscopical observations of the gels showed vesicles of optimum size from 3.030 mm (P2) - 3.735 mm (P5). The gel also showed optimum rate of spontaneity in the range 9.60 mm3x1000 (P7) to 11.80 mm3x1000 (P4) and entrapment efficiency of vesicles in the range 66.15% (P5) to 86.92% (P3). The gels had pH in suitable range of skin (5.92-6.9). The in vitro drug diffusion studies revealed that the drug diffusion was affected by the various surfactants used. The rank order of surfactant effect on in-vitro drug diffusion was Tween 80 > Tween 60 > Tween 40 >Tween 20 > Span 80 > Span 60 > Span 40 > Span 20. The proniosomal gel containing Tween 80 showed maximum drug diffusion (99.24%) and the gel containing Span 20 showed minimum drug diffusion (71.74%). FT-IR studies of optimized proniosome gel P8 revealed the absence of any chemical interactions between drug and carriers used. Keywords: Galantamine hydrobromide, Proniosome gel, Coacervation phase separation method,   Surfactants, in vitro drug diffusion studies.

Hybrid Liquisolid technique: A novel approach to enhance the in-vitro performance of antidiabetic drugs

2021 ◽  
Vol 16 ◽  
Author(s):  
Saloni Dalwadi ◽  
Vaishali T. Thakkar ◽  
Hardik B. Rana
Keyword(s):  
Tween 80 ◽  
Fixed Dose ◽  
Coating Materials ◽  
Boswellia Serrata ◽  
Peg 400 ◽  
Kneading Method ◽  
The Impact ◽  
In Vitro Performance

Background: A combination of Glimepiride and Boswellia serrata extract reduces Neuropathic diabetic complications by reducing the peroxidase level and improving the antioxidant level. The hybrid Liquisolid method includes a combination of two methods, kneading and the Liquisolid method to enhance drug in-vitro performance. Objective: The objective of this study was to enhance the in-vitro performance of antidiabetics drugs. Method: Tablets of the fixed dose combination of Glimepiride and Boswellia serrata extract were formulated by kneading method followed by Liquisolid method. Screening of non-volatile solvents, carriers, and coating materials was performed. The design of the experiment was applied to optimize the formulation and validation was done to validate the obtained model from the design of the experiment. 3 level 2 factorial (32) Design was applied by using Design expert software 11. Various pre-compression parameters were performed to check the quality of the formulation. Results: Screening of excipients for kneading method, Glimepiride with PVP K 30 (5%), and Boswellia serrata extract with Poloxamer 188 (13%) give optimum drug release. For the Liquisolid method Propylene glycol: PEG 400: Tween 80 (1:2:4) ratio for Glimepiride and PEG 400: Tween 80 (1:3) ratio for Boswellia serrata extract were selected. Common carrier and coating material for both drug Syloid XDP 3150: Aeroperl 300 (3:1) ratio were selected, which improves the in-vitro performance of the drug. Conclusion: This study gives an overall understanding of the impact of excipients on the quality of formulation, a critical knowledge to the implementation of this kind of novel application of Liquisolid systems.

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