scholarly journals Bosentan loaded Microemulsion: A novel formulation and evaluation of their in-vitro and in-vivo characteristic

2020 ◽  
pp. 464-472
Author(s):  
Bhupendra Prajapati ◽  
Umang Varia
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Spherical Shape ◽  
Pulmonary Artery Hypertension ◽  
Tween 20 ◽  
Globule Size ◽  
Pure Drug ◽  
The Stability

The main objective of the research work was to improve the solubility of Bosentan by preparing Microemulsion (ME) for pulmonary artery hypertension therapy. Capmul MCM C8 was selected as oil, Tween 20 as a surfactant and Transcutol HP as a co-surfactant. From Pseudoternary phase diagram ratio of Smix (1:1) selected. From the Microemulsion area of ternary diagram different batches were prepared, but the drug was precipitate from the formulation which can be avoid by adding precipitate inhibitor. Pluronic F 127 was utilized as precipitate inhibitor in the concentration of 1.5%. The optimized formulation ME 8 contain oil (30 %V/V), Smix (60 %V/V) and water (10 %V/V). The prepared Microemulsion evaluated for globule size 96.71±0.11 nm, % transmittance 99.45±0.54 % and >99 % drug content. TEM confirm the spherical shape of globule. The physicochemical parameter of ME 8 was performed and to enhance the stability of Microemulsion it is converted in to solid ME by using adsorbent. Aeroperl 300 was selected as an adsorbent in the drug to adsorbent ratio (1:0.5 %W/W) based on physicochemical properties. From the in-vitro drug release investigation after 7 hours %CDR of ME 8 was found to be 78.87±0.17% and solid Microemulsion (SME 3) shows 76.83±0.29%. The pure drug shows only 27.63±0.23% CDR, which indicate that ME revealed better drug release than pure drug. There was a 2.8 fold increases in solubility compare to pure drug. From the In-vivo data compared to convention formulation, there was significant change in pharmacokinetics data observed.

scholarly journals Design and in vivo Evaluation of Manidipine by Self-Nanoemulsifying Drug Delivery Systems

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
S Srikanth Reddy ◽  
G Suresh
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Spherical Shape ◽  
Pharmacokinetic Studies ◽  
In Vivo Evaluation ◽  
Enhanced Solubility ◽  
Pure Drug

The current research is aimed at developing liquid self-nanoemulsifying drug delivery system (liquid-SNEDDS) of Manidipine for enhanced solubility and oral bioavailability. The Manidipine SNEDDS are formulated with excipients comprising of Capmul MCM (oil phase), Transcutol P (surfactant) Lutrol L 300 as co-surfactant. The prepared fifteen formulations of Manidipine SNEDDS analysed for emulsification time, percentage transmittance, particle size, in vitro drug release, and stability studies. In vivo pharmacokinetic studies of the optimized formulation were carried out in Wistar rats in comparison with control (pure drug). The morphology of Manidipine SNEDDS indicates spherical shape with uniform particle distribution. The percentage drug release from optimized formulation F14 is 98.24 ± 5.14%. The particle size F14 formulation was 22.4 nm and Z-Average 23.3 nm. The PDI and zeta potential of Manidipine SNEDDS optimized formulation (F14) were 0.313 and-5.1mV respectively. From in vivo bioavailability data the optimized formulation exhibited a significantly greater Cmax and Tmax of the SNEDDS was found to be 3.42 ± 0.46ng/ml and 2.00 ± 0.05 h respectively. AUC0-∞ infinity for formulation was significantly higher (11.25 ± 3.45 ng.h/ml) than pure drug (7.45 ± 2.24ng. h/ml). Hence a potential SNEDDS formulation of Manidipine developed with enhanced solubility and bioavailability.

scholarly journals Preparation and preclinical evaluation of aceclofenac loaded pectinate mucoadhesive microspheres

2012 ◽  
Vol 2 (1) ◽  
pp. 8 ◽  
Author(s):  
Santanu Chakraborty ◽  
Priyanka Nayak ◽  
Bala Murali Krishna ◽  
Madhusmruti Khandai ◽  
Ashoke Kumar Ghosh
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Polymer Concentration ◽  
Research Work ◽  
In Vivo Studies ◽  
Systemic Absorption ◽  
Cross Linking ◽  
Significant Difference

The aim of the present research work was to fabricate aceclofenac loaded pectinate microspheres by ionic gelation method and evaluate the effect of different cross-linking agents and polymer concentration on particle size, encapsulation efficacy and drug release behavior. It was also investigated that whether this pectinate dosage form was able to target the drug release in intestinal region and prevent the different side effect associated with the drug in stomach or not. It was observed that particle size, encapsulation efficacy and in vitro drug release were largely depended on polymer concentration and cross-linking agents. It was also observed that pectinate microspheres showed excellent pH depended mucoadhesive properties and they were able to restrict the drug release in stomach. <em>In vitro</em> drug release study showed that alminium-pectinate microspheres have more sustaining property as compared to barium-pectinate microspheres. Holm-Sidak multiple comparison analysis suggested a significant difference in measured t<sub>50%</sub> values among all the formulations with same cross-linking agent. In vivo studies revealed that the anti inflammatory and analgesic effects induced by pectinate microspheres were significantly high and prolonged as compared to pure drug. So, pectinate microspheres can be an excellent carrier for targeting the delivery of aceclofenac as well as help in improving the patient compliance by prolonging the systemic absorption.

scholarly journals FORMUALTION AND DEVELOPMENT OF MUCOADHESIVE SUSTAINED RELEASE BUCCAL TABLETS AND PATCHES OF 5-FLUOROURACIL USING DIFFERENT POLYMERS

2018 ◽  
Vol 11 (5) ◽  
pp. 174
Author(s):  
Nitin Gawai ◽  
Zahid Zaheer
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Research Work ◽  
Sodium Deoxycholate ◽  
Content Uniformity ◽  
Design Expert ◽  
Buccal Tablet ◽  
Buccal Tablets

 Objective: The present research study was undertaken to formulate mucoadhesive sustained release buccal tablets and patches of 5-fluorouracil (5-FU).Method: For the research experiment work design expert software version 10, stat-ease, Inc. has been used. A 32 full factorial design was selected for the formulation of the buccal tablet as well as buccal patches. In this research work, formulated tablets and patches using different polymers such as carbopol 974p, polyvinylpyrrolidone-K 30, sodium deoxycholate, microcrystalline cellulose, and polyvinyl alcohol. An after formulation of batches formulated products studied for characterization, namely, Fourier transform infrared (FTIR) and differential scanning calorimeter (DSC). Evaluation parameters studied such as weight uniformity, thickness, hardness, friability, and content uniformity also carried out. For drug release purpose from the formulation of buccal tablet and patches in vitro drug released performed. In vivo drug releases study also carried out using Rabbit for drug reaction point of view.Results: Design expert showed the significant results on independent and dependent variables. The R-Squared 0.9943 for drug release and 0.9985 for swelling index is in reasonable agreement with the formulations. FTIR and DSC indicating compatibility of the drug and polymers in the tablet formulation and patch formulations at the molecular level. The drug release of buccal tablet showed 75.10–99.34% and buccal patches showed 58.41–81.43%. These formulations showed good results when compared to the conventional tablet.Conclusion: Formulation of mucoadhesive sustained release buccal tablets and patches of 5-FU successfully done using different polymers, which would definitely help in increasing bioavailability of the drug.

scholarly journals Development and Optimization of Proniosomal Gel Containing Etodolac: In-vitro, Ex-vivo and In-vivo Evaluation

2021 ◽  
Vol 62 (3) ◽  
pp. 290-304
Author(s):  
Moreshwar Patil ◽  
Prashant Pandit ◽  
Pavan Udavant ◽  
Sandeep Sonawane ◽  
Deepak Bhambere
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
In Vivo Evaluation ◽  
Vesicle Size ◽  
Skin Delivery ◽  
The Stability

Introduction: Etodolac is used in the treatment of acute pain and inflammation. It has low solubility because of high hydrophobicity and it is reported that upon oral administration shows gastric disturbances. This encourages the development of topical vesicular formulation. Method: In this work we used coacervation-phase separation method for the development of etodolac loaded vesicular system by using non-ionic surfactants, cholesterol and soya lecithin. Central composite design (rotatble) was used to optimize the concentrations of soy lecithin, surfactant and cholesterol. The prepared formulations were characterized by number of vesicles formed, vesicle size, zeta potential, entrapment efficiency, in-vitro permeation, ex-vivo permeation and anti-inflammatory study. Results: Etodolac was successfully entrapped in all formulations having efficiency in the range of 74.36% to 90.85%, which was more at 4 °C than room temperature. When hydrated with water; niosome in the range of 54 to 141 (per cubic mm) were spontaneously produced. The results of in-vitro diffusion study revealed that etodolac was released in the range of 71.86 to 97.16% over a period of 24 hrs. The average vesicle size of optimized formulation was found 211.9 nm with PDI of 0.5. The observed responses i.e. % encapsulation efficiency and drug release were 74.12 and 95.08 respectively. The zeta potential was -19.4mV revealed the stability of formulation which was further confirmed by no changes in drug content and drug release after stability studies. The % inhibition in paw volume was 40.52% and 43.61% for test and marketed proniosomal gel. Conclusion: Proniosomal gel formulation was stable and could enhance skin delivery of etodolac because of excellent permeation capability of vesicular system.

scholarly journals DESIGN AND EVALUATION OF SELF-NANO EMULSIFYING DRUG DELIVERY SYSTEMS OF ALVERINE FOR ENHANCEMENT OF SOLUBILITY

2021 ◽  
Vol 12 (7) ◽  
pp. 25-31
Author(s):  
Pooja . ◽  
Pankaj Kumar Sharma ◽  
Viswanath Agrahari
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Ethyl Oleate ◽  
Spherical Shape ◽  
Tween 80 ◽  
In Vitro Dissolution ◽  
Transmission Electron ◽  
The Stability

Background: The aim of this study is to develop a liquid self-nano emulsifying drug delivery system for alverine (liquid-SNEDDS).Excipients in the alverine SNEDDS include Ethyl oleate as the oil phase, Tween 80 as a surfactant, and PEG600, Propylene glycol as a cosurfactant.The prepared eleven formulations of alverine SNEDDS were performed for emulsification time, percentage transmittance, particle size, drug release, in vitro dissolution and stability studies.The optimised alverine liquid SNEDDS formulation (D1) was studied for drug-excipient compatibility using infrared spectroscopy, as well as particle size, zeta potential, transmission electron microscopy, and stability. Alverine SNEDDS have a spherical shape with uniform particle distribution, according to their morphology. D1's optimised formulation's drug release percentage (96.6). The stability data revealed no discernible changes in drug content, emulsifying properties, drug release, or appearance. As a result, a potential SNEDDS formulation of alverine with improved solubility, dissolution rate, and bioavailability was developed.

scholarly journals IMPROVED CIPROFLOXACIN PENETRATION IN GOAT EYES USING COMPLEXATION TECHNIQUE

2019 ◽  
pp. 168-171
Author(s):  
DURGA PANDEY ◽  
DEEPTI JAIN
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Penetrating Trauma ◽  
Spherical Shape ◽  
High Energy ◽  
Ion Pair ◽  
Precipitation Method ◽  
Globule Size ◽  
Sustain Release

Objective: The objective of the present work was to improve the retention and penetration of ciprofloxacin (CF) ion pair entrapped within submicron emulsion (SE) in goat eyes and characterize the SE for improvement of ocular activity. The developed delivery system resulted with prolonged drug release as compared to the conventional dosage form. Methods: SE prepared by high-energy emulsification and sonication to obtain uniform globule size. Ion-pair complex is prepared by precipitation method. Results: Average internal droplets size of the optimized formulation was 0.300 μm, pH of the optimized formulation was 6.4±0.7 (average of three determinations) and viscosity 3.2±0.3 cP suitable for ocular use. Entrapment was 92.12%. In vitro drug release pattern in dialysis membrane showed sustain release of CF, a cumulative percent release of CF was found 77% in 10 h. Scanning electron microscopy showed spherical shape and size within 1 μm. In vitro release in goat eyes was found 35.86 % for optimized formulation compared to market, 26.83% in 60 min. Conclusion: Developed optimized formulation can be a good candidate for ocular drug delivery in severe ocular infections where frequent dosing required such as endophthalmitis, corneal ulcer, and penetrating trauma.

Development, characterization and optimization of polymeric mucoadhesive microcapsules containing anticancer agent using response surface method: in vitro and in vivo study

2020 ◽  
Vol 11 (3) ◽  
pp. 3429-3442
Author(s):  
Chinmaya Mahapatra ◽  
Padala Narasimha Murthy ◽  
Anjan Kumar Mahapatra ◽  
Sudhir Kumar Sahoo ◽  
Prasanna Kumar Dixit
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Area Under The Curve ◽  
In Vitro Drug Release ◽  
Colon Cancer Cell Lines ◽  
Percentage Yield ◽  
Swelling Characteristics ◽  
Mixing Proportion

The present research work covenants the preparation, characterisation and optimisation of mucoadhesive microcapsules containing paclitaxel through ionic gelation method using 32 statistical factorial designs. The effect of mixing proportion of primary polymer sodium alginate to copolymer (X1) and speed of magnetic stirrer (X2) on the microcapsules size (Y1), efficiency of paclitaxel encapsulation (Y2), and percentage yield (Y3) was optimised. The morphology of microcapsules was characterised and evaluated by in vitro and in vivo tests to study the swelling characteristics, mucoadhesion and drug release characteristics, followed by MTT assay on human HT-29 colon cancer cell lines. The size of prepared microcapsules was within the range of 361 ± 4.50 to 931 ± 22.41; encapsulation efficiency (%) was within the range of 42.72 ± 0.43 to 98.12 ± 0.43 %. The in vitro paclitaxel released over 24 hours were in a range of 82.15 ± 3.43 % to 96.75 ± 2.41 %. The controlled release pattern of paclitaxel was observed from the in vitro drug release study of microcapsules. The prepared microcapsules that showed better mucoadhesion were in the range of 73.66 ± 1.42 to 97.85 ± 1.08 % for a period of 6 h. The in vivo pharmacokinetic study conducted in rats resulted in high Tmax, the area under the curve and mean residence time for microcapsules as compared to that of the marketed formulation. It could be concluded that the microcapsules containing povidone polymer showed superior results.

Development, Optimization, Characterization and Impact of In vitro Lipolysis on Drug Release of Telmisartan Loaded SMEDDS

2019 ◽  
Vol 9 (4) ◽  
pp. 330-340 ◽  
Author(s):  
Ravinder Verma ◽  
Deepak Kaushik
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Oral Bioavailability ◽  
Research Work ◽  
Mixture Design ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
In Vitro Lipolysis ◽  
Globule Size

Objective: The objective of the current research is systematic optimization and development of microemulsion preconcentrates to get better solubility that results in improvement of oral bioavailability profile of Telmisartan utilizing D-optimal mixture design. Methods: Solubility studies in a variety of lipidic ingredients and optimization of formulations were carried out for the development of liquid SMEDDS. D-optimal mixture design was utilized for assessing the interaction performance of desired responses (such as % cumulative drug release and globule size) and optimized using desirability approach. The optimized batch was evaluated for its % cumulative drug release and globule size performance for determining the dissolution rate and oral bioavailability of drug. Results: The optimized batch (F-8), which contained 10% oil (Capmul MCM EP), 45% surfactant (Labrasol) and 45% co-surfactant (Transcutol HP) resulted in desired qualities of measured responses with 84.6nm globule size and 98.5% drug release within 15 minutes. Optimized SMEDDS showed brilliant goodness of fit between drug release. Stability studies indicated stability of the optimized SMEDDS batch over 3-month storage at 40°C/75% RH and improved dissolution rate in contrast to pure API. The optimized SMEDDS showed no impact of in vitro lipolysis on drug release. Conclusion: Developed and optimized SMEDDS showed improved in vitro dissolution rate and dissolution profile in contrast to pure drug. These investigations further confirm dose reduction in SMEDDS by gaining an equivalent therapeutic profile with non-SMEDDS formulation. This research work successfully shows the potential usage of SMEDDS for delivery of BCS-II class drugs.

Efficient Delivery of Dexibuprofen Using Nanocrystals

2013 ◽  
Vol 678 ◽  
pp. 281-285
Author(s):  
Natesan Subramanian ◽  
Sugumanran Abimanyu ◽  
P. Chandra Sekar ◽  
Murugan Sivakumar ◽  
Yachamaneni Varun ◽  
...  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Spherical Shape ◽  
Homogenization Method ◽  
Efficient Delivery ◽  
Particle Size And Morphology ◽  
Pure Drug ◽  
Size And Morphology ◽  
Dialysis Bag

The main aim of present study is to develop the nanocrystals as a viable drug delivery strategy for the improvement of dissolution rate and bioavailability of dexibuprofen. Dexibuprofen nanocrystals were prepared by the combination of precipitation and high shear homogenization method. Particle size and morphology of produced nanocrystals were compared with that of the pure drug. Particle size of nanocrystals is in the range of 95 to 117 nm were as 2.43µm for pure drug. Photomicrographs of phase contrast microscopy and the TEM showed the spherical shape of the nanocrystals. In-vitro drug release of dexibuprofen nanocrystals formulations was studied by dialysis bag method and observed the drug release of 92 to 100% within 6 hrs. Hence we conclude that the formulated nanocrystals may offer exciting opportunities for oral and other formulations.

scholarly journals PARENT CHILD RELATIONSHIP OF SECONDARY SCHOOL GIRL CHILDREN IN THE CONTEXT OF LOCALITY AND DIFFERENT SCHOOL BACKGROUND

2017 ◽  
Vol 4 (37) ◽  
Author(s):  
J. Shakila
Keyword(s):  
Rheumatoid Arthritis ◽  
Drug Release ◽  
Research Work ◽  
Lag Time ◽  
Oral Dosage ◽  
Blood Levels ◽  
Lag Phase ◽  
Parent Child Relationship

Objective: The objective of this research work was to develop and evaluate the floating– pulsatile drug delivery system (FPDDS) of meloxicam intended for Chrono pharmacotherapy of rheumatoid arthritis. Methods: The system consisting of drug containing core, coated with hydrophilic erodible polymer, which is responsible for a lag phase for pulsatile release, top cover buoyant layer was prepared with HPMC K4M and sodium bicarbonate, provides buoyancy to increase retention of the oral dosage form in the stomach. Meloxicam is a COX-2 inhibitor used to treat joint diseases such as osteoarthritis and rheumatoid arthritis. For rheumatoid arthritis Chrono pharmacotherapy has been recommended to ensure that the highest blood levels of the drug coincide with peak pain and stiffness. Result and discussion: The prepared tablets were characterized and found to exhibit satisfactory physico-chemical characteristics. Hence, the main objective of present work is to formulate FPDDS of meloxicam in order to achieve drug release after pre-determined lag phase. Developed formulations were evaluated for in vitro drug release studies, water uptake and erosion studies, floating behaviour and in vivo radiology studies. Results showed that a certain lag time before drug release which was due to the erosion of the hydrophilic erodible polymer. The lag time clearly depends on the type and amount of hydrophilic polymer which was applied on the inner cores. Floating time and floating lag time was controlled by quantity and composition of buoyant layer. In vivo radiology studies point out the capability of the system of longer residence time of the tablets in the gastric region and releasing the drug after a programmed lag time. Conclusion: The optimized formulation of the developed system provided a lag phase while showing the gastroretension followed by pulsatile drug release that would be beneficial for chronotherapy of rheumatoid arthritis and osteoarthritis.

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