scholarly journals Development and Evaluation of Nanoemulsifying Preconcentrate of Curcumin for Colon Delivery

2015 ◽  
Vol 2015 ◽  
pp. 1-13 ◽  
Author(s):  
Jyoti Wadhwa ◽  
Abhay Asthana ◽  
Gyati Shilakari ◽  
Arun Kumar Chopra ◽  
Ranjit Singh
Keyword(s):  
Drug Release ◽  
Phosphate Buffer ◽  
Stability Study ◽  
Alkaline Media ◽  
Systemic Absorption ◽  
Size Analysis ◽  
Globule Size ◽  
Time Required

The present study aimed to develop and optimize a nanoemulsifying preconcentrate formulation of curcumin with good emulsification ability and optimal globule size, for controlled targeting in colon. Content of formulation variables, namely,X1(Peceol),X2(Cremophor-EL), andX3(Transcutol HP), were optimized by Box-Behnken design of experiments for its impact on mean globule size (Y1), emulsification time (Y2), and time required for drug release (85%) in phosphate buffer (pH 7.2),t85%(Y3). Transmission electron micrographs confirmed that there is no coalescence among globules, with size range concordant with the globule size analysis by dynamic light scattering technique (100 nm). 3D plots indicated that concentration of formulation ingredients significantly influences the formulation properties (globule size, emulsification time, and drug release).In vitrorelease profile (in phosphate buffer; pH 7.2) represents the fact that more than 50% of the drug was released within initial 15 min whereasin vivorelease showed limited systemic absorption (Cmax200 ng/mL) of curcumin. Stability study ensures the protection of drug in alkaline media which may further confirm the localised delivery of drug to colonic region. Study demonstrated that the nanoemulsifying preconcentrate can be a promising system for the colon specific delivery of curcumin to treat local pathologies.

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).

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 FORMULATION AND EVALUATION OF SELF-EMULSIFYING DRUG DELIVERY SYSTEM OF ETORICOXIB

2017 ◽  
Vol 10 (7) ◽  
pp. 367 ◽  
Author(s):  
Surendra Singh Saurabh ◽  
Roshan Issarani ◽  
Nagori Bp
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
In Vitro Release ◽  
Stability Study ◽  
In Vitro Drug Release ◽  
In Vitro Permeation ◽  
Globule Size ◽  
Vitro Release ◽  
As Solubility

Objective: In the present dissertation work, the aim was to prepare self-emulsifying drug delivery systems (SEDDS) of etoricoxib to improve its solubility with a view to enhance its oral bioavailability.Methods: The prepared SEDDS was the concentrate of drug, oil, surfactants, and cosurfactant. The formulation was evaluated for various tests such as solubility, globule size, thermodynamic stability study, pH determination, ease of dispersibility, uniformity index, drug content, in-vitro release study, and in-vitro permeation study.Results: The optimized formulation F6 showed drug release (79.21±2.73%), droplet size (0.546 μm). In vitro drug release of the F6 was highly significant (p<0.05) as compared to the plain drug.Conclusion: All formulations of etoricoxib SEDDS were showed faster dissolution than plain drug (p<0.05), mean bioavailability of etoricoxib increase in respect to the plain drug. The F6 can be further used for the preparation of various solid SEDDS formulations.

scholarly journals Mouth Dissolving Film of Domperidone: An approach towards Formulation and its Evaluation

2021 ◽  
pp. 140-150
Author(s):  
Khanderao Jadhav ◽  
Shivraj Jadhav ◽  
Deepak Sonawane ◽  
Deepak Somvanshi ◽  
Hina Shah ◽  
...  
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Stability Study ◽  
Preparation Technique ◽  
In Vivo Evaluation ◽  
Casting Technique ◽  
Dsc Studies ◽  
Oral Films

The objective of the current work is to formulate and evaluate the mouth dissolving film of domperidone. It is ideally suitable for the treatment of emesis. The mouth dissolving film of domperidone is useful in the vomiting through the journey. Mouth dissolving films were formulated by the solvent casting technique and its in-vitro as well as the in-vivo evaluation was done by the usual pharmacopoeial and unofficial tests and by using human volunteers. The main benefit of the preparation technique includes fewer operation units, better content consistency. The mouth dissolving film formed was found to be disintegrated in 1 minute. The ratio of components in the aqueous phase affected the thickness, drug content, tensile strength, percentage elongation, folding endurance, and release profile of mouth dissolving film and the best results were obtained for the HPMC E15 and polyethyleneglycol. The compatibility between domperidone and excipients was confirmed by FTIR and DSC studies. The developed mouth dissolving film of domperidone demonstrated usefulness for fast release of drug in mouth, for better drug utilization, and improved patient compliance. The optimized formulation, due to low HPMC E15 content, has optimum tensile strength and thickness. Formulation F8 containing HPMC E15 and PG showed a cumulative % drug release of 95.10 at the end of 12 minutes. HPMC E15 films showed higher cumulative % drug release than films of other HPMC E grades at different concentrations. It was found to be stable during the accelerated stability study. The effect of different concentrations of polymers and plasticizers on in-vitro evaluation parameters was evaluated. Hence, data showed that formulation F8 was the most suitable for the development of fast dissolving oral films of domperidone.

Nano-Liposomal Dry Powder Inhaler of Amiloride Hydrochloride

2006 ◽  
Vol 6 (9) ◽  
pp. 3001-3009 ◽  
Author(s):  
Mahavir Bhupal Chougule ◽  
Bijay Kumar Padhi ◽  
Ambikanandan Misra
Keyword(s):  
Cystic Fibrosis ◽  
Drug Release ◽  
Phosphate Buffer ◽  
Dry Powder Inhaler ◽  
Dry Powder ◽  
Phosphate Buffer Saline ◽  
Amiloride Hydrochloride ◽  
Spray Dried

The purpose of this study was to encapsulate Amiloride Hydrochloride into nano-liposomes, incorporate it into dry powder inhaler, and to provide prolonged effective concentration in airways to enhance mucociliary clearance and prevent secondary infection in cystic fibrosis. Liposomes were prepared by thin film hydration technique and then dispersion was passed through high pressure homogenizer to achieve size of nanometer range. Nano-liposomes were separated by centrifugation and were characterized. They were dispersed in phosphate buffer saline pH 7.4 containing carriers (lactose/sucrose/mannitol), and glycine as anti-adherent. The resultant dispersion was spray dried. The spray dried powders were characterized and in vitro drug release studies were performed using phosphate buffer saline pH 7.4. in vitro and in vivo drug pulmonary deposition was carried out using Andersen Cascade Impactor and by estimating drug in bronchial alveolar lavage and lung homogenate after intratracheal instillation in rats respectively. Nano-liposomes were found to have mean volume diameter of 198 ± 15 nm, and 57% ± 1.9% of drug entrapment. Mannitol based formulation was found to have low density, good flowability, particle size of 6.7 ± 0.6 μm determined by Malvern MasterSizer, maximum fine particle fraction of 67.6 ± 0.6%, mean mass aerodynamic diameter 2.3 ± 0.1 μm, and geometric standard deviation 2.4 ± 0.1. Developed formulations were found to have prolonged drug release following Higuchi's Controlled Release model and in vivo studies showed maximal retention time of drug of 12 hrs within the lungs and slow clearance from the lungs. This study provides a practical approach for direct lung delivery of Amiloride Hydrochloride encapsulated in liposomes for controlled and prolonged retention at the site of action from dry powder inhaler. It can provide a promising alternative to the presently available nebulizers in terms of prolonged pharmacological effect, reducing systemic side effects such as potassium retention due to rapid clearance of the drug from lungs in patients suffering from cystic fibrosis.

scholarly journals Bioadhesive vaginal tablets containing spray dried microspheres loaded with clotrimazole for treatment of vaginal Candidiasis

2013 ◽  
Vol 63 (3) ◽  
pp. 359-372 ◽  
Author(s):  
Naresh Vishal Gupta ◽  
Shirodker Natasha ◽  
Anil Getyala ◽  
Ramnath Sudeendra Bhat
Keyword(s):  
Drug Release ◽  
Chemical Interaction ◽  
Drug Loading ◽  
Particle Size Analysis ◽  
Vaginal Candidiasis ◽  
Size Analysis ◽  
In Vitro Drug Release ◽  
Dsc Studies

Abstract The aim of the present investigation was to prepare and evaluate novel bioadhesive vaginal tablets containing clotrimazole loaded microspheres in order to provide long-term therapeutic activity at the site of infection. Tablets were prepared by incorporating drug loaded microspheres and using bioadhesive polymers hydroxypropylmethylcellulose, sodium carboxymethylcellulose and Carbopol. Microspheres were prepared by the spray drying technique using Eudragit RS-100 and Eudragit RL-100. Microspheres were characterized by SEM, DSC, FTIR, particle size analysis and evaluated for percentage yield, drug loading, encapsulation efficiency and in vitro drug release. To achieve bioadhesion to the mucosal tissue, optimized microspheres were incorporated into bioadhesive tablets and were evaluated for in vitro drug release, in vitro and in vivo mucoadhesion. FTIR and DSC studies showed that no chemical interaction occurred between the drug and polymers. The sphericity factor indicated that the prepared microspheres were spherical. Formulation Mt6 indicated a controlled in vitro drug release and good bioadhesive strength. The in vivo images confirmed the bioadhesion and retention property of tablets up to 24 h. The results indicated that this drug delivery system can be explored for controlled intravaginal drug release.

scholarly journals Development and evaluation of floating tablet of metoprolol succinate for increased bioavailability

2018 ◽  
Vol 9 (4) ◽  
Author(s):  
Kauser Fatema ◽  
SR Shahi ◽  
Shaikh Tauqeer
Keyword(s):  
Drug Release ◽  
Oral Bioavailability ◽  
Stability Study ◽  
Hydrophilic Polymers ◽  
Physical Parameters ◽  
Sustained Drug Release ◽  
Metoprolol Succinate ◽  
Floating Tablet

<p>The present study is based on development and evaluation of gastroretentive floating tablets of metoprolol succinate by direct compression method, to increase the oral bioavailability of MS. For this, we used a combination of two different hydrophilic polymers that is polyethylene oxide PEO N-80 (X1) and hydroxy ethylcellulose HEC (X2) as independent variables and studied its effect on drug release (as dependent variable) at 20h for MS. A 3<sup>2</sup> factorial design was used for optimization purpose.</p><p>The DSC result shows no interaction between two polymers and the drug (MS). Further, in vitro drug release studies have shown a sustained drug release for more than 20h in upper gastrointestinal region (stomach). In vivo study using rabbits have shown increased AUC<sub>0-24 </sub>(bioavailability) of prepared optimized F6 formulation as compared to the marketed sustain release tablet of MS. Stability study shows no comparable differences on physical parameters and the drug release after 3 months of accelerated stability testing.  Hence, we can conclude that a floating tablet containing combination of hydrophilic polymers can be used for gastric retention for more than 20hr which will increase the oral bioavailability of MS.</p>

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 FORMULATION AND IN VIVO EVALUATION OF SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEM OF RAMIPRIL IN WISTAR RATS

2021 ◽  
pp. 126-136
Author(s):  
NALLAPU JAYAPAL ◽  
YAMSANI VAMSHI VISHNU
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Systemic Absorption ◽  
Content Uniformity ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
Pure Drug

Objective: The aim was to formulate and evaluate self-nanoemulsifying drug delivery systems (SNEDDS) of ramipril, an antihypertensive drug to improve the solubility and bioavailability. Methods: Based on solubility studies oil phase (Sefsol 218), surfactant (Acrysol EL135), and cosurfactant (Transcutol P), respectively, were selected to prepare SNEDDS. Ramipril SNEDDS optimized employing box-Behnken design through the study of factors. All formulations were evaluated for particle size, zeta potential (ZP), polydispersity index (PDI), entrapment efficiency (EE), drug content, and in vitro drug release. The optimized formulation was characterized for Fourier transform infrared (FTIR), scanning electron microscopy (SEM), stability studies, and pharmacokinetic study. Results: The mean particle size, PDI, ZP, EE, content uniformity, and in vitro drug release profile of optimized ramipril-loaded SNEDDS (RF14) were found to be 75.3±2.21nm, 0.126±0.05, −24.4±5.78mV, 98.74±1.97%, 99.52±1.67%, and 98.65±1.73%, respectively. FTIR studies revealed that there is no incompatibility between drug and excipients, SEM images exhibited nanoparticles to be more porous and in spherical shape. Stability studies indicated formulation was stable for 6 months. In vivo studies were conducted for optimized formulation RF14, the Tmax was found to be 0.5±0.62 and 0.5±0.95 h for the optimized and commercial formulations respectively, while Cmax was 25.16±1.73 ng/mL was significant (p<0.05) as compared to the ramipril pure drug 8.02±0.086 ng/mL. AUC0-t of the SNEDDS formulation was higher 355.49±1.76ng h/ml compared to pure drug 116.57±1.64 ng h/ml indicated higher amount of drug concentration in blood proving better systemic absorption of ramipril from SNEDDS formulation as compared to the pure drug. Conclusion: It is concluded from the results that ramipril was successfully formulated into SNEDDS with higher concentration with fast action.

Nanofibrous Polydioxanone Depots for Prolonged Intraperitoneal Paclitaxel Delivery

2019 ◽  
Vol 16 (7) ◽  
pp. 654-662 ◽  
Author(s):  
Smrithi Padmakumar ◽  
Deepthy Menon
Keyword(s):  
Drug Release ◽  
Phosphate Buffer ◽  
Entrapment Efficiency ◽  
In Vivo Studies ◽  
Drug Release Profile ◽  
Sustained Drug Delivery ◽  
Drug Concentrations ◽  
Peritoneal Wall

Background: Prolonged chemodrug delivery to the tumor site is a prerequisite to maintaining its localised therapeutic concentrations for effective treatment of malignant solid tumors. Objective: The current study aims to develop implantable polymeric depots through conventional electrospinning for sustained drug delivery, specifically to the peritoneum. Methods: Non-woven electrospun mats were fabricated by simple electrospinning of Polydioxanone solution loaded with the chemodrug, Paclitaxel. The implants were subjected to the analysis of morphology, mechanical properties, degradation and drug release in phosphate buffer and patient-derived peritoneal drain fluid samples. In vivo studies were conducted by surgical knotting of these implants to the peritoneal wall of healthy mice. Results: Non-woven electrospun mats with a thickness of 0.65±0.07 mm, weighing ~ 20 mg were fabricated by electrospinning 15 w/v% polymer loaded with 10 w/w% drug. These implants possessing good mechanical integrity showed a drug entrapment efficiency of 87.82±2.54 %. In vitro drug release studies in phosphate buffer showed a sustained profile for ~4 weeks with a burst of 10 % of total drug content, whereas this amounted to >60% in patient samples. Mice implanted with these depots remained healthy during the study period. The biphasic drug release profile obtained in vivo showed a slow trend, with peritoneal lavage and tissues retaining good drug concentrations for a sustained period. Conclusion: The results indicate that non-woven electrospun mats developed from biodegradable Polydioxanone polymer can serve as ideal candidates for easily implantable drug depots to address the challenges of peritoneal metastasis in ovarian cancer.

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