scholarly journals DIACEREIN-LOADED NIOSOMES (DC-NS): A NEW TECHNIQUE TO SUSTAIN THE RELEASE OF DRUG ACTION

2022 ◽  
pp. 156-163
Author(s):  
RASHAD M. KAOUD ◽  
EMAN J. HEIKAL ◽  
TAHA M. HAMMADY
Keyword(s):  
Physical Stability ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Molar Ratios ◽  
Tween 40 ◽  
A New Technique ◽  
The Stability ◽  
Tween 60

Objective: The study's main goal is to develop a suitable niosomes (NS) encapsulated drug for anti-inflammatory effects such as diacerein (DC) and to evaluate the system's vesicle size (VS), entrapment efficiency (EE %), physical stability and in vitro release. Methods: Tween (40 and 60), cholesterol, and stearylamine were used in a 1:1:0.1 molar ratios as non-ionic surfactants. Thin film hydration was used to create the NS. Results: The higher EE% was observed with NS (F11) prepared from tween 60, cholesterol and 2.5 min sonication. These formulations' release patterns were Higuchi diffusion and first order. For the stability study, NS formulations were stored at temperature between 2-8 °C for 60 d retains the most drugs when compared to room and high temperature conditions. Conclusion: The findings of this study have conclusively shown that after NS encapsulation of DC, drug release is prolonged at a constant and controlled rate.

Ultra-deformable Liposomes as Flexible Nanovesicular Carrier to Penetrate Versatile Drugs Transdermally

2020 ◽  
Vol 10 (1) ◽  
pp. 12-20
Author(s):  
Gaurav Tiwari ◽  
Ruchi Tiwari ◽  
Rachna Singh ◽  
Awani K. Rai
Keyword(s):  
Skin Permeation ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Human Organ ◽  
Ethanol Injection ◽  
Release Studies ◽  
Junction Protein ◽  
Penetration Ability

Introduction: Transferosomes also known as ultra-deformable liposomes were introduced by Gregor Cevc in 1990. These are deformable vesicles that transport drug across the skin, which is the best route of drug delivery because skin is the largest human organ with 3 kg total weight and a surface area of 1.5-2.0 m2. Methods: Transferosomes are able to efficiently deliver low as well as high molecular weight drug across the skin in terms of quantity and depth. Various methods used for the preparation of transferosomes such as thin film hydration method, reverse phase evaporation method, vortex/sonication method, ethanol injection method and freeze thaw method. Results: The prepared transferosomal preparation will be evaluated for particle shape and size, entrapment efficiency, stability study, penetration ability and skin permeation study. In vitro release studies are to be performed using a specific dissolution medium. Conclusion: Ultra deformable liposomes can be used for delivery of different drugs e.g. analgesic, anesthetic, corticosteroids, anticancer, sex hormone, insulin, gap junction protein, and albumin.

scholarly journals DESIGN, FORMULATION AND EVALUATION OF LIPOSOME CONTAINING ISONIAZID

2018 ◽  
Vol 10 (2) ◽  
pp. 52 ◽  
Author(s):  
Akshay Singha Roy ◽  
Sudipta Das ◽  
Arnab Samanta
Keyword(s):  
In Vitro Release ◽  
Particle Diameter ◽  
Weight Ratio ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Release Profile ◽  
Skewed Distribution ◽  
Size Analysis ◽  
Scanning Calorimetry

Objective: The objective of the present study was to formulate and evaluate liposomes loaded with isoniazid.Methods: Liposome of isoniazid was made by thin layer film hydration method. L-α-phosphatidylcholine and cholesterol were used to make multiamellar vesicles. Six batches of liposomes were prepared based on the different weight ratio of L-α-phosphatidylcholine and cholesterol. Differential scanning calorimetry (DSC) study conducted to study in any incompatibility.Results: The prepared liposomes were evaluated by particle size analysis, entrapment efficiency, release study and stability study. Particle sizes were determined from the scanning electron microscopy (SEM) photographs. When particle frequencies were plotted against particle diameter in the histogram, it showed that F1 batch had a skewed distribution towards smaller liposomes while F6 shows a proper bell-shaped curve with a mean at 225 mm. The percentage entrapment efficiency was found to be 8.99 ± 0.15 to 4.19 ± 0.12 % respectively. From the release profile, it was seen that F1 batch was fastest and F6 was slowest to release the drug. The satisfactory batch F1 was packed in Eppendorf tube and stored at 4 °C temperature for one month. At the end of one month, the samples were analyzed for their physical properties, drug entrapment and in vitro release profile. The percentage release was found to be 96.5 ± 3.2 after 4 h.Conclusion: The F1 batch showed most promising results compared to other. No significant change was found during one month’s stability study of final batch (F1).

Ibuprofen loaded nano-ethanolic liposomes carbopol gel system: in vitro characterization and anti-inflammatory efficacy assessment in Wistar rats

2018 ◽  
Vol 38 (3) ◽  
pp. 291-298 ◽  
Author(s):  
Atefeh Afshar Moghaddam ◽  
Abdul Ahad ◽  
Mohd. Aqil ◽  
Farhan J. Ahmad ◽  
Yasmin Sultana ◽  
...  
Keyword(s):  
Transdermal Delivery ◽  
Wistar Rats ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
In Vitro Characterization ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
The Stability

AbstractThe objective of the present study was to develop and characterize nano-ethanolic liposomes (NEL) for transdermal delivery of ibuprofen (IBU). The NEL for transdermal delivery of IBU were prepared by thin film hydration technique and evaluated for vesicle size, shape, entrapment efficiency, transdermal flux, andin vivoanti-inflammatory activity in Wistar rats. The NEL optimized formulation (NEL-Opt) presented vesicle sizes of 32.85±1.98 nm and entrapment efficiency of 86.40±0.55% with improved transdermal flux. The presence of ethanol and flexibility of NEL could be the reasons for better permeation enhancement of IBU via rat’s skin.In vivoanti-inflammatory study of IBU-loaded NEL-Opt gel showed significant reduction (41.18%) of edema in carrageenan-induced rat paw edema as compared to conventional gel of IBU, where reduction of edema was found to be 12.50%. Our results suggest that developed NEL formulations are efficient systems for transdermal IBU delivery against inflammation. The stability study confirmed that the NEL-Opt gel formulation was considerably stable at refrigerator temperature. Our results concluded that NEL are an efficient carrier for transdermal delivery of IBU.

scholarly journals FORMULATION AND OPTIMIZATION OF NIFEDIPINE LOADED NANOCARRIERS

2021 ◽  
pp. 311-317
Author(s):  
ASHWINI JADHAV ◽  
BINOY VARGHESE CHERIYAN
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Physical Stability ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Physicochemical Characteristics ◽  
Good Choice ◽  
The Stability

Objective: The main aim of this study to formulate a nifedipine-loaded nanocarrier for improving solubility and bioavailability. Methods: To improve the solubility of drug, nifedipine-loaded nanocarrier (lipotomes) were prepared by using the film lipid hydration technique. lipotomes were prepared by using tween 80, which is used for increasing solubility and cetyl alcohol for lipophilic environment. Drug excipients interaction determined by FTIR. lipotomes were characterized for particle size, Entrapment efficiency and zeta potential. lipotomes were optimized by using Design-Expert 12 software. Optimized formula further lyophilized by using different cyroproyectant to improve the stability and oral administration of the drug. Results: FTIR shows there was no interaction between formulation ingredients. Mean particle size, entrapment efficiency, zeta potential was determined and found to be 308.1 nm, 96.7%, 20.1mV, respectively. Surface morphology of lipotomes was observed by a scanning electron microscope (SEM). Optimized lipotomes was lyophilized with Mannitol (8% w/v) was the ideal cryoprotectant to retain the physicochemical characteristics of the OLT formulation after lyophilization. Conclusion: Nifedipine loaded nanocarrier was successfully prepared, using film hydration method. Which have good particle size, EE% and zeta potential. After lyophilization no significant changes was observed in particle size with good physical stability, so it could be a good choice for conventional drug delivery system by doing further investigation as in vitro and in vivo study

scholarly journals TRIVALENT ION CROSS-LINKED AND ACETALATED GELLAN GUM MICROSPHERES OF GLIMEPIRIDE

2020 ◽  
pp. 66-68
Author(s):  
SUDIPTA DAS ◽  
RIMI DEY
Keyword(s):  
In Vitro Release ◽  
Microscopic Analysis ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Release Profile ◽  
Gellan Gum ◽  
Long Term Stability ◽  
Vitro Release

Objectives: A novel formulation was developed with glimepiride loaded trivalent ion Al+3 cross-linked and acetalated gellan gum microspheres. Methods: The glimepiride loaded microspheres were formulated using sodium alginate and gellan gum. Cross-linking agents used for the microspheres were aluminum chloride (AlCl3) and glutaraldehyde (GA). The evaluation processes of prepared microspheres were carried out by in-vitro release study, swelling index, microscopic analysis, and entrapment efficiency. Results: All the formulations show good entrapment efficiency and the maximum entrapment 84.6% was governed by the formulation (F3) cross-linked by AlCl3 and GA and their obtained mean particle size were 12.46±3.21 μm. Release profile of the formulations revealed the sustained design of the drug, particularly this formulation (F3), releasing approximately 40% over 4 h. Conclusions: From this experiment, it can be accustomed that F3 possesses higher standard formulation than the rest due to good release profile and entrapment efficiency. Therefore, the long term stability study is required for future development of this formulation.

scholarly journals Preparation and Characterization of Nano Structured Lipid Carriers for Ocular Bacterial Infection

2021 ◽  
pp. 8-23
Author(s):  
Shubhangi Aher ◽  
Ravindra Pal Singh ◽  
Manish Kumar
Keyword(s):  
Ex Vivo ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Tolerance Test ◽  
Stability Study ◽  
Scanning Calorimetry ◽  
Bacterial Conjunctivitis ◽  
Pure Drug

The problem of bacterial conjunctivitis has dramatically increased in recent years due increased pollution and modern lifestyle. The present study was focused to fabricate Sparfloxacin loaded nanostructured lipid carriers (Spar-NLCs) for ophthalmic application to improve ocular penetration of drug and give sustained release of drug to reduce dosing frequency and toxic effect of drug associated with ocular membrane. A regular two-level factorial design was used to optimize the formulation parameters that are significantly affecting the formulation attributes. Spar-NLCs with particle size 171.1 ± 11 nm, zeta potential -49 ± 6.47 mV, entrapment efficiency 89.5 ± 5% and spherical in shape was obtained. Besides this, FTIR spectroscopy, differential scanning calorimetry, and transmission electron microscopy results suggest that the drug is successfully incorporated in NLC and has excellent compatibility with the excipients. In vitro release study follows Korsmeyer peppas model and suggests that 81.35 ± 6.2% release of drug from Spar-NLCs in 12 hours. The result of ex-vivo permeation study demonstrated 349.75 ± 7.3 µg/cm2 of permeation of drug, 44.482 µg cm-2 hr -1 of flux, and 0.1482 cm hr-1 of permeability coefficient which is 1.7 folds higher than pure drug suspension. The antimicrobial activity of Spar-NLCs was better than the pure drug suspension and equivalent to the marketed formulation. Spar-NLC formulation did not showed any ocular damage, swelling, and redness in in -vivo Draize test. The ocular tolerance test (HET-CAM test) also suggests that the Spar-NLC formulation and its excipients were nonirritant to the ocular tissues. The formulation was found to be stable over the three month of stability study. Therefore, this work strongly suggest that Spar-NLCs has higher penetration and extended release of drug which can be effectively used in prevention of bacterial conjunctivitis.

scholarly journals FORMULATION AND OPTIMIZATION BY APPLYING 32 FULL FACTORIAL DESIGN OF MUCOADHESIVE MICROSPHERES OF NIFEDIPINE

2019 ◽  
pp. 321-327
Author(s):  
CHIMAN LAL ◽  
RAJEEV GARG ◽  
GHANSHYAM DAS GUPTA
Keyword(s):  
Research Work ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Microscopy Study ◽  
Electron Microscopy Study ◽  
Stability Study ◽  
Stirring Time ◽  
Drug Entrapment Efficiency ◽  
Full Factorial

Objective: The purpose of this research work is to formulate and optimize mucoadhesive microspheres of nifedipine using Carbopol 934P as mucoadhesive and ethyl cellulose as a carrier polymer for controlling the release of nifedipine. Methods: The emulsion solvent evaporation technique was used for the preparation of microspheres and the 32 full factorial designs were employed for optimization of microspheres. The developed microspheres were characterized for percent yield, entrapment efficiency, particle size, in vitro release study, percent mucoadhesion, surface morphology, and stability study. Results: Evaluating outcomes of preliminary batches indicated that 100 ml volume of processing medium, 5 h stirring time and 2% concentration of emulsifying agent were suitable for spherical, free-flowing microspheres and high percentage drug entrapment efficiency. The optimized batch exhibited 84.35% drug entrapment efficiency, 61.78% mucoadhesion and drug release were also sustained for more than 12 h. Scanning electron microscopy study revealed that produced microspheres were spherical in shape. Conclusion: Experimental responses of the optimized batch have close proximity with the predicted value and stability study of the optimized formulation proved the formulation is stable for a long period of time; hence, it is an excellent alternative over the conventional delivery system.

scholarly journals Formulation Development and Optimization of Sustained Release Microspheres of Acebrophylline

2021 ◽  
pp. 13-28
Author(s):  
Niyati Shah ◽  
Ayesha Sheikh ◽  
Hitesh Jain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Release Kinetic ◽  
Vitro Release ◽  
Polymer Ratio ◽  
Sustained Release Microspheres

Objectives: Aim of present work is to prepare and evaluate Sustained release microspheres of Acebrophylline for treatment of Asthma. Experimental work: In present investigation, attempt was made to prepare sustained release microspheres of Acebrophylline with different polymer ratio using Ionic gelation method. Drug- excipient compatibility studies were performed by FTIR. The best suited Microspheres formulation was found on the basis production yield, entrapment efficiency and in vitro release study. Optimized batch of microspheres (B2) was characterized for FTIR, DSC, and SEM analysis. The drug release data of optimized batch was fitted into different release kinetic models. The optimized batch of microspheres (B2) was subjected for the short term stability study at 40 ± 2°C with RH of 75% for a period of 1 month. Results and discussion: There was no interaction found between drug and excipients. Sodium alginate (2%) concentration, Eudragit RS-100 (1:2) ratio gave highest sustainable property and CaCl2 (2.5%) concentration had a good cross linking property. This observation done on the basis of production yield, entrapment efficiency and In vitro release study. The Microspheres prepared from Ionic gelation method had Drug : Eudragit RS100 (1:2), 2 % Sodium alginate and 2.5 % CaCl2 (B2) give 99.2 % drug release over the periods of 12 hr. The drug release from optimized microspheres formulation (B2) follows first order release kinetic. DSC study showed the melting behavior of drug present into microspheres. SEM studies showed that optimized microspheres were spherical and rough surface.  Stability study proved that optimized formulation (B2) was stable. Conclusion:  Drug: Polymer ratio and Volume of CaCl2 had significant effect on % Entrapment efficiency and Drug release. From the Scanning Electron Microscopy (SEM) study observed that microspheres was spherical and rough surface. Non Fickian diffusion was the mode of drug release from Acebrophylline- loaded microspheres. After stability study no physical changes & almost same drug release was observed in microspheres. Hence, the formulation B2 was stable.

scholarly journals Cubosomes Dispersions as Enhanced Indomethacin Oral Delivery Systems: In vitro and Stability Evaluation

2021 ◽  
pp. 24-35
Author(s):  
Iman M. Alfagih ◽  
Bushra AlQuadeib ◽  
Basmah Aldosari ◽  
Alanood Almurshedi ◽  
Mohamed M. Badran ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Diffusion Mechanism ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Poloxamer 407 ◽  
Fickian Diffusion ◽  
The Stability ◽  
Oral Delivery Systems ◽  
Kinetics Of

Aims: To improve the dissolution of indomethacin through developing liquid indomethacin loaded cubosomes dispersion for oral delivery. Methodology: Glyceryl monooleate based indomethacin loaded cubosomes dispersion were prepared using Taguchi design to study the effect of indomethacin to the disperse phase ratio and poloxamer 407 (PLX%) concentrations on the particle size and entrapment efficiency (%EE). Furthermore, in vitro release in phosphate buffer (pH 6.8), and morphology were investigated. Also, the stability of indomethacin loaded cubosomes dispersions was examined after 6 months storage at 25°C in the dark. Results: The prepared indomethacin cubosomes dispersions were in the nanoscale (184.53±0.7 to 261.33±0.8 nm) with reasonable %EE (49.30±2.6 to 95.55±3.4 %). Moreover, a biphasic release profile was predominant for all formulations, up to 50% of payload released after 2h followed by a second continuous sustained release phase over 24h. The kinetics of indomethacin release was best explained by Higuchi model and the mechanism of drug release from these cubosomes dispersions was by fickian diffusion mechanism. In general, the indomethacin loaded cubosomes dispersions were stable after 6 months storage at 25°C in the dark. Conclusion: Indomethacin loaded cubosomes dispersions proved to be a successful platform to encapsulate and enhance the release of indomethacin with a good stability profile over 6 months.

scholarly journals Synthesis and evaluation of B-cyclodextrin Based Nanosponges of 5- Fluorouracil by Using Ultrasound Assisted Method

2020 ◽  
Vol 29 (2) ◽  
pp. 88-98
Author(s):  
Ihsan K. Jasim ◽  
Shaimaa N. Abd Alhammid ◽  
Alaa A. Abdulrasool
Keyword(s):  
Particle Size ◽  
In Vitro Release ◽  
Particle Morphology ◽  
Entrapment Efficiency ◽  
Molar Ratio ◽  
Phase Solubility ◽  
Molar Ratios ◽  
Phase Solubility Study ◽  
Ultrasound Assisted

  CD-nanosponges were prepared by crosslinking B-CD with diphenylcarbonate (DPC) using ultrasound assisted technique. 5-FU was incorporated with NS by freeze drying, and the phase solubility study, complexation efficiency (CE) entrapment efficiency were performed. Also, the particle morphology was studied using SEM and AFM. The in-vitro release of 5-FU from the prepared nanosponges was carried out in 0.1N HCl. 5-FU nanosponges particle size was in the nano size. The optimum formula showed a particle size of (405.46±30) nm, with a polydispersity index (PDI) (0.328±0.002) and a negative zeta potential (-18.75±1.8). Also the drug entrapment efficiency varied with the CD: DPC molar ratio from 15.6 % to 30%. The SEM and AFM showed crystalline and porous nature of the nanosponges. The in vitro drug release study of the selected formula 5-FUNS2 exhibited the fastest dissolution rate which is 56% in the first hr. Different molar ratios of (cyclodextrin to crosslinker) (CD: DPC) has a proficient effect on complexation efficiency (CE), apparent stability constant (Kst) and entrapment efficiency of 5-FU. 5-FUNS2 with (1:4) molar ratio showed the best result of CE, Kst and entrapment efficiency. 5-FUNS2 gave a higher release rate than the 5-FU-BCD inclusion complex and 5-FU solution. Surface morphology of the prepared nanosponges by SEM, AFM indicate that nanosized and highly porous nanosponges was obtained. The overall results suggest that cyclodextrin nanosponges could be a promising 5-FU delivery system utilizing the suitable formula.

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