scholarly journals Itraconazole Niosomes Drug Delivery System and Its Antimycotic Activity against Candida albicans

2012 ◽  
Vol 2012 ◽  
pp. 1-7 ◽  
Author(s):  
Vijay D. Wagh ◽  
Onkar J. Deshmukh

Niosomes have potential applications in topical drug delivery system. The objective of the study was to formulate and evaluate the niosome of Itraconazole. Surfactant : cholesterol ratio and quantity of ethanol used were studied by applying factorial design. Formulated niosomes were evaluated for vesicle size, entrapment efficiency, drug release, skin permeation, and antimycotic activity. Vesicle size, entrapment efficiency, and drug release were markedly dependent on surfactant : cholesterol ratio and quantity of ethanol used. Permeation of the drug through the skin was affected by cholesterol content in formulation. Itraconazole niosome were having larger zone of inhibition than marketed formulation when activity was checked against C. albicans. Niosomes may be a promising carrier for topical delivery of Itraconazole especially due to their simple production.

Author(s):  
Anupam K Sachan ◽  
Saurabh Singh ◽  
Kiran Kumari ◽  
Pratibha Devi

Microspheres carrier system made from natural or synthetic polymers used in sustained release drug delivery system. The present study involves formulation and evaluation of floating microspheres of Curcumin for improving the drug bioavailability by prolongation gastric residence time. Curcumin, natural hypoglycemic agent is a lipophilic drug, absorbed poorly from the stomach, quickly eliminated and having short half-life so suitable to formulate floating drug delivery system for sustained release. Floating microspheres of curcumin were formulated by solvent evaporation technique using ethanol and dichloromethane (1:1) as organic solvent and incorporating various synthetic polymers as coating polymer, sustain release polymers and floating agent. The final formulation were evaluated various parameters such as compatibility studies, micrometric properties, In-vitro drug release and % buoyancy. FTIR studies showed that there were no interaction between drug and excipients. The surface morphology studies by SEM confirmed their spherical and smooth surface. The mean particles size were found to be 416-618µm, practical yield of microspheres was in the range of 60.21±0.052% - 80.87±0.043%, drug entrapment efficiency 47.4±0.065% - 77.9±0.036% and % buoyancy 62,24±0.161% - 88.63±0.413%. Result show that entraptmency increased as polymer (Eudragit RS100) conc. Increased. The drug release after 12 hrs. was 72.13% - 87.13% and it decrease as a polymer (HPMC, EC) concentration was decrease.


2021 ◽  
Author(s):  
Cheran K ◽  
Udaykumar B Bolmal ◽  
Archana S Patil ◽  
Umashri A Kokatanur ◽  
Rajashree S Masareddy

Abstract Background: The goal of this study was to develop a gastro retentive floating drug delivery system that would improve site specific activity, patient compliance and therapeutic efficacy.Methodology: Floating microspheres of Miglitol were formulated by double emulsion method using ethyl cellulose and eudragit E100 different weight ratio and PVA as an emulsifier. It has been prepared with respect quantity of polymer concentration and stirring speed to evaluate for % buoyancy, drug entrapment efficiency, particle size drug release rate. Result: The percent of buoyancy, drug entrapment efficiency, particle size, and percentage yield were increased with increase the polymer mixture concentration. Among all formulation batches, F6 showed acceptable results drug entrapment efficiency (86.57%) and buoyancy (94.25%). F10 formulation was prepared to check the predicted and actual factors and compared with optimized formulation F6. The drug release was increased as the polymer concentration was decrease. The kinetic model zero order had the highest regression coefficient value, it was described as a sustained release dosage form. According to ICH guideline accelerated stability studies of F6 and F10 formulations were conducted for 90 days. After 90 days buoyancy and in vitro drug release was performed and the results were F6 and F10 buoyancy was found to be 88.21%, 87.22% and in vitro drug release was found to be 62.87%, 63.51%. Conclusion: The present study, showed compatibility of drug with polymers by FTIR in formulation. Floating microsphere of Miglitol was prepared by double emulsion technique. The F6 Miglitol floating microsphere was optimized formulation demonstrated with excellent drug entrapment performance (86.57%), good floating behaviour (94.25%), and the largest particle size (670µm). The present study concludes that floating based gastro retentive delivery system of Miglitol microspheres has a safe and effective drug delivery system with increased therapeutic efficacy and a longer duration of action.


Author(s):  
Samreen ◽  
M. Aruna ◽  
Shaik Harun Rasheed

In the past few decades, considerable attention has been focused on the development of new drug delivery system (NDDS). The NDDS should ideally fulfill two prerequisites. Firstly, it should deliver the drug at a rate directed by the needs of the body, over the period of treatment. Secondly, it should channel the active entity to the site of action. Conventional dosage forms including prolonged release dosage forms are unable to meet none of these. At present, no available drug delivery system behaves ideally, but sincere attempts have been made to achieve them through various novel approaches in drug delivery. The aim of present work is to develop a niosomal drug delivery system of aceclofenac. To perform drug-polymer compatibility FT-IR studies were carried out and observed that there was no interaction between the APl and excipients. 8 niosomal formulations are prepared by the thin film hydration method using the cholesterol as the phospholipid. Prepared niosomal formulations were characterized by vesicle size, shape, surface charge, entrapment efficiency, drug content and invitro drug release studies. The vesicle size, size distribution and zeta potential of the optimized formulation (F5) was found to be 65.6 nm and zeta potential was found to be -1.5mV. Size distribution curve confirms the normal size distribution of the vesicles. The % entrapment efficiency of niosomal vesicles formulations were found to be in the range of 54.18±0.59 to 92.71±0.56 and optimized formulation was found to be 92.71±0.56 and drug content of niosomes formulations (F1to F8) were determined to be in the range of 94.6 -97.8%. The pH of all topical niosomal gels were found to be in the range of 7.4±0.02 to 7.4±0.08.The best fit with higher correlation (r2> 0.99) was found with the Zero Order Release and follows Korsemeyer peppas equation for all the formulations, which means that release of Aceclofenac from the lipid bilayer vesicles were due to diffusion. The stability studies were carried out and there was no significant change found in the formulations.


Author(s):  
ShirishaG. Suddala ◽  
S. K. Sahoo ◽  
M. R. Yamsani

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.


2007 ◽  
Vol 25 (6) ◽  
pp. 1347-1354 ◽  
Author(s):  
Heiko Kranz ◽  
Erol Yilmaz ◽  
Gayle A. Brazeau ◽  
Roland Bodmeier

2018 ◽  
Vol 115 (3) ◽  
pp. 501-506 ◽  
Author(s):  
Meng Qiu ◽  
Dou Wang ◽  
Weiyuan Liang ◽  
Liping Liu ◽  
Yin Zhang ◽  
...  

A biodegradable drug delivery system (DDS) is one the most promising therapeutic strategies for cancer therapy. Here, we propose a unique concept of light activation of black phosphorus (BP) at hydrogel nanostructures for cancer therapy. A photosensitizer converts light into heat that softens and melts drug-loaded hydrogel-based nanostructures. Drug release rates can be accurately controlled by light intensity, exposure duration, BP concentration, and hydrogel composition. Owing to sufficiently deep penetration of near-infrared (NIR) light through tissues, our BP-based system shows high therapeutic efficacy for treatment of s.c. cancers. Importantly, our drug delivery system is completely harmless and degradable in vivo. Together, our work proposes a unique concept for precision cancer therapy by external light excitation to release cancer drugs. If these findings are successfully translated into the clinic, millions of patients with cancer will benefit from our work.


Author(s):  
Harini Amballa ◽  
Navaneetha Kaluva ◽  
Sree Giri Prasad Beri ◽  
Krishna Mohan Chinnala ◽  
Mayuri Konda

Mucoadhesive drug release system is a preferably unidirectional release system where mucosal epithelial exterior is enclosed by the mucus deposit that interacts with the bio-adhesive drug delivery system and swelling time of the buccal dosage form which is amplified by mucin molecules at the location of administration. Eplerenone is an Anti-hypertensive drug that undergoes hepatic first pass metabolism and shows 69% of bioavailability. In order to bypass the hepatic first pass metabolism the drug is designed to be delivered through buccal cavity to avoid the first pass metabolism. Eplerenone buccal tablets were formulated by using direct compression method with different polymers like HPMC K 100M, Carbopol 934P, Carbopol 974P, Xantham Gum, Eudragit L100 and NaCMC in various concentrations and compositions. Incompatibility complications were not observed from the FTIR spectrums. The formulated and prepared buccal solid dosage forms were evaluated for pre-compressions and post- compression parameters such as hardness, weight variation, thickness, friability, surface pH, swelling index, in-vitro dissolution studies, drug content uniformity, mucoadhesion strength and mucoadhesion time. Evaluation results of formulation F12 are proven to be the optimal formulation showing highest mucoadhesion time, mucoadhesion strength and in-vitro drug release for prolonged period of time about 8 hours. Eplerenone is best delivered through buccal drug delivery system to enhance its oral bioavailability and bypass the hepatic first pass metabolism.


Author(s):  
Kanuri Lakshmi Prasad ◽  
Kuralla Hari

Objective: To enhance solubility and dissolution rate of budesonide through development of solid self-nanoemulsifying drug delivery system (S-SNEDDS). Methods: Liquid self-nanoemulsifying drug delivery systems (L-SNEDDS) were prepared and ternary phase diagram was constructed using Origin pro 8. Liquid self-nanoemulsifying formulation LF2 having 20% oil and 80% of surfactant/co-surfactant was optimized from the three formulations (LF1-LF3) to convert in to solid, through various characterization techniques like self-emulsification, in vitro drug release profile and drug content estimation. The prepared L-SNEDDS converted into S-SNEDDS, SF1-SF6 by adsorption technique using Aerosil 200, Neusilin US2, and Neusilin UFL2 to improve flowability, compressibility and stability. Results: Formulation LF2 exhibited globule size of 82.4 nm, PDI 0.349 and Zeta potential -28.6 mV with drug indicating the stability and homogeneity of particles. The optimized formulation SF4 containing Neusilin UFL2 was characterized by DSC, FTIR, X-Ray diffraction studies and found no incompatibility and no major shifts were noticed. Formulation SF4 released 100 % drug in 20 min against pure drug release of 47 % in 60 min. Regardless of the form (i.e. liquid or solid) similar performance of emulsification efficiency is observed. Conclusion: The results demonstrated that the technique of novel solid self-nanoemulsifying drug delivery system can be employed to enhance the solubility and dissolution rate of poorly water-soluble drug budesonide.


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