scholarly journals SCREENING AND OPTIMIZATION OF VALACYCLOVIR NIOSOMES BY DESIGN OF EXPERIMENTS

2018 ◽  
Vol 10 (1) ◽  
pp. 79 ◽  
Author(s):  
Surya Teja Sp ◽  
Mothilal M. ◽  
Damodharan N ◽  
Jaison D
Keyword(s):  
Drug Release ◽  
Design Of Experiments ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Substantial Effect ◽  
Fickian Diffusion ◽  
Vesicle Size ◽  
Zero Order Kinetics ◽  
Significant Difference ◽  
Span 60

Objective: The objective of the study was to perform a screening, optimization of valacyclovir niosomal formulation to achieve a sustained release of drug using the design of experiments by 32 full factorial design.Methods: Valacyclovir loaded niosomes were prepared using thin film hydration method by varying the ratio of Span 60 and Cholesterol. The prepared niosomes were evaluated for vesicle size, entrapment efficiency, cumulative drug release, fourier transformed infrared spectroscopy (FTIR), zeta potential and surface morphology by field emission scanning electron microscopy (FESEM).Results: The valacyclovir was successfully encapsulated and its entrapment efficiency ranged from 36.70 % to 50.62 %. The average vesicle size of the niosomes was found to be 431 to 623 nm. At 8th hour the drug release varied from 77.50% to 96.31 %. The optimized niosomes were multilamellar with a surface charge potential of about-43.2 mV. The studies revealed that the interaction of cholesterol and surfactant had a substantial effect on vesicle size, entrapment efficiency and drug release from the niosomes. The release kinetics of the optimized niosomes followed zero order kinetics with fickian diffusion controlled mechanism. The stability studies were performed for the optimized formulation and found that the formulation is stable at 4°C ± 2°C.Conclusion: Model equations were developed for the responses. No significant difference was observed between the predicted and observed value, showing that the developed model is reliable.

scholarly journals Development and Characterization of Elastic Liposomes of Metronidazole for the Treatment of Bacterial Infection

2020 ◽  
Vol 10 (6-s) ◽  
pp. 83-88
Author(s):  
Priyam Chaurasiya ◽  
Ritesh Agarwal ◽  
Kavita R. Loksh
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Topical Administration ◽  
Stability Study ◽  
Vesicle Size ◽  
Rotary Evaporation ◽  
Span 60

Objective: The objective of present study is to develop and evaluate the elastic liposomes of metronidazole so as to provide the sustained release and improve its bioavailability. Methods: Elastic liposomes were prepared by rotary evaporation method using Span 80 and Span 60 as a surfactants. The prepared elastic liposomes were evaluated for entrapment efficiency, vesicle size, In vitro drug release. Results: The drug release profiles from different elastic liposomes-in-vehicle formulations were in agreement with the physicochemical properties of the formulations. The formulation prepared showed an average vesicle size 185.4nm. The amount of drug entrapped into the elastic liposomes formulations was determined. The entrapment efficiency was found to be 73.45±0.78 %. A good amount of drug was entrapped in the liposome formulations prepared. Based on different parameters formulations of batch TG2 was found to be the best formulations. Stability study was performed on the selected formulation TG2. When the regression coefficient values of were compared, it was observed that ‘r’ values of first order was maximum i.e. 0.993 hence indicating drug release from formulations was found to follow Korsmeyer Peppas model release kinetics Conclusion: These results indicate that elastic liposome can function as probable drug delivery systems to enhance transdermal permeation of metronidazole for treating the topical infections. Keywords: Metronidazole, Elastic liposomes, Topical administration, Skin infection

FORMULATION AND EVALUATION OF ACECLOFENAC NIOSOMES BY USING MIXTURE OF SURFACTANTS

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (12) ◽  
pp. 21-26
Author(s):  
C.H. Sravanthi ◽  
◽  
S. Punitha
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Therapeutic Index ◽  
Reverse Phase ◽  
Evaporation Method ◽  
Zero Order Kinetics ◽  
Reduced Toxicity ◽  
Span 60

The present study was aimed at the overall improvement in the efficacy, reduced toxicity andenhancement of therapeutic index of aceclofenac. Niosomal delivery system of aceclofenac has beendeveloped by various techniques using mixture of Span 60/40 (surfactant) along with cholesterol in1:1 ratio. The formulations were then characterized with respect to vesicle diameter, drug content,entrapment efficiency, in-vitro drug release and release kinetics. The formulated aceclofenac niosomeswere discrete and round in shape. The lowest entrapment efficiency was found to be 75% (F2) andwas highest in reverse phase evaporation method 95% (F5). Percentage cumulative drug release waswell retarded for up to 24 h in F5 (59%) compared to all other formulations and its release pattern wasanalysed by using various mathematical models and found to follow under zero order kinetics. From thet50% values of F5, it is concluded that the reverse phase evaporation method seems to extend the drugrelease for prolonged period.

Design and Synthesis of a Novel Gabapentin-Phosphotidylcholine Conjugate for Targeting to Phospholipase A2 Enzyme through Nanostructured Lipid Carrier

2020 ◽  
Vol 16 ◽  
Author(s):  
Anjali P.B ◽  
Jawahar N. ◽  
Jubie S. ◽  
Neetu Yadav ◽  
Selvaraj A. ◽  
...  
Keyword(s):  
Drug Release ◽  
Phospholipase A2 ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Structural Analog ◽  
Fickian Diffusion ◽  
Release Kinetic ◽  
Nanostructured Lipid Carrier ◽  
Discovery Studio

Background: : Epilepsy is a genuine neurological turmoil that effects around 50 million individuals around the world. Practically 30% of epileptic patients experience the ill effects of pharmaco-obstruction, which is related with social seclusion, subordinate conduct, low marriage rates, joblessness, mental issues and diminished personal satisfaction. At present accessible antiepileptic drugs have a restricted viability, and their negative properties limit their utilization and cause challenges in patient administration. Gabapentin 1-(aminomethyl)cyclohexane acetic acid, Gbp , (trade name Neurontin), a structural analog of γ-aminobutyric acid (GABA), BCS class 3 drug with having permeability issues. Objective: This work was an attempt to formulate and characterize a new approach to treat epilepsy by targeting to Phospholipase A2 Enzyme through Nanostructured Lipid Carrier. Methods: Docking studied carried out using Accelrys Discovery studio 4.1 Client and gabapentin and phosphotidylcholine were conjugated through chemical conjugation. Nanostructured lipid carrier (NLC) was prepared using hot homogenization technique. Results: The libdock score of Gabapentin- Phosphotidylcholine conjugate (192.535) were found to be more than Gabapentin (77.1084) and Phosphotidylcholine (150.212). For the optimized formulation the particle size (50.08), zeta potential (-1.48), PDI (0.472) and entrapment efficiency (77.8) was observed. The NLC was studies for in-vitro drug release studies and release kinetics. Finally found that the drug release from the NLC followed Higuchi release kinetic and the mode of drug release from the NLC was found to be Non- Fickian diffusion. Conclusion: The formulated Nanostructured lipid carrier of Gabapentin-Phosphotidylcholine conjugate may be able to use to prevent seizure.

scholarly journals Fabrication and in vitro characterization of polymeric nanoparticles for Parkinson's therapy: a novel approach

2014 ◽  
Vol 50 (4) ◽  
pp. 869-876 ◽  
Author(s):  
Neha Gulati ◽  
Upendra Nagaich ◽  
Shubhini Saraf
Keyword(s):  
Drug Release ◽  
Polymeric Nanoparticles ◽  
Release Kinetics ◽  
Mode Of Delivery ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Fickian Diffusion ◽  
Novel Approach

The objective of the research was to formulate and evaluate selegiline hydrochloride loaded chitosan nanoparticles for the Parkinson's therapy in order to improve its therapeutic effect and reducing dosing frequency. Taguchi method of design of experiments (L9 orthogonal array) was used to get optimized formulation. The selegiline hydrochloride loaded chitosan nanoparticles (SHPs) were prepared by ionic gelation of chitosan with tripolyphosphate anions (TPP) and tween 80 as surfactant. The SHPs had a mean size of (303.39 ± 2.01) nm, a zeta potential of +32.50mV, and entrapment efficiency of SHPs was 86.200 ± 1.38%. The in vitro drug release of SHPs was evaluated in phosphate buffer saline (pH 5.5) using goat nasal mucosa and found to be 82.529% ± 1.308 up to 28 h. Release kinetics studies showed that the release of drug from nanoparticles was anomalous (non-fickian) diffusion indicating the drug release is controlled by more than one process i.e. superposition of both phenomenon, the diffusion controlled as well as swelling controlled release. SHPs showed good stability results as found during stability studies at different temperatures as mentioned in ICH guidelines. The results revealed that selegiline hydrochloride loaded chitosan nanoparticles are most suitable mode of delivery of drug for promising therapeutic action.

Formulation, Design and Optimization of Glycerosomes for Topical Delivery of Minoxidil

2021 ◽  
pp. 2367-2374
Author(s):  
Deepika Rani ◽  
Vaishali Sharma ◽  
Rashmi Manchanda ◽  
Himanshu Chaurasia
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Topical Delivery ◽  
Fickian Diffusion ◽  
Glycerol Concentration ◽  
Lipid Film ◽  
Formulation Design ◽  
Design And Optimization

Background: Present work reports the formulation design and optimization of minoxidil loaded glycerosomes for topical application. The delivery system enhances the vesicular properties of vesicles by modifying the fluidity of lipid bilayer. The major component of formulation consists of phospholipid, glycerol, and cholesterol. Methodology: Glycerosomes were prepared by using lipid film hydration method. Prepared formulations were optimized using Box behnken 32 full factorial experimental designs. Two independent variables were selected which were Sonication time (X1), and Glycerol Concentration (X2) and with respect to these two dependent variables were selected which were % cumulative drug release after eight hours (Y1), and Entrapment efficiency (Y2). Nine formulations of (G1-G9) were prepared based on factorial design for optimization. Result and Discussion: Prepared formulations were evaluated in terms of surface analysis, charge distribution, encapsulation efficiency, in-vitro diffusion studies, stability testing and release kinetics. The fabricated glycerosomes found to possess entrapment efficiency in the range of 70.29±0.75 to 87.91±0.23%, cumulative drug release: 73.12 to 89.39%; a shelf life of 356 days at 4± 1°C and show higuchi release kinetics, fickian diffusion. Conclusion: As glycerol present in formulation in high quantity, this is itself used as humectant, emollient and penetration enhancer. So this formulation is best suitable for topical delivery of drugs.

scholarly journals Formulation and Evaluation of Controlled Release Maintenance Dose Loaded Niosomes of Anti-Hypertensive Drug

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
Chandani Makvana ◽  
Satyajit Sahoo
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Zeta Potential ◽  
Drug Carrier ◽  
Entrapment Efficiency ◽  
Drug Carriers ◽  
Vesicle Size ◽  
Drug Content ◽  
Span 60

The present study was aimed to formulate, comparatively evaluate and optimize multiple lipid drug carriers of valsartan for oral controlled release to overcome the problems associated with the drug such as bioavailability, to reduce the dosage regimen, half life and to determine the appropriateness of niosomal formulation as a drug carrier. Ether injection method was chosen for the formulation of physically and chemically stable niosomes of valsartan. The formulation and process parameters were optimized by manufacturing placebo niosomes. Than drug loaded niosome was prepared by varying the concentration of span 60. The prepared nine formulations were evaluated for various parameters. Placebo niosomes were evaluated for appearance, odour, texture, creaming volume, pH and changes after 15 days. The medicated nine formulations were evaluated for organoleptic properties (appearance/color, odour), pH, total drug content, entrapment efficiency, mean particle size and polydispersibility index, zeta potential and In-vitro drug release. All formulations were off-white in color, odourless, and fluid in nature. It was stable and did not show sedimentation. The pH was found to be in the range of 4.6-5.4. Drug content was found in the range of 89.13 to 99.52. The Entrapment efficiency was found in range of 79.05 to 98.24. The mean vesicle size of drug loaded niosomes of the different batches ranged between 2.52-3.42μm. The polydispersvity index was in the range of 0.325 to 0.420 which indicates a narrow vesicle size distribution. The values of zeta potential were in the range of -20.29 mV to -30.55 mV which indicates that niosome had sufficient charge and mobility to inhibit aggregation of vesicles. All the nine formulations shows constant drug release in controlled manner up to 24 h. Formulation V7 was considered to be the best formulation as the % drug content (99.52 ± 0.97), % entrapment efficiency (98.24 ± 1.50) and % drug release at the end of 24th h (98.55) were high for V7. The optimized formulation V7 showed higher degree of correlation coefficient (r2) 0.9805 which indicates process of constant drug release from dosage form. The present study concludes that the prepared niosome is a convenient and efficiency carrier for the delivery of antihypertensive drug. Besides this, it provided controlled delivery of drug.

scholarly journals Effects of drug solubility on the release kinetics of water soluble and insoluble drugs from HPMC based matrix formulations

2009 ◽  
Vol 59 (3) ◽  
pp. 313-323 ◽  
Author(s):  
Santanu Chakraborty ◽  
Madhusmruti Khandai ◽  
Anuradha Sharma ◽  
Ch. Patra ◽  
V. Patro ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Research Work ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Physical Parameters ◽  
Drug Solubility ◽  
Significant Difference ◽  
Insoluble Drugs ◽  
Kinetics Of

Effects of drug solubility on the release kinetics of water soluble and insoluble drugs from HPMC based matrix formulations The purpose of the present research work was to observe the effects of drug solubility on their release kinetics of water soluble verpamil hydrochloride and insoluble aceclofenac from hydrophilic polymer based matrix formulations. Matrix formulations were prepared by the direct compression method. The formulations were evaluated for various physical parameters. Along with the dynamics of water uptake and erosion, SEM and in vitro drug release of the tablets were studied. Applying an exponential equation, it was found that the kinetics of soluble drug release followed anomalous non-Fickian diffusion transport whereas insoluble drug showed zero-order release. SEM study showed pore formation on the tablet surface that differed depending on drug solubility. t-Test pointed to a significant difference in amount of both drugs released due to the difference in solubility. Solubility of the drug effects kinetics and the mechanism of drug release.

scholarly journals PHYSICAL PROPERTIES AND RATE OF DIFFUSION TRANSETHOSOME CURCUMIN USING A COMBINATION OF TWEEN 60 AND SPAN 60 AS SURFACTANT

2021 ◽  
pp. 66-70
Author(s):  
ANISA AMALIA ◽  
YUDI SRIFIANA ◽  
AMALIA ANWAR
Keyword(s):  
Particle Size ◽  
Physical Properties ◽  
Diffusion Rate ◽  
Entrapment Efficiency ◽  
Zero Order Kinetics ◽  
Significant Difference ◽  
Tween 60 ◽  
Span 60

Objective: Curcumin penetration can be increased by formulating it into the transethosome system. Surfactant is one of the transethosome components that affect the physical properties and penetration of vesicles. In this study, a combination of two surfactants was used to see the effect of surfactants on physical properties and curcumin penetration. Methods: This study used a combination of tween 60 and span 60 with a concentration ratio of 0:5 (F1), 1:1 (F2), 2:1 (F3), and 1:2 (F4). An evaluation included testing the distribution of particle size, zeta potential, and entrapment efficiency in the system. Evaluation continued with the determination of the diffusion rate in vitro.  Results: The transethosome system formed has a particle size of 167.9±4.7 nm-396±3.7 nm with a potential zeta value (-) 49.54±1.77 mV-(-) 59.05±0.95 mV, polydispersion index 0.0%-57.1% and entrapment efficiency of 83.76%-93.75%. The diffusion rate of F1 and F3 followed the Higuchi kinetics model, while F2 and F4 followed zero-order kinetics and the Korsmeyer-Peppas kinetics. Conclusion: The combination of tween 60 and span 60 could form a nano-sized transethosome of curcumin. Diffusion rate testing results show that using a surfactant combination can increase the diffusion rate of curcumin, where there is a significant difference between each formula (p<0.05).

scholarly journals FORMULATION AND EVALUATION OF PRONIOSOMAL GEL-BASED TRANSDERMAL DELIVERY OF ATORVASTATIN CALCIUM BY BOX–BEHNKEN DESIGN

2019 ◽  
pp. 335-343 ◽  
Author(s):  
SOUJANYA C ◽  
RAVI PRAKASH P
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Skin Permeation ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Transmission Electron Microscopy Analysis ◽  
Box Behnken Design ◽  
Atorvastatin Calcium ◽  
Span 60

Objective: The aim of this study was to investigate the combined influence of three independent variables in the preparation of atorvastatin proniosomes by coacervation-phase separation method. Methods: On the basis of the preliminary trials, a 3-factor, 3-level Box–Behnken design was employed to study the effect of cholesterol, soya lecithin, and Span 60 independent variable on dependent variables (particle size and % entrapment efficiency). Transmission electron microscopy analysis of optimized formulation has demonstrated the presence of individual proniosomes in spherical shape. Results: Atorvastatin optimized proniosomal formulation F2 shown better particle size and % entrapment efficiency, and also, the drug release was 99.72% within 24 h in slow and controlled manner when compared with control. Kinetic analysis of drug release profiles showed that the drug release was followed by zero-order manner with Korsmeyer–Peppas model, which implies super case II release kinetics. The particle size and zeta potential of the optimized atorvastatin proniosomal gel were found to be 65.72 and −10.5, respectively. The optimized batch of proniosomes was used for the preparation of atorvastatin-based proniosomal hydrogel by incorporating hydrated proniosomes to carbopol matrix to enhance the stability and viscosity of the system. Conclusion: The enhanced skin permeation, for a prolonged period of time, may lead to improved efficacy and better patient compliance. This study suggests that proniosomal gel-containing atorvastatin could perform therapeutically better effects than the conventional formulations.

Formulation and Evaluation of Lovastatin Loaded Nanosponges for the treatment of Hyperlipidemia

2021 ◽  
pp. 5653-5660
Author(s):  
Ranjitha R ◽  
Elango K ◽  
Devi Damayanthi R ◽  
Sahul Hameed Niyaz U
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Flow Property ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Average Particle ◽  
Stability Studies ◽  
Formulation Parameters

The present investigations was aimed to improve the solubility, to release the drug in a controlled manner for extended period of time, reduce dose dependent side effects and improve the bioavailability of a poorly water soluble BCS class II drug of Lovastatin by formulating it as Nanosponges drug delivery system. Lovastatin Nanosponges were formulated by emulsion solvent evaporation method using Eudragit RS 100 and Ethyl Cellulose as a polymers, PVA as a stabilizer and finally enclosed in hard gelatin Capsules. The prepared Nanosponges were evaluated for FTIR, particle size, polydispersity index (PDI), zeta potential, morphological characteristics by scanning electron microscopy (SEM), production yield, entrapment efficiency, solubility studies, in vitro drug release studies, release kinetics study, stability studies, Flow property and porosity. The optimized formulation filled in capsules and Post formulation parameters of capsule were determined. FTIR studies showed no interaction between drug and excipients. Percentage yield of all the formulation (F1-F10) was found to be in the range of 85.83 to 99.85%. The entrapment efficiency of all the formulations was found to be in the range of 61.68 to 91.18%, among all the formulations F3 (90.04%) and F8 (91.18%) shows high entrapment efficiency. The solubility of all formulation improved (from insoluble to slightly soluble) compared to pure drug of Lovastatin. Among all the formulations F3 (98.15%) and F8 (97.57%) shown complete drug release at the end of 12th hrs. The average particle size of optimized formulation F3 and F8 was found to be 727.0 nm and 769.5 nm respectively. SEM images of optimized formulation showed that the Nanosponges were spherical with numerous pores on their surface, uniform and spongy in nature. The release kinetics of the optimized formulation was best fitted into Higuchi model and showed zero order drug release with Non Fickian diffusion. Stability studies indicated that the formulation is stable as per ICH guidelines. The flow property measurements for optimized formulation observed good were its filled in capsules. Post formulation parameters of capsule were comply with official specifications. They concluded that the both polymers used were efficient carriers for Lovastatin Nanosponges.

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