scholarly journals DEVELOPMENT AND EVALUATION OF NANOEMULSION AS A CARRIER FOR TOPICAL DELIVERY SYSTEM BY BOX-BEHNKEN DESIGN

2018 ◽  
Vol 11 (8) ◽  
pp. 286
Author(s):  
Pallavi M Chaudhari ◽  
Madhavi A Kuchekar
Keyword(s):  
Drug Release ◽  
Ftir Spectroscopy ◽  
Ex Vivo ◽  
Topical Delivery ◽  
Homogenization Method ◽  
Permeation Rate ◽  
Scanning Calorimetry ◽  
Box Behnken Design ◽  
Globule Size

Objective: The aim of this study was to develop a nanoemulsion for topical delivery. Methods: Topical nanoemulsion was prepared by homogenization method. Box-behnken design was utilized to study the effect of oil, surfactant and Co-surfactant, on droplet size, entrapment efficiency and drug release. Nabumetone a non-steroidal anti-inflammatory drug was incorporated in castor oil with Tween 80 and Polyethylene glycol 600 to form the nanoemulsion by homogenization method. The nanoemulsion was further subjected to different evaluation parameters and ex-vivo study. The crystalline nature of drug was confirmed by powder X-ray diffraction studies. Drug-excipient compatibility was confirmed by Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), respectively. Results: The average globule size of nabumetone-containing nanoemulsion decreased with decrease in concentration of oil and surfactant. Nanoemulsion was evaluated by pH, rheology, globule size, zeta potential, scanning electron microscopy, DSC, FTIR spectroscopy, and stability. In vitro drug release shows maximum 84.35% permeation rate through cellophane membrane and ex-vivo drug release shows 86.32% permeation rate through goat skin. Conclusion: Thus, the nanoemulsion formulated showed good results regarding topical delivery.

The Development of Pemetrexed Diacid-Loaded Gelatin-Cloisite 30B (MMT) Nanocomposite for Improved Oral Efficacy Against Cancer: Characterization, In-Vitro and Ex-Vivo Assessment

2020 ◽  
Vol 17 (3) ◽  
pp. 246-256
Author(s):  
Kriti Soni ◽  
Ali Mujtaba ◽  
Md. Habban Akhter ◽  
Kanchan Kohli
Keyword(s):  
Drug Release ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Confocal Laser ◽  
Release Mechanism ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
Cloisite 30B ◽  
Ft Ir

Aim: The intention of this investigation was to develop Pemetrexed Diacid (PTX)-loaded gelatine-cloisite 30B (MMT) nanocomposite for the potential oral delivery of PTX and the in vitro, and ex vivo assessment. Background: Gelatin/Cloisite 30 B (MMT) nanocomposites were prepared by blending gelatin with MMT in aqueous solution. Methods: PTX was incorporated into the nanocomposite preparation. The nanocomposites were investigated by Fourier Transmission Infra Red Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscope (SEM) X-Ray Diffraction (XRD) and Confocal Laser Microscopy (CLSM). FT-IR of nanocomposite showed the disappearance of all major peaks which corroborated the formation of nanocomposites. The nanocomposites were found to have a particle size of 121.9 ± 1.85 nm and zeta potential -12.1 ± 0.63 mV. DSC thermogram of drug loaded nanocomposites indicated peak at 117.165 oC and 205.816 oC, which clearly revealed that the drug has been incorporated into the nanocomposite because of cross-linking of cloisite 30 B and gelatin in the presence of glutaraldehyde. Results: SEM images of gelatin show a network like structure which disappears in the nanocomposite. The kinetics of the drug release was studied in order to ascertain the type of release mechanism. The drug release from nanocomposites was in a controlled manner, followed by first-order kinetics and the drug release mechanism was found to be of Fickian type. Conclusion: Ex vivo gut permeation studies revealed 4 times enhancement in the permeation of drug present in the nanocomposite as compared to plain drug solution and were further affirmed by CLSM. Thus, gelatin/(MMT) nanocomposite could be promising for the oral delivery of PTX in cancer therapy and future prospects for the industrial pharmacy.

scholarly journals Design and Optimization of Cationic Nanocapsules for Topical Delivery of Tretinoin: Application of the Box-Behnken Design, In Vitro Evaluation, and Ex Vivo Skin Deposition Study

2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Saeed Ebrahimi ◽  
Reza Mahjub ◽  
Rasool Haddadi ◽  
Seyed Yaser Vafaei
Keyword(s):  
Particle Size ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Topical Delivery ◽  
Free Drug ◽  
Acrylic Polymer ◽  
Box Behnken Design

Cationic nanocapsules represent a promising approach for topical delivery purposes. We elaborated on a novel formulation based on the cationic nanocapsules to enhance the pharmacodynamic efficacy, user compliance, and photostability of tretinoin (TTN). To achieve this goal, TTN nanocapsules were prepared by the nanoprecipitation method. In order to statistically optimize formulation variables, a Box-Behnken design, using Design-Expert software, was employed. Three independent variables were evaluated: total weight of the cationic acrylic polymer ( X 1 ), oil volume ( X 2 ), and TTN amount ( X 3 ). The particle size and encapsulation efficiency percent (EE%) were selected as dependent variables. The optimal formulation demonstrated spherical morphology under scanning electron microscopy (SEM), optimum particle size of 116.3 nm, and high EE% of 83.2%. TTN-loaded nanocapsules improved photostability compared to its methanolic solution. The in vitro release study data showed that tretinoin was released in a sustained manner compared to the free drug. The ex vivo skin permeation study demonstrated that greater drug deposition into the epidermal region rather than the deep skin was observed with a gel containing TTN-loaded nanocapsules than that of drug solution, respectively. The skin irritation test revealed that the nanoencapsulation of the drug decreased its irritancy compared to the free drug. These results revealed the promising potential of cationic nanocapsules for topical delivery of tretinoin

Fast Dissolving Sublingual Strips: A Novel Approach for the Delivery of Isosorbide Dinitrate

2019 ◽  
Vol 25 (4) ◽  
pp. 311-318
Author(s):  
Marzieh Fathei ◽  
Mitra Alami-milani ◽  
Sara Salatin ◽  
Sharahm Sattari ◽  
Hassan Montazam ◽  
...  
Keyword(s):  
Drug Release ◽  
Isosorbide Dinitrate ◽  
Moisture Absorption ◽  
Ex Vivo ◽  
Hydroxypropyl Methylcellulose ◽  
Drug Bioavailability ◽  
Scanning Calorimetry ◽  
Surface Ph ◽  
Drug Content

Background: Isosorbide dinitrate (ISDN) is used for treating the angina attacks. In addition, oral ISDN is available in immediate and sustained release formulations and the bioavailability of ISDN is about 20-25% when taken orally. Further, the ISDN films are developed for sublingual drug delivery by improving drug bioavailability. The present study aimed to design and evaluate the physicochemical properties of the film formulation for sublingual delivery of ISDN. Methods: In the present study, sublingual films were prepared by the solvent casting technique using the hydroxypropyl methylcellulose (HPMC) polymers (i.e., 100, 150 and 200 mg) with a different drug to polymer ratios (i.e., 1:5, 1:7.5 and 1:10). Then, ISDN was evaluated for the film appearance, drug content, surface pH, mucoadhesion force, differential scanning calorimetry (DSC), in vitro drug release, and ex vivo permeability. Results: Based on the results, F3 formulation (1:10 ISDN to HPMC ratio) showed acceptable thickness (0.93 mm), weight (11.14 mg), surface pH (7.82), moisture absorption capacity (6.08%), elasticity (>200), mucoadhesion force (18.05 N/cm2), and drug content (6.22%). Furthermore, the results demonstrated that HPMC polymer improved the characteristics of the films, modified the bioadhesiveness, and finally, enhanced elasticity. However, DSC thermogram failed to show any crystalline drug substance in the films except for F1 (immediate release) and the endothermic peak of ISDN was absent in F2 and F3 films. Therefore, the drug which was entrapped into the film was in an amorphous or disturbed-crystalline phase of the molecular dispersion or dissolved in the melted polymer in the polymeric matrix. Moreover, the drug release from the films was faster compared to the tablet® (P<0.05). Conclusion: In general, the formulation of F1 was observed to be an appropriate candidate for developing the sublingual film for the remedial use.

scholarly journals Optimization of Microemulgel for Tizanidine Hydrochloride

2020 ◽  
Vol 19 (2) ◽  
pp. 158-179
Author(s):  
Swati Jagdale ◽  
Sujata Brahmane ◽  
Anuruddha Chabukswar
Keyword(s):  
Spinal Cord ◽  
Drug Release ◽  
Zeta Potential ◽  
Ternary Phase Diagram ◽  
Ex Vivo ◽  
Research Work ◽  
Isopropyl Myristate ◽  
Globule Size ◽  
Cord Injury

Background: Tizanidine hydrochloride acts centrally as a muscle relaxant. It is used for the treatment of painful muscle spasm, spasticity associated with multiple sclerosis or spinal cord injury and treatment of muscle spasticity in spinal cord disease. Tizanidine hydrochloride belongs to BCS class II. It has low oral bioavailability and short halflife. Incorporating this drug in microemulgel is an excellent way to overcome problems associated with the drug. Objective: Present research work was aimed to develop and optimize a microemulsion based gel system for tizanidine hydrochloride. Methods: Screening of oil, surfactant and co-surfactant was carried out. Ternary phase diagram was constructed to obtain concentration range of components. The prepared microemulsion was evaluated for pH, globule size, zeta potential, conductivity, density and viscosity. 32 level factorial design was applied to study the effect of concentration of carbopol 934 and HPMC K15M on % cumulative drug release and viscosity of microemulgel using software Design Expert. Microemulgel was evaluated for pH, spreadability, viscosity, syneresis, drug content, bioadhesive strength, in-vitro as well as ex-vivo diffusion study. Results: Microemulsion was prepared by using isopropyl myristate as oil, tween 80 as a surfactant and transcutol P as cosurfactant. Largest transparent microemulsion region was found with Smix ratio of 1:1. FE-SEM showed globule size 28μm for batch B1 and zeta potential was -1.27mV indicating good stability of the microemulsion. Optimised batch was F6 which showed 92% drug release within 8 hours. It followed the Korsmeyer-Peppas model. Conclusion: A stable, effective and elegant microemulgel formulation, exhibiting good in-vitro and ex-vivo drug release was formulated.

Silver sulfadiazine loaded breathable hydrogel sponge for wound healing

2020 ◽  
Vol 0 (0) ◽  
Author(s):  
Anamika Pandey ◽  
Munira Momin ◽  
Anita Chando
Keyword(s):  
Wound Healing ◽  
Drug Release ◽  
Ex Vivo ◽  
Release Kinetics ◽  
Antimicrobial Property ◽  
Morphological Characteristics ◽  
Silver Sulfadiazine ◽  
Scanning Calorimetry ◽  
Casting Technique

AbstractObjectivesPatients with serious injury need special care and treatment to control the infection, as wound sepsis is one of the major causes of death. Silver sulfadiazine (SSD) is widely used as an antimicrobial agent which promotes healing and re-epithelialization. However, due to certain drawbacks such as inflammation and cytotoxicity, the need for novel drug delivery modality emerges. The objective of this study was to develop natural polymeric (chitosan and gelatin) hydrogel sponges containing SSD and evaluate its efficacy in wound healing using animal models.MethodsSSD containing hydrogel sponges were prepared by solvent casting technique. Scanning electron microscopy (SEM) and Differential scanning calorimetry (DSC) were used to evaluate morphological characteristics of the hydrogel sponges. Anti-thrombogenic property, drug release studies, drug release kinetics, antimicrobial property, and wound healing effect were also studied in detail.ResultsThe optimized batch of hydrogel sponges (CG4) consists of 1% SSD wt., 10% wt. Gelatin, 1% wt. Chitosan and honey 7.5% wt. as plasticizer. At the 12th hour, in vitro and ex vivo drug release was found to be 76.994±0.67% and 24.22±0.57% respectively. CG4 batch had enhanced in vitro antimicrobial activity as compared to conventional marketed cream. The developed SSD hydrogel sponges showed a faster rate of wound healing as compared to a marketed cream. Animals treated with CG4 formulation showed complete angiogenesis and re-epithelialization by 8th day, whereas 12 days were required for complete wound healing with marketed cream.ConclusionsThe prepared hydrogel sponges can serve as a potential alternative for wound healing dressing as compared to the marketed product.

Development and Characterization of Water-in-Oil Microemulsion for Transdermal Delivery of Eperisone Hydrochloride

2020 ◽  
Vol 7 (1) ◽  
pp. 45-64
Author(s):  
Monika D. Kumbhar ◽  
Manisha S. Karpe ◽  
Vilasrao J. Kadam
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Droplet Size ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Tween 80 ◽  
Physical Parameters ◽  
Scanning Calorimetry ◽  
Spontaneous Emulsification

Background: Eperisone hydrochloride possesses short biological half-life due to first pass metabolism resulting in low bioavailability and short duration of response with toxic effects, ultimately limits its utilization for treatment of muscle spasm. Objective: In view of this background, current study was designed for the development of Eperisone hydrochloride-loaded microemulsion and Eperisone hydrochloride-loaded microemulsion based cream for topical delivery and compared it with conventional cream. Methods: Firstly, water-in-oil microemulsion was prepared by spontaneous emulsification method. The concentration of components was found out from existence of microemulsion region by constructing pseudoternary phase diagram. The oil was selected on the basis of drug solubility effect on the drug release, whereas surfactant and cosurfactant were screened on the basis of their efficiency to form microemulsion region. The influence of components on microemulsion formation, drug release capacity, permeation was studied by differential scanning calorimetry, X-ray diffraction, in-vitro release and ex-vivo drug permeation studies respectively. By using microemulsion, the cream was prepared for proving optimum structure for topical application. Microemulsion was evaluated for droplet size, zeta potential, pH, viscosity and conductivity. Besides the cream was characterized for pH, rheology and stability. Permeation of EPE from microemulsion across the rat skin was evaluated and compared with conventional cream. Results: The microemulsion consisting Isopropyl Myristrate/Water/Span 80:Tween 80 (50/8/42% by weight) possessed droplet size of 95.77nm, zeta potential of −5.23 mV with 7.25 pH and conductivity near to zero (<0.05mScm-1). Physical parameters of the cream were satisfactory, also 2.33-fold higher permeation and 1.57-fold higher release observed as compared to conventional cream. Conclusion: It can be concluded that Eperisone hydrochloride-loaded microemulsion and its cream is being effectively used for muscle spasticity by topical route.

Formulation Optimization and Evaluation of Nanostructured Lipid Carriers Containing Valsartan

2013 ◽  
Vol 6 (2) ◽  
pp. 2077-2086
Author(s):  
Ravish J Patel ◽  
Zil P Patel
Keyword(s):  
Drug Release ◽  
Oral Bioavailability ◽  
Ex Vivo ◽  
Drug Loading ◽  
Nanostructured Lipid Carriers ◽  
Spherical Particles ◽  
Lymphatic Absorption ◽  
Scanning Calorimetry ◽  
First Pass

Nanostructured lipid carriers (NLCs), a lipid based colloidal carrier system, offer many advantages such as increase the solubility, improves the bioavailability and therapeutic efficacy. Incorporation of liquid lipid can improve the drug loading capacity in the NLCs. Valsartan is an antihypertensive drug with low oral bioavailability ranging from 10-35% because of poor solubility and extensive first pass hepatic metabolism. The purpose of present study was to develop and characterize the valsartan loaded nanostructured lipid carriers (Val-NLCs) to enhance the solubility, bypass the hepatic first-pass metabolism, and enhance the lymphatic absorption leading to greater oral bioavailability. Valsartan loaded NLCs were prepared by melt emulsification method and optimized using a two level full factorial design. Effect of content of Capmul MCM EP on crystallinity of tristearin was studied by differential scanning calorimetry (DSC) method. The particle size, entrapment efficiency, drug loading and zeta potential values of optimized batch were 62±0.494 nm, 86.59±0.671, 8.65±0.06 % and -17.4 mV, respectively. TEM images showed spherical particles with diameter of around 50 nm. In vitro drug release of 70% was observed at the end of 12 hrs. Ex-vivo drug release of 90% was observed in 2 hrs. Stability study indicated that the prepared Val-NLCs suspension was stable at refrigerator conditions for one month. Lyophilization produced free flowing Val-NLCs powder from suspension and was easy to reconstitute. Based on these results, it is concluded that NLCs are promising drug delivery for improving the oral bioavailability of valsartan.

Design and Optimization of Itraconazole Loaded SLN for Intranasal Administration Using Central Composite Design

2020 ◽  
Vol 10 (6) ◽  
pp. 884-891
Author(s):  
Sarvjeet S. Rana ◽  
Shailendra Bhatt ◽  
Manish Kumar ◽  
Anuj Malik ◽  
Jai B. Sharma ◽  
...  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Intranasal Administration ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Scanning Calorimetry ◽  
Solid Lipid ◽  
Ex Vivo Study ◽  
Central Composite

Introduction: Solid Lipid nanoparticles (SLN) are comprising of a solid lipid core with a mean diameter between 50 and 1000 nm. SLN is an advanced carrier system to traditional colloidal carriers such as emulsion, liposomes, and polymeric microparticles. Objective: The objective of this study was to formulate SLN of Itraconazole (ITZ) for intranasal administration. Methods: ITZ-loaded SLN were prepared by high pressure homogenization technique using the Central Composite Design (CCD). The concentration of surfactant (X1) and drug to lipid ratio (X2) was considered as independent variables, whereas particle size (Y1) and percentage entrapment efficiency (Y2) were considered as a response. The compatibility of ingredients with the drug was tested using differential scanning calorimetry. SLN were characterized for their particle size, entrapment efficiency, transmission electron microscopy, in vitro drug release, and ex vivo study. Results: The solid lipid nanoparticles were successfully prepared using high pressure homogenization technique and glyceryl monostearate was used as solid lipid. The lipid ratio significantly increases the particle size as well as entrapment efficiency. The particle size and (%) entrapment efficiency of optimized formulation were found to be 29 nm and 78.9%, respectively. The differential scanning calorimetry confirmed that the drug existed in amorphous form. Nasal histopathology study on sheep mucosa revealed that the developed SLN was non-toxic and safe to use for intranasal administration. The results of ex vivo study showed that the Higuchi pattern of drug release was followed. The in vitro release studies showed the significant difference in drug release from ITZ-loaded SLN compared to plain ITZ-solution. Conclusion: ITZ-loaded SLN were successfully prepared and validated. The best batch was selected based on the desired particle size, and EE which is an important characteristic for SLN formulations. The developed formulations were nontoxic as determined by histo-pathological studies.

scholarly journals FORMULATION AND EVALUATION OF ACECLOFENAC MUCOADHESIVE MICROSPHERES FOR ORAL CONTROLLED DRUG DELIVERY

2019 ◽  
pp. 184-190
Author(s):  
SAROJA SP ◽  
PREETHI SUDHEER
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Scanning Calorimetry ◽  
Electron Microscopic ◽  
Ex Vivo Permeation ◽  
Frequent Administration ◽  
Microscopic Studies

Objective: Drug delivery is a broad field of research on the development of novel materials or carrier systems for effective therapeutic delivery of drugs. The main purpose of delivering the drugs to mucosal membrane is lengthening of the residence time at site of drug delivery, followed by sustained release of the drug after the deposition. Aceclofenac is a non-steroidal anti-inflammatory drug that has a half-life of 4 h. The frequent administration of the drug irritates the gastric mucosa when it is given in conventional dosage forms. Method: Hence in this study, a mucoadhesive microsphere of biopolymer chitosan was formulated with an aim to enhance the efficacy of the drug. The microsphere of aceclofenac was prepared by o/w/o emulsification cross linking method. Results: Various ratios of drug: polymer were studied, and it was found that microspheres with 1:4 ratio was the superior in terms drug content of 87.23±0.56%.and entrapment efficiency of 85.8±0.16 %.The in vitro drug release profiles indicated a maximum drug release of 89.55± 0.62 % in 12 h. The extent of mucoadhesion and ex- vivo permeation of the drug was studied using porcine intestinal mucosal sample. The microspheres were retained on the intestinal mucosa up to 12 h. The surface of the selected microsphere formulation was observed to be uneven during surface electron microscopic studies. Infrared spectroscopy and differential scanning calorimetry studies indicated that there was no major interaction between the drug and the polymer used. Conclusion: Therefore, the studies demonstrate that mucoadhesive microspheres could be an appropriate dosage to improve the gastric retention and efficacy of aceclofenac.

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