Preparation, characterizations and in vitro evaluation of Econazole-Btamethasone loaded solid lipid nanoparticles (SLNs)

2021 ◽  
pp. 1-12
Author(s):  
Kamran Khan ◽  
Shefaat Ullah Shah ◽  
Yusuf S. Althobaithi ◽  
Kifayat Ullah Shah ◽  
Aman Ullah ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Side Effects ◽  
Drug Release ◽  
Oral Delivery ◽  
Encapsulation Efficiency ◽  
Fungal Infections ◽  
Ex Vivo ◽  
Sem Images ◽  
Drug Content

Tremendous increase of fungal infections in hospitalized or immune compromised patients has been reported from the last two decades. These infections are commonly treated using econazole and miconazole that have shorter half-life and produce severe side effects. All such issues can be addressed using targeted drug delivery. We developed SNLs based formulation for the treatment of mycosis. The high pressure homogenization method was employed for formulation followed by characterization, assay for antifungal activity, in vitro drug release and ex vivo permeation. The particle size of Econazole-Betamethasone-loaded SLNs, Econazole-loaded SLNs, Betamethasone-loaded SLNs and Blank SLNs were 377.4±23 nm, 298.7±9 nm, 177.7±15 nm and 113.4±6 nm respectively. The SEM images displayed that droplets are uniform and spherical in shape which ranged from 113.4±6 to 377.4±23 nm. In DSC, the SLNs formulation showed endothermic peak at 185.2 °C±0.9. Drug content of Econazole loaded SLNs was 82±0.1 and its entrapment efficiency was approximately 90.4±0.2. Betamethasone SLNs displayed highest drug content which was 83.5±0.4 while encapsulation efficiency of same formulation was 94.2±0.4. The Econazole and Betamethasone combined SLNs exhibited drug content of 80±0.3 while its encapsulation efficiency was 93.1±0.5. E-SLNs have significantly high drug release (p <  0.05) as compared to other formulation B-SLNs and EB-SLNs.The Econazole loaded formulations displayed antifungal activity with no synergistic or antagonistic effect with each other. Drug permeation from Econazole SLNs, Betamethasone SLNs and combined Econazole and Betamethasone SLNs was 45%, 40% and 38% respectively. Overall, SLN’s are an effective carrier for topical delivery of antifungals agents and that may be helpful in bypassing the serious side effects associated with oral 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 FORMULATION OF KETOCONAZOLE LOADED NANO DISPERSIVE GEL USING SWOLLEN MICELLES TECHNIQUE AND ITS IN VITRO CHARACTERIZATION

2018 ◽  
Vol 10 (3) ◽  
pp. 162
Author(s):  
Mohammad Irshad Reza ◽  
Divya Goel ◽  
Rahul Kumar Gupta ◽  
Musarrat Hussain Warsi
Keyword(s):  
Antifungal Activity ◽  
Drug Release ◽  
Ex Vivo ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Permeation Study ◽  
Ex Vivo Permeation ◽  
Enhanced Solubility ◽  
Ex Vivo Permeation Study

Objective: The objective of the present work was to formulate and characterize nano dispersive gel (NDG) for topical delivery of water-insoluble antifungal agent ketoconazole in order to enhance its solubility, penetration through the skin and antifungal activity.Methods: Nano dispersion of the drug was first prepared by swollen micelles technique (SMT) using tween 80 and chloroform which is then incorporated into the gel using carbopol 934. Ten formulations of ketoconazole loaded NDG was prepared and characterized for different physicochemical parameters like homogeneity, pH, spreadability, extrudability, practical yield, drug content, in vitro drug release, ex vivo permeation study, and biological parameter antifungal activity.Results: The formulated topical preparation exhibit pH in the range of 6.5 to 7.4, and unveiled excellent homogeneity, spreadability and extrudability. Out of 10 formulations, formulation F4 showed maximum drug content of 95.56±1.13% and practical yield of 97.23±0.51%. The in vitro drug release studies were performed using pH 7.4 phosphate buffer. Formulation F4 showed best in vitro drug release 96.52±0.52% at the end of 24 h of study. Ex vivo permeation study of formulation F4 carried out using franz diffusion cell, also manifested good permeation and flux of drug across the chicken skin. Antifungal activity test of formulation F4 was carried out by the cup plate method using Aspergillus niger strain against marketed ketoconazole unveiled higher antifungal activity than marketed one.Conclusion: The study confirmed formulation F4 to be an optimized and promising formulation for the effective treatment of topical fungal infections with enhanced solubility and penetration through the skin.

Synthesis and characterization of Chitosan-Catechol conjugates: Development and in vitro, in silico and in vivo evaluation of mucoadhesive pellets of lafutidine

2021 ◽  
pp. 088391152199784
Author(s):  
Loveleen Kaur ◽  
Ajay Kumar Thakur ◽  
Pradeep Kumar ◽  
Inderbir Singh
Keyword(s):  
Drug Release ◽  
In Silico ◽  
Ex Vivo ◽  
Strong Interactions ◽  
Dissolution Time ◽  
Sem Images ◽  
In Vivo Evaluation ◽  
Release Studies

Present study was aimed to synthesize and characterize Chitosan-Catechol conjugates and to design and develop mucoadhesive pellets loaded with lafutidine. SEM images indicated the presence of fibrous structures responsible for enhanced mucoadhesive potential of Chitosan-Catechol conjugates. Thermodynamic stability and amorphous nature of conjugates was confirmed by DSC and XRD studies respectively. Rheological studies were used to evaluate polymer mucin interactions wherein strong interactions between Chitosan-Catechol conjugate and mucin was observed in comparison to pristine chitosan and mucin. The mucoadhesion potential of Chitosan-Catechol (Cht-C) versus Chitosan (Cht) was assessed in silico using molecular mechanics simulations and the results obtained were compared with the in vitro and ex vivo results. Cht-C/mucin demonstrated much higher energy stabilization (∆E ≈ −65 kcal/mol) as compared to Cht/mucin molecular complex. Lafutidine-loaded pellets were prepared from Chitosan (LPC) and Chitosan-Catechol conjugates (LPCC) and were evaluated for various physical properties viz. flow, circularity, roundness, friability, drug content, particle size and percent mucoadhesion. In vitro drug release studies on LPC and LPCC pellets were performed for computing t50%, t90% and mean dissolution time. The values of release exponent from Korsmeyer-Peppas model was reported to be 0.443 and 0.759 for LPC and LPCC pellets suggesting Fickian and non-Fickian mechanism representing drug release, respectively. In vivo results depicted significant controlled release and enhanced residence of the drug after being released from the chitosan-catechol coated pellets. Chitosan-Catechol conjugates were found to be a promising biooadhesive polymer for the development of various mucoadhesive formulations.

scholarly journals DEVELOPMENT AND EVALUATION OF TRANSDERMAL FILM CONTAINING SOLID LIPID NANOPARTICLES OF RIVASTIGMINE TARTRATE

2017 ◽  
Vol 9 (6) ◽  
pp. 85
Author(s):  
G. Ravi ◽  
N. Vishal Gupta
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Cost Effective ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Study Results ◽  
Transdermal Film

Objective: The objective of present investigation was to develop rivastigmine tartrate transdermal film employing factorial design.Methods: The formulations were designed by Design-Expert software-version10. A series of films were prepared by solvent casting method using polymers, plasticizer, permeation enhancer and other solvents. Transdermal films were evaluated for flatness, drug content, tensile strength, in vitro drug release and ex vivo skin permeation study.Results: The flatness was found 100% (percentage) for all film formulations. The drug content of transdermal film was found in the range of 96.51±0.2 to 98.81±0.3%. The tensile strength of transdermal film was found in the range of 6.28±0.06 to 11.56±0.03 N/mm2 (newton/millimeter2) and in vitro drug release at 24th h (hour) was found in the range of 86.24±0.25 to 96.1±0.48%% for various formulations and ex vivo skin permeation study results at 24th h was found in the range of 85.83±0.74 to 97.36±0.93%.Conclusion: These results support the feasibility of developing transdermal film of rivastigmine tartrate for human applications. Thus, transdermal delivery of rivastigmine tartrate film is a safe, painless and cost effective drug delivery system for Alzheimer’s patients.

scholarly journals Development and Evaluations of Transdermally Delivered Luteolin Loaded Cationic Nanoemulsion: In Vitro and Ex Vivo Evaluations

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1218
Author(s):  
Mohammad A. Altamimi ◽  
Afzal Hussain ◽  
Sultan Alshehri ◽  
Syed Sarim Imam ◽  
Usamah Abdulrahman Alnemer
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Transdermal Delivery ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Oral Drug ◽  
In Vitro Drug Release ◽  
Drug Deposition ◽  
Drug Content

Introduction: Luteolin (LUT) is natural flavonoid with multiple therapeutic potentials and is explored for transdermal delivery using a nanocarrier system. LUT loaded cationic nanoemulsions (CNE1–CNE9) using bergamot oil (BO) were developed, optimized, and characterized in terms of in vitro and ex vivo parameters for improved permeation. Materials and methods: The solubility study of LUT was carried out in selected excipients, namely BO, cremophor EL (CEL as surfactant), labrasol (LAB), and oleylamine (OA as cationic charge inducer). Formulations were characterized with globular size, polydispersity index (PDI), zeta potential, pH, and thermodynamic stability studies. The optimized formulation (CNE4) was selected for comparative investigations (% transmittance as %T, morphology, chemical compatibility, drug content, in vitro % drug release, ex vivo skin permeation, and drug deposition, DD) against ANE4 (anionic nanoemulsion for comparison) and drug suspension (DS). Results: Formulations such as CNE1–CNE9 and ANE4 (except CNE6 and CNE8) were found to be stable. The optimized CNE4 based on the lowest value of globular size (112 nm), minimum PDI (0.15), and optimum zeta potential (+26 mV) was selected for comparative assessment against ANE4 and DS. The %T values of CNE1–CNE9 were found to be ˃95% and CEL content slightly improved the %T value. The spherical CNE4 was compatible with excipients and showed % total drug content in the range of 97.9–99.7%. In vitro drug release values from CNE4 and ANE4 were significantly higher than DS. Moreover, permeation flux (138.82 ± 8.4 µg/cm2·h), enhancement ratio (8.23), and DD (10.98%) were remarkably higher than DS. Thus, ex vivo parameters were relatively high as compared to DS which may be attributed to nanonization, surfactant-mediated reversible changes in skin lipid matrix, and electrostatic interaction of nanoglobules with the cellular surface. Conclusion: Transdermal delivery of LUT can be a suitable alternative to oral drug delivery for augmented skin permeation and drug deposition.

Fabrication and Characterization of Ocular Phase Transition Systems for Blepharitis: A Novel Approach

2020 ◽  
Vol 10 (1) ◽  
pp. 24-37
Author(s):  
Deepali Verma ◽  
Shreya Kaul ◽  
Neha Jain ◽  
Upendra Nagaich
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Eye Drops ◽  
Stability Studies ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Drug Content ◽  
Erythromycin Estolate

Introduction: In the present research, erythromycin estolate loaded in-situ gel was formulated and evaluated for blepharitis in order to improve its therapeutic efficacy, precorneal residence time of the system and to enhance the ocular bioavailability. Material and Methods: The developed formulation was characterized by several parameters viz. FTIR, clarity, pH, gelation temperature, rheological studies, drug content, in vitro drug release studies, transcorneal permeation studies, bioadhesion studies, isotonicity and stability studies. Results: The optimized formulation exhibited non-fickian release diffusion with a sustained release of drug 82.76 ± 0.94% up to 8h and drug content 93.64%. Isotonicity revealed that the formulation was isotonic in nature and there was no shrinkage and busting of cells. Bioadhesion study was performed to check the adherence of the prepared in situ gel to the corneal surface for 4h. Ex vivo transcorneal permeation was observed to be significantly higher when compared with market eye drops. Histopathological studies were conducted to confirm the presence of normal ocular surface tissues by maintaining their morphological structures without causing damage to the tissues. The formulation was nonirritant as confirmed by the HET-CAM test. Stability studies and accelerated stability studies were conducted for 13 weeks and 26 weeks respectively and formulations were analyzed for the visual appearance, pH, viscosity, gelling capacity, drug content and in vitro drug release and results showed no change in the formulations. Conclusion: The formulation was therapeutically efficacious, sterile, stable and provided controlled release over a period of time. The developed system could be a viable alternative to conventional eye drops for treatment of various ocular diseases.

scholarly journals Formulation and Evaluation of Minoxidil Gel Using Acrylamide/Sodium Acryloyldimethyl taurate copolymer for Alopecia areata

2018 ◽  
Vol 10 (01) ◽  
Author(s):  
Shailendra Kumar Singh ◽  
Pawan Kumar ◽  
Deepak Kumar Jindal ◽  
Vandana Handa ◽  
Jyoti Bilonia
Keyword(s):  
Drug Release ◽  
Alopecia Areata ◽  
Ex Vivo ◽  
Skin Permeation ◽  
In Vitro Release ◽  
Chronic Inflammatory Disease ◽  
Effective Dosage ◽  
World Population ◽  
Drug Content

Alopecia areata is a common, chronic inflammatory disease, characterized by patchy hair loss on the scalp, affecting about 2.1% of world population. Presently, minoxidil has been used for treatment of alopecia as topical lotion, but associated with many drawbacks like systemic side effects and low contact time with skin. Therefore, in the present work, minoxidil gel was prepared using a novel copolymer, Sepineo P 600 to overcome these drawbacks. The prepared gel was characterized for pH, drug content, viscosity, spreadability, skin adhesivity, occlusivity, in vitro drug release, ex vivo skin permeation, stability and finally for skin corrosivity. The drug content of the finalized gel was found to be 99.80 ± 0.82%. The formulation showed good spreadability, occlusivity, adhesiveness and viscosity. In vitro release studies showed that the drug release from prepared gel followed matrix release pattern as compared to lotion. Mathematical modelling of the drug release data suggested Higuchi release model. The formulated minoxidil gel was found to be non-corrosive and stable when subjected to accelerate as well as real time stability studies. Overall, the minoxidil gel formulation was suitable for skin application and can be an effective dosage form for the treatment of Alopecia areata.

scholarly journals Antifungal activities of quince seed mucilage hydrogel decorated with essential oils of Nigella sativa, Citrus sinensis and Cinnamon verum

2021 ◽  
Author(s):  
Mehdi Mirzaii ◽  
Marzieh Yaeghoobi ◽  
Meysam Afzali ◽  
Neginsadat Amirkhalili ◽  
Majid Mahmoodi ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Side Effects ◽  
Essential Oils ◽  
Ultrasonic Treatment ◽  
Fungal Infections ◽  
Vitro Assay ◽  
Antifungal Activities ◽  
Antifungal Properties

Background and Objectives: Candidiasis and pityriasis versicolor are opportunistic fungal infections that are caused by Candida spp. and Malassezia spp. yeasts. Conventional drugs like azole and amino derivatives are known to treat fungal skin diseases. However, drawbacks like long-term side effects and drug resistance lead to investigate on antifungal properties of phytochemicals as an alternative to available synthetic drugs. Materials and Methods: The herbal nano hydrogel was successfully synthesized from Quince Seed extract followed by ultrasonic treatment and it has been formulated using a mixture of essential oils. We evaluated the antifungal in vitro assay for a mixture of essential oils in combination with herbal nano hydrogel against Candida albicans and Malasezia furfur strains by micro dilution method. Results: The results indicated that essential oils possess antifungal activity with the MIC value of 12.5 and 6.24 mg/ml against C. albicans and M. furfur, respectively. No fungicidal effect was reported for the herbal hydrogel before nanofabrication while it shown some antifungal activity after ultrasonic treatment for 5 and 10 minutes. As anticipated; the antifungal property of essential oil mixture was appreciably improved when it combined with herbal nano hydrogel where the highest level of inhibition was observed at concentration of 3.125 mg/ml for both strains. The loss in biological activity observed when the ultrasonic treatment on herbal nano hydrogel performed for longer time. Conclusion: The proposed plant-based nano formulation shown promising in vitro antifungal activities against C. albicans and M. furfur strains and its antifungal properties were comparable with commercially available agents like clotrimazole. The new formulation expected to be safe with minimum long-term side effects. Further investigations are underway to confirm the safety and the mechanism of the action of this new herbal formulation.

Development of Effervescent Tablets of Alendronate Sodium with Improved Intestinal Permeation

2018 ◽  
Vol 11 (1) ◽  
pp. 3990-3997
Author(s):  
Prasad Vure ◽  
Sundeep Chaurasia
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Alendronate Sodium ◽  
Drug Content ◽  
Weight Variation ◽  
Permeation Studies ◽  
Intestinal Permeation

The aim of the present study is to develop effervescent tablets of alendronate sodium to improve their intestinal permeability to treat osteoporosis. Effervescent tablets of alendronate sodium were developed with different ratios of acid to alkaline components having a pH of about 3 to about 6.5. The tablets were prepared by direct compression method. The physical mixture blend was evaluated for angle of repose, true density, bulk density, compressibility index. The formulated tablets were subjected to thickness, weight variation, hardness, friability, drug content and pH. The in vitro dissolution studies were carried out using the USP Type 2 apparatus. Formulation F14 was considered as optimized formulation because it shows drug release pattern higher than that of the other formulations and conventional marketed formulation. Ex vivo permeation studies were performed for the optimized formulation (F14) and that of the conventional marketed formulation. The drug release of the formulation (F14) was higher than the marketed formulation. Accelerated stability studies of the optimized formulation indicated that there were no signs of visually distinguishable changes, drug content and in vitro dispersion time. Thus, an increase in drug release may enhance absorption, in turn may enhance bioavailability.       

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.

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