Curcumin Loaded Ethosomal Gel for Improved Topical Delivery: Formulation, Characterization and Ex-vivo Studies

2021 ◽  
Vol 09 ◽  
Author(s):  
Bhumika Kumar ◽  
P.K. Sahoo ◽  
Satish Manchanda
Keyword(s):  
Transdermal Delivery ◽  
Smooth Surface ◽  
Therapeutic Potential ◽  
Ex Vivo ◽  
Curcuma Longa ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Active Constituent ◽  
Transdermal Penetration ◽  
Drug Solution

Background: Curcumin is a curcuminoid which is an active constituent of turmeric and is obtained from the rhizomes of Curcuma longa, family Zingiberaceae. Curcumin modulates the activity of various transcription factors and regulates the expression of inflammatory enzymes, cell survival proteins, adhesion molecules and cytokines by binding to a variety of proteins and inhibiting the activity of various kinases. Curcumin falls in the BCS class IV drug, with poor solubility and poor permeability which makes it very challenging in utilizing the maximum therapeutic potential of this moiety. Objective: The major aim of the study was to enhance transdermal penetration of curcumin via ethosomal gel and to overcome the barriers of poor permeability of transdermal drug delivery. Methods: Curcumin loaded ethosomes were prepared with varying quantities of ethanol and soya lecithin by cold method and were optimised based on entrapment efficiency, vesicular size and Ex-vivo studies. Optimised ethosomal formulation was further incorporated into a gel and was evaluated. Ex-vivo studies were performed with the ethosomal gel of curcumin and was compared with simple drug solution. Result: Prepared ethosomal system showed a vesicle size ranging from 211 to 320 nm with spherical, smooth surface and entrapment efficiency of 87 to 91%. Optimised ethosomal system (ET3) was incorporated into gel and was further evaluated. Conclusion: The findings of the research work suggested that the ethosomal gel holds an excellent potential for transdermal delivery of curcumin.

Design and Evaluation of Long Acting Biodegradable PLGA Microspheres for Ocular Drug Delivery

2019 ◽  
Vol 10 ◽  
Author(s):  
Anjali Pandya ◽  
Rajani Athawale ◽  
Durga Puro ◽  
Geeta Bhagwat
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Degradation Products ◽  
Ex Vivo ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Rational Approach ◽  
Plga Microspheres ◽  
Long Acting

Background: The research work involves development of PLGA biodegradable microspheres loaded with dexamethasome for intraocular delivery. Objective: To design and evaluate long acting PLGA microspheres for ocular delivery of dexamethasone. Method: Present formulation involves the development of long acting dexamethasone loaded microspheres composed of a biodegradable controlled release polymer, Poly(D, L- lactide-co-glycolide) (PLGA), for the treatment of posterior segment eye disorders intravitreally. PLGA with monomer ratio of 50:50 of lactic acid to glycolic acid was used to achieve a drug release up to 45 days. Quality by Design approach was utilized for designing the experiments. Single emulsion solvent evaporation technique along with high pressure homogenization was used to facilitate formation of microspheres. Results: Particle size evaluation, drug content and drug entrapment efficiency were determined for the microspheres. Particle size and morphology was observed using Field Emission Gun-Scanning Electron Microscopy (FEG-SEM) and microspheres were in the size range of 1-5 μm. Assessment of drug release was done using in vitro studies and transretinal permeation was observed by ex vivo studies using goat retinal tissues. Conclusion: Considering the dire need for prolonged therapeutic effect in diseases of the posterior eye, an intravitreal long acting formulation was designed. Use of biodegradable polymer with biocompatible degradation products was a rational approach to achieve this aim. Outcome from present research shows that developed microspheres would provide a long acting drug profile and reduce the frequency of administration thereby improving patient compliance.

scholarly journals Topical Delivery of Meloxicam using Liposome and Microemulsion Formulation Approaches

Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 282 ◽  
Author(s):  
Julia Zhang ◽  
Anna Froelich ◽  
Bozena Michniak-Kohn
Keyword(s):  
Transdermal Delivery ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Topical Delivery ◽  
Onset Of Action ◽  
Promising Alternative ◽  
Inflammatory Drugs ◽  
Systemic Onset

The aim of this study is to develop, characterize and compare conventional liposome, deformable liposome (transfersome) and microemulsion formulations as potential topical delivery systems for meloxicam. Liposomes were characterized in terms of vesicle size, zeta potential and entrapment efficiency. For microemulsions, particle size, electrical conductivity and viscosity studies were performed to assess the structure of the investigated systems. An ex vivo skin permeation study has been conducted to compare these formulations. The dermal and transdermal delivery of meloxicam using these formulations can be a promising alternative to conventional oral delivery of non-steroidal anti-inflammatory drugs (NSAIDs) with enhanced local and systemic onset of action and reduced side effects.

scholarly journals FORMULATION AND EVALUATION OF GEL CONTAINING ETHOSOMES ENTRAPPED WITH TRETINOIN

2018 ◽  
Vol 8 (5-s) ◽  
pp. 315-321
Author(s):  
Rakhi Mishra ◽  
Shradha Shende ◽  
Prabhat Kumar Jain ◽  
Vivek Jain
Keyword(s):  
Transdermal Delivery ◽  
Skin Permeation ◽  
Three Dimensional ◽  
Entrapment Efficiency ◽  
Brick Wall ◽  
Topical Formulation ◽  
Ir Studies ◽  
Skin Retention ◽  
Drug Solution

A skin disease, like acne, is very common and normally happens to everyone at least once in their lifetime. The structure of the stratum corneum is often compared with a brick wall, with corneocytes surrounded by the mortar of the intercellular lipid lamellae. One of the best options for successful drug delivery to the affected area of skin is the use of ethosomes which can be transported through the skin through channel-like structures. Tretinoin is a widely used retinoid for the topical treatment of acne, photo-aged skin, psoriasis and skin cancer which makes it a good candidate for topical formulation. Yet side effects, like redness, swelling, peeling, blistering and, erythema, in addition to its high lipophilicity make this challenging. Drug loaded ethosomes had been prepared using phospholipid and ethanol, were optimized and characterized for entrapment efficiency, vesicular size, shape, In-vitro skin permeation, skin retention, drug‐membrane component interaction and stability. The ethosomal formulation having 0.5 %w/v of phospholipid and 20 %v/v of ethanol (F2) showing the greatest entrapment efficiency (80.25±0.23) with small particle size (205.40±2.31nm) was selected for further skin permeation studies. The skin permeation and skin retention studies were performed on ethosomal formulation, liposomal formulation (0.5 %w/v of phospholipid without alcohol), hydroethanolic drug solution and phosphate buffer saline (pH7.4) drug solution. Among them, ethosomal formulation showed higher cumulative percentage of drug permeation (93.36±0.45%) and 8 hours than the other formulations. Scanning electron microscopy confirmed the three dimensional nature of ethosomes. Dynamic light scattering technique proved that the ethosomes has smaller vesicular size than the liposomes prepared without alcohol. FT‐IR studies revealed no interaction between the drug and membrane components. The ethosomal vesicles were incorporated in carbopol gel base and its anti‐acne was compared with the marketed gel. Our results suggest that the ethosomes are an efficient carrier for dermal and transdermal delivery of tretinoin. Keywords: Tretinoin, Ethosomes, Diffusion, Carbopol gels, Transdermal delivery.

scholarly journals Polymeric Inserts Containing Eudragit® L100 Nanoparticle for Improved Ocular Delivery of Azithromycin

Biomedicines ◽  
2020 ◽  
Vol 8 (11) ◽  
pp. 466
Author(s):  
Shiva Taghe ◽  
Shahla Mirzaeei ◽  
Raid G. Alany ◽  
Ali Nokhodchi
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Hydroxypropyl Methylcellulose ◽  
Entrapment Efficiency ◽  
Hydroxyethyl Cellulose ◽  
Burst Release ◽  
Ocular Delivery ◽  
Sustained Drug Release ◽  
Diffusion Technique ◽  
Drug Solution

Polymeric inserts containing azithromycin-loaded Eudragit® L100 nanoparticles were developed to sustain the drug release and enhance its ocular performance. The solvent diffusion technique was employed to prepare nanoparticles. The developed nanoparticles (NPs) were fully characterized and investigated. The solvent casting method was used to prepare azithromycin ocular inserts (azithromycin, AZM film) by adding hydroxypropyl methylcellulose (HPMC) or hydroxyethyl cellulose (HEC) solutions after the incorporation of AZM-loaded Eudragit® L100 nanoparticles into plasticized PVA (polyvinyl alcohol) solutions. The optimized nanoparticles had a particle size of 78.06 ± 2.3 nm, zeta potential around −2.45 ± 0.69 mV, polydispersity index around 0.179 ± 0.007, and entrapment efficiency 62.167 ± 0.07%. The prepared inserts exhibited an antibacterial effect on Staphylococcus aureus and Escherichia coli cultures. The inserts containing AZM-loaded nanoparticles showed a burst release during the initial hours, followed by a sustained drug release pattern. Higher cumulative corneal permeations from AZM films were observed for the optimized formulation compared to the drug solution in the ex-vivo trans-corneal study. In comparison to the AZM solution, the inserts significantly prolonged the release of AZM in rabbit eyes (121 h). The mucoadhesive inserts containing azithromycin-loaded Eudragit® L100 nanoparticles offer a promising approach for the ocular delivery of azithromycin (antibacterial and anti-inflammatory) to treat ocular infections that require a prolonged drug delivery.

scholarly journals Development of ethosomes with taguchi robust design-based studies for transdermal delivery of alfuzosin hydrochloride

2012 ◽  
Vol 1 (11) ◽  
pp. 370-375 ◽  
Author(s):  
D Prasanthi ◽  
P K Lakshmi
Keyword(s):  
Robust Design ◽  
Transdermal Delivery ◽  
Design Method ◽  
Entrapment Efficiency ◽  
Pharmaceutical Journal ◽  
Dependent Variables ◽  
Alfuzosin Hydrochloride ◽  
Robust Design Method ◽  
Taguchi Robust Design ◽  
Drug Solution

In the present investigation efficiency of ethosomes as novel lipid carriers for transdermal delivery of Alfuzosin Hydrochloride (AH) has been evaluated. Taguchi robust design method was used for optimization of ethosomal formulations. Phospholipid type, concentration of phospholipid and concentration of ethanol was selected as independent variables and their effect on the dependent variables (entrapment efficiency and flux) was studied. Ethosomal formulation (EA8) with soya phosphatidylcholine (3%) and ethanol 20% were optimized. Vesicles were spherical, unilamellar with smooth surface. The optimized formulation exhibited vesicle size (6.85 ± 1.35µm), zeta potential (-8.14 ± 0.62mv), entrapment efficiency (91.86 ± 3.25%), flux (27.42 ± 0.04µg/cm2/hr), lag time (0.26±0.20hr) and skin deposition (298.01 ± 15.4µg/g). Transdermal flux was enhanced by 6.92 times over drug solution. Vesicle skin interaction studies showed fatty change in the dermis. The formulations were stable at 4°C for 120 days. Results suggested ethosomes as efficient carriers for AH transdermal delivery.DOI: http://dx.doi.org/10.3329/icpj.v1i11.12063 International Current Pharmaceutical Journal 2012, 1(11): 370-375

scholarly journals DoE Directed Optimization, Development and Characterization of Resveratrol Loaded Nlc System for the Nose to Brain Delivery in the Management of Glioblastoma Multiforme

2021 ◽  
Author(s):  
Nitish Kumar ◽  
Ghanshyam Das Gupta ◽  
Daisy Arora
Keyword(s):  
Particle Size ◽  
Nasal Mucosa ◽  
Ex Vivo ◽  
Research Work ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Antioxidant Property ◽  
Brain Delivery ◽  
Antioxidant Assay

Abstract Nose to brain delivery of resveratrol can be a very useful method to overcome the limitations possessed by conventional delivery approaches namely, hepatic metabolism, low bioavailability and half-life of resveratrol, and presence of blood-brain barrier (BBB). The objective of this research work was to develop and optimize the resveratrol-loaded NLCs and coating these carriers with chitosan to increase the residence time of the formulation into the nasal cavity and enhanced permeation across the nasal mucosa. Three CQAs (Particle size, Entrapment efficiency, and PDI), and CMAs (Solid: total lipid concentration, surfactant concentration, and bioactive amount) were selected and the formulation was optimized using the Box-Behnken design (BBD) approach. The optimized batch was evaluated for physicochemical characteristics such as particle size (168.24 ± 8.24 nm), PDI (0.151 ± 0.003), and entrapment efficiency (77.42 ± 3.76 %). This optimized batch was coated with chitosan, which produced coated NLCs with a particle size of 317.7 ± 15.9 nm, and PDI was 0.089 ± 0.009. The morphological study using TEM confirmed the spherical shape, size, and surface coating of the NLCs. Furthermore, both the uncoated and coated particles were analyzed for in vitro resveratrol release, ex vivo diffusion study, and antioxidant assay. NLCs was founded to show sustained in vitro release characteristic, and enhanced bioactive diffusion across the nasal mucosa compared to the bioactive solution of resveratrol. The antioxidant assay revealed that the antioxidant property of resveratrol was intact in the formulation, and a slight increase in antioxidant activity of the formulation was also observed which may be due to the presence of sesame oil in the formulation. These results indicated that the chitosan-coated NLCs can be used to deliver therapeutic moieties more efficiently via the nose to brain drug delivery.

scholarly journals STUDY OF ENHANCED ANTI-INFLAMMATORY POTENTIAL OF NIGELLA SATIVA IN TOPICAL NANOFORMULATION

2018 ◽  
Vol 10 (7) ◽  
pp. 41 ◽  
Author(s):  
Faisal Obaid Alotaibi ◽  
Gulam Mustafa ◽  
Alka Ahuja
Keyword(s):  
Zeta Potential ◽  
Size Distribution ◽  
Therapeutic Potential ◽  
Ex Vivo ◽  
Nigella Sativa ◽  
In Vitro Release ◽  
Spherical Shape ◽  
Active Constituent ◽  
Anti Inflammatory

Objective: Formulate a nanocarrier for enhancing the anti-inflammatory activity of thymoquinone (Tq), a major active constituent of Nigella sativa.Methods: Nanoformulation of Tq was developed by low energy emulsification techniques. NanoTqs were pre-screened by different thermodynamic stability tests, followed by in vitro release, zeta potential, viscosity, the transmittance (%), globule size distribution and ex vivo studies. The morphology of the optimized NanoTq was determined by transmission electron microscopy (TEM) which revealed fairly spherical shape and good correlation with particle size distribution study. The formulation used for assessment of the anti-inflammatory potential and permeability enhancement contained mixture of essential oil of Nigella sativa: Capryol 90 (3:7, 10%, v/v), Tween 80 (21.75%, v/v), PEG 400 (7.25%, v/v) and double distilled water (61%, v/v).Results: The in vitro permeation of Tq from optimized formulations was found extremely significant (p<0.001) in comparison to apiTq. The steady state flux (Jss), the permeability coefficient (Kp) and enhancement ratio (Er) of NanoTq gel was determined and compared with apiTq. The comparative anti-inflammatory effects of the optimized formulations NanoTq, apiTq and DicloGel was assessed on the edema in the carrageenan-induced paw model in Wistar rats. Therapeutic potential of NanoTq was found statistically extremely significant (P<0.0001) compared to apiTq and insignificant comparable with standard DicloGel. Storage stability of NanoTq showed insignificant changes in the zeta potential, droplet size and was free from any physical instability.Conclusion: The optimized nano formulation with a lower dose of Tq showed better anti-inflammatory effects, indicating greater absorption capability through the stratum corneum.

scholarly journals A COMPARATIVE STUDY OF TERBINAFINE ETHOSOMAL FORMULATIONS: A NOVEL APPROACH

2013 ◽  
Vol 03 (04) ◽  
pp. 023-029
Author(s):  
Narayana Charyulu R. ◽  
Mehta Satveek ◽  
Harish N. M. ◽  
Amit B. Patil
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Research Work ◽  
Entrapment Efficiency ◽  
Topical Administration ◽  
Comparative Investigation ◽  
Drug Accumulation ◽  
Dose Frequency ◽  
The Impact

AbstractThe present research work aimed at the impact of reduced vesicular size on the characteristics of ethosomes by comparing with the regular vesicular size of ethosomes as topical drug delivery vehicle to achieve optimal localized drug concentration and reduced dose frequency of the Terbinafine hydrochloride (TH), an antifungal drug. Oral use of TH contraindicated resulting from sever side effect, thus topical administration is recommended. Commercially available TH creams, lotions and sprays, have limitation of relatively short residual period at target site. The entrapment of drug in vesicles improves localization, solubility and availability of drug at the site; resulting in reduction of the dose. Ethosomes containing drug were prepared by employing higher concentration of alcohol in the form of hydroalcoholic or hydroglycolic phospholipid. Sonicated and unsonicated ethosomes were investigated for shape, particle size, and entrapment efficiency. Electronic microscope investigation not only revealed, vital evidence for presence of phospholipid vesicles in TH ethosomal systems but also displayed greater uniformity in size and shape of sonicated ethosomes than unsonicated ethosomes. Furthermore, the Comparative investigation was carried out for ex vivo skin permeation, ex vivo drug release and entrapment efficiency studies. Drug release followed zero order release rate kinetics. Drug accumulation study showed more than 19.01 % of drug was deposited into skin by sonicated ethosomal formulation as compared to 2.57 % by unsonicated ethosomal formulation. Sonicated and unsonicated ethosomes were found stable at refrigeration and room temperature conditions during stability studies. Drug accumulation studies in deep skin strata was found to be comparatively greater in sonicated ethosomes, which indicates higher localized drug and that in turn reduces dose frequency.

Assessment of a Novel Vitamin D3 Formulation with Nanostructured Lipid Carriers for Transdermal Delivery

2021 ◽  
Vol 18 ◽  
Author(s):  
Laura Junqueira ◽  
Hudson Polonini ◽  
Cristiano Ramos ◽  
Anderson O. Ferreira ◽  
Nádia Raposo ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Vitamin D3 ◽  
Transdermal Delivery ◽  
Ex Vivo ◽  
Skin Permeation ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
Nanoparticle Dispersion ◽  
Vitamin D3 Supplementation

Objective: Develop and assess a transdermal emulsion loaded with nanostructured lipid carriers for vitamin D3 supplementation. Methods: Vitamin D3 loaded nanostructured lipid carriers, produced via high shear homogenization and ultrasonication, were assessed for their particle size, distribution, morphology, zeta potential, entrapment efficiency, and cytotoxicity. They were incorporated into a transdermal vehicle, and the stability and ex vivo permeation were evaluated. Results: Spherical nanoparticles were developed with a particle size of 192.5 nm, a polydispersity index of 0.13, a zeta potential of -29.0 mV, and an entrapment efficiency of 99.75%. They were stable (particle size and distribution) for 15 days when stored in a refrigerator and for 30 days at room temperature and 32 °C. The nanoparticles decreased the drug cytotoxicity against fibroblasts, as shown by IC50 (nanoparticle: 32.48 μg mL−1; vitamin D3: 16.73 μg mL−1). The emulsion loaded with nanoparticles minimized the degradation of vitamin D3 when compared with the nanoparticle dispersion. Additionally, the emulsion provided the skin permeation of vitamin D3 following the recommended daily allowance. Conclusion: To the best of our knowledge, this is the first study to use nanostructured lipid carriers for transdermal delivery of vitamin D. The developed formulation is a promising strategy to overcome the vitamin D3 variable oral bioavailability. It also represents a comfortable route of administrationd. Thus it could be beneficial for patients and clinicians. However, further studies are needed to allow the permeation of larger amounts of vitamin D3, and the combination of these nanoparticles with microneedles would be interesting.

scholarly journals Development of CelecoxibTransfersomal gel for the Treatment of Rheumatoid Arthritis

2014 ◽  
Vol 2 (02) ◽  
pp. 07-13 ◽  
Author(s):  
Preeti . ◽  
Murugesan Senthil Kumar
Keyword(s):  
Rheumatoid Arthritis ◽  
Transdermal Delivery ◽  
Ex Vivo ◽  
Skin Irritation ◽  
Entrapment Efficiency ◽  
Sodium Deoxycholate ◽  
Vesicle Shape ◽  
Gel Formulations

The aim of the present study was to investigate the potential of Transfersomal gel formulations for transdermal delivery of Celecoxib and to evaluate the effect of concentration of Soya PC and Sodium deoxycholate. Transfersomal vesicles containing Soya PC mixed with Sodium deoxycholate and Celecoxib were prepared by conventional rotatory evaporation (Film hydration method) and characterized for various parameters including vesicle shape, size and size distribution, surface morphology, entrapment efficiency, in-vitro and ex-vivo drug release and in-vivo anti-inflammatory activity. Vesicles were also evaluated for skin irritation study and permeation studies.Results of all the studies suggested that CelecoxibTransfersomal gel formulation was therapeutically effective drug delivery system for treatment of Rheumatoid Arthritis.

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