scholarly journals In Vitro Performance of Dutasteride-Nanostructured Lipid Carriers Coated with Lauric Acid-Chitosan Oligomer for Dermal Delivery

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 994
Author(s):  
Norhayati Mohamed Noor ◽  
Azila Abdul-Aziz ◽  
Khalid Sheikh ◽  
Satyanarayana Somavarapu ◽  
Kevin M. G. Taylor
Keyword(s):  
Lauric Acid ◽  
Skin Irritation ◽  
Systemic Exposure ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
Androgenic Alopecia ◽  
Fluorescent Marker ◽  
Chitosan Oligomer ◽  
Coumarin 6

Dutasteride, licensed as an oral medicine for the treatment of benign prostatic hypoplasia, has been investigated as a treatment for androgenic alopecia. In this study, the potential for dustasteride to be delivered topically in order to reduce systemic exposure, irritation of the skin, and also cytotoxicity was explored. Chitosan oligomer (CSO) was successfully synthesised with lauric acid as a coating for a dutasteride-loaded nanostructured lipid carriers (DST-NLCs) system. DST-NLCs were prepared using a combination of melt-dispersion and ultrasonication. These negatively charged NLCs (−18.0 mV) had a mean particle size of ~184 nm, which was not significantly increased (p > 0.05) when coated with lauric acid-chitosan oligomer (CSO-LA), whilst the surface charge changed to positive (+24.8 mV). The entrapment efficiency of DST-NLCs was 97%, and coated and uncoated preparations were physically stable for up to 180 days at 4–8 °C. The drug release was slower from DST-NLCs coated with CSO-LA than from uncoated NLCs, with no detectable drug permeation through full-thickness pig ear skin from either preparation. Considering the cytotoxicity, the IC50 values for the DST-NLCs, coated and uncoated with CSO-LA were greater than for dutasteride alone (p < 0.05). DST-NLCs and empty NLCs coated with CSO-LA at 25 µM increased the cell proliferation compared to the control, and no skin irritation was observed when the DST-NLC formulations were tested using EpiDerm™. The cell and skin uptake studies of coated and uncoated NLCs incorporating the fluorescent marker Coumarin-6 showed the time-dependent uptake of Coumarin-6. Overall, the findings suggest that DST-NLCs coated with CSO-LA represent a promising formulation strategy for dutasteride delivery for the treatment of androgenic alopecia, with a reduced cytotoxicity compared to that of the drug alone and lower irritancy than an ethanolic solution of dutasteride.

scholarly journals FORMULATION AND IN VITRO, IN VIVO EVALUATION OF PRONIOSOMAL GEL OF NEOMYCIN SULPHATE

2019 ◽  
pp. 156-163
Author(s):  
AMOL SHETE ◽  
PRIYANKA THORAT ◽  
RAJENDRA DOIJAD ◽  
SACHIN SAJANE
Keyword(s):  
Phase Separation ◽  
Skin Irritation ◽  
Entrapment Efficiency ◽  
Separation Method ◽  
Gelling Agent ◽  
In Vivo Evaluation ◽  
Skin Delivery ◽  
Span 60

Objective: The objectives of present investigation were to prepare and evaluate proniosomes of neomycin sulphate (NS) by coacervation phase separation method by using sorbitan monostearate (span 60) and lecithin as a surfactant to increase the penetration through the skin and study the effect of concentration of the same. Methods: Proniosomes of neomycin sulphate (NS) were prepared by coacervation phase separation method by using span 60 and lecithin. The effect of concentration of span 60 and lecithin was studied by factorial design. The prepared proniosomes were converted to gel by using carbopol as a gelling agent. The prepared formulations were evaluated for entrapment efficiency, in vitro drug diffusion, in vitro antibacterial activity and in vivo skin irritation test etc. Results: All Formulation showed the percentage entrapment efficiency in the range 38.31±0.05% to 77.96±0.06%, good homogeneity and gel was easily spreadable with minimal of shear. Optimized formulation showed enhanced rate of diffusion in vitro, increase in zone of inhibition against staphylococcus aureus, no skin irritation and showed good stability. Conclusion: The results of present study indicates that proniosomal gel formulated by using combination of span 60, Lecithin, cholesterol can be used to enhance skin delivery of NS because of excellent permeation of drug. Developed proniosomal gel formulation was promising carrier for NS

scholarly journals Enhanced Transdermal Delivery of Concentrated Capsaicin from Chili Extract-Loaded Lipid Nanoparticles with Reduced Skin Irritation

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 463 ◽  
Author(s):  
Phunsuk Anantaworasakul ◽  
Wantida Chaiyana ◽  
Bozena B. Michniak-Kohn ◽  
Wandee Rungseevijitprapa ◽  
Chadarat Ampasavate
Keyword(s):  
Skin Irritation ◽  
Chorioallantoic Membrane ◽  
Crystallinity Index ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Loading Capacity ◽  
High Concentration ◽  
Fatty Esters ◽  
Solid Lipid

The aim of this study was to develop lipid-based nanoparticles that entrapped a high concentration of capsaicin (0.25%) from a capsicum oleoresin extract. The solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were strategically fabricated to entrap capsaicin without a hazardous solvent. Optimized nanosize lipid particles with high capsaicin entrapment and loading capacity were achieved from pair-wise comparison of the solid lipid mixtures consisting of fatty esters and fatty alcohols, representing small and large crystal-structure molecules combined with a compatible liquid lipid and surfactants (crystallinity index = 3%). This report was focused on selectively captured capsaicin from oleoresin in amorphous chili extract-loaded NLCs with 85.27% ± 0.12% entrapment efficiency (EE) and 8.53% ± 0.01% loading capacity (LC). The particle size, polydispersity index, and zeta potential of chili extract-loaded NLCs were 148.50 ± 2.94 nm, 0.12 ± 0.03, and −29.58 ± 1.37 mV, respectively. The favorable zero-order kinetics that prolonged capsaicin release and the significantly faster transdermal penetration of the NLC attributed to the reduction in skin irritation of the concentrated capsaicin NLCs, as illustrated by the in vitro EpiDermTM three-dimensional human skin irritation test and hen’s egg test chorioallantoic membrane assay (HET-CAM).

Optimized Preparation of Capsaicin-Loaded Nanoparticles Gel by Box-Behnken Design

2014 ◽  
Vol 1061-1062 ◽  
pp. 359-368 ◽  
Author(s):  
Mei Ling Tang ◽  
Li Hua Chen ◽  
Dong Sheng Zhou ◽  
Wei Feng Zhu ◽  
Yong Mei Guan ◽  
...  
Keyword(s):  
Skin Permeation ◽  
Skin Irritation ◽  
Morphological Characteristics ◽  
Entrapment Efficiency ◽  
Box Behnken Design ◽  
Irritation Test ◽  
Predicted Values ◽  
Skin Irritation Test

A three-factor three-level Box-Behnken design(BBD) was employed to optimize capsaicin-loaded nanoparticles(Cap-NPs), and its properties in vitro and in vivo were evaluated. Particle size, morphological characteristics, entrapment efficiency of Cap-NPs were investigated respectively by Zetasizer, H7000 TEM and HPLC. Release, skin permeation and skin irritation test were investigated on mouse and rabbits. The predicted values of Cap-NPs were 94.50±6.33% for entrapment efficiency(EE) and 170.30±7.81 nm for particle mean diameter(PMD) under optimal conditions which were 346.33 bar (homogenization pressure, X1), 4.67 min(homogenization time, X2), and 15421.42 rpm (shear rate, X3). The in vitro permeation study showed that capsaicin permeability in NPs-gel was a 2.80-fold greater flux values than conventional ointment after 24 h. Cap-NPs-gel produce no observable skin irritation in rabbits within 72h. The optimized Cap-NPs-gel would be a good candidate for transdermal delivery.

scholarly journals Anastrozole Loaded Nanostructured Lipid Carriers : Preparation and Evaluation

2021 ◽  
Vol 30 (2) ◽  
pp. 185-195
Author(s):  
Alaa Abdul-Jabbar Hashim ◽  
Nawal A. Rajab
Keyword(s):  
Hot Flashes ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Nanostructured Lipid Carriers ◽  
Poloxamer 407 ◽  
Fourth Generation ◽  
Glycol Succinate ◽  
Release Mechanism ◽  
Optimum Formula

Anastrozole (ANZ) is considered constitute of the fourth –generation of Non–steroidal aromatase blockage, ANZ has use for hormone receptor positive breast cancer in postmenopausal women. The serious side effects of ANZ including, vaginal dryness, hot flashes, irritability, breast tenderness and un–stability in circulation. Nanostructured lipid carriers (NLCs) have recently emerged as a multifunctional platform for drug delivery in cancer therapy. Five formula were composed of (200 mg of glyceryl monostearate, 40 mg of oleic acid , 1% (w/w) Tween 80, 1% (w/w) Poloxamer 407, 1% (w/w) soy lecithin and Vitamin E Polyethylene Glycol Succinate. The mean particle size, polydispersity index, zeta potential, entrapment efficiency, loading capacity range of optimum formula F05 (166±3.86 nm), (0.271±0.04), (–23.7±2.65 mV), (42.43±3.90%) and (1.23±0.35%) respectively that prepared by same above composition but higher amplitude value (70%). The in–vitro drug leakage study demonstrated intact formula through 5 hours, with an approximately 78.37% of the drug was encapsulated, that exhibit an anomalous release mechanism.

scholarly journals Formulation and Evaluation of Clarithromycin Loaded Nanostructured Lipid Carriers for the Treatment of Acne

2021 ◽  
pp. 26-38
Author(s):  
Pooja Shettigar ◽  
Marina Koland ◽  
S. M. Sindhoor ◽  
Ananth Prabhu
Keyword(s):  
Electron Microscopy ◽  
Particle Size ◽  
Drug Release ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
In Vitro Drug Release ◽  
Ex Vivo Permeation ◽  
Acne Treatment

Background: Clarithromycin is a macrolide antibiotic used in acne treatment, but it has poor solubility, which decreases its permeability through lipid barriers such as skin. Nanostructured lipid carriers can enhance the permeability of clarithromycin through the skin, thus improving its potential for controlling acne. Aim: To formulate and evaluate Nanostructured lipid carriers of clarithromycin for topical delivery in acne treatment Methods: Nanostructured lipid carriers were prepared by emulsification and ultrasonication methods using lipids such as glycerol monostearate and oleic with poloxamer 188 as stabilizer. These nano-carriers were optimized with the help of the Quality by Design (QbD) approach employing Design-Expert® software. The nanoparticles were characterized for particle size analysis, zeta potential, drug-excipient compatibility, entrapment efficiency, and surface morphology by Scanning Electron Microscopy (SEM) and Transmission Electron Microscopy (TEM). The nano-carriers were also investigated for in vitro drug release and ex vivo permeation through excised goat skin. The optimized formulation was incorporated into topical carbopol gel base, formulated and examined for pH, viscosity, spreadability, in vitro drug release, ex vivo permeation, and stability under accelerated conditions. Results: The average particle size of the optimized nanoparticles was 164.8 nm, and zeta potential was -39.2 mV. FTIR studies showed that drug and lipids are compatible with each other. The morphology study by SEM and TEM showed spherical shaped particles. The entrapment efficiency of the optimized formulation was found to be 88.16%. In vitro drug release studies indicated sustained release from the formulation due to diffusion through the lipid matrix of the particles. The ex vivo permeation study using goat skin produced greater permeation from the NLC gel (89.5%) than marketed gel (65%) due to the lipid solubility of the nanoparticles in the skin. The formulation was stable under accelerated conditions. Conclusion: The optimized formulation can be considered as promising nano-carriers suitable for the sustained release of clarithromycin into the skin for effective control of acne.

scholarly journals Lipid Nanoparticles for Enhancing the Physicochemical Stability and Topical Skin Delivery of Orobol

Pharmaceutics ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 845
Author(s):  
Min-Hwan Kim ◽  
Yae-Eun Jeon ◽  
Soobeen Kang ◽  
Jae-Young Lee ◽  
Ki Won Lee ◽  
...  
Keyword(s):  
Skin Irritation ◽  
Entrapment Efficiency ◽  
Aging Effect ◽  
Lipid Nanoparticles ◽  
Skin Aging ◽  
Shea Butter ◽  
Skin Delivery ◽  
Cadaver Skin ◽  
The Stability

Orobol is one of the major soy isoflavones, and has been reported to have various pharmacological activities, including an anti-skin-aging effect. However, since it has low solubility in water and physicochemical instability, the formulation of orobol for delivery into the dermal layer of the skin could be challenging. The objective of this study was to prepare lipid nanoparticles formulations of orobol to enhance its stability as well as its deposition into the skin. Formulations of orobol-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were characterized in terms of their mean particle size, entrapment efficiency, and morphology. The nano-sized spherical NLCs formulations maintained the stability of orobol for up to 28 days. Moreover, the NLCs formulation significantly increased the in vitro deposition of orobol into both Strat-M membranes and human cadaver skin compared with the other formulations. Additionally, the NLCs formulation did not cause significant skin irritation in clinical study. These results demonstrate that a shea butter-based NLC formulation could be a promising and safe carrier system for improving the stability of orobol and enhancing its topical skin delivery.

Development and optimization of Luliconazole Nanostructured lipid carriers based gel by Quality by Design its skin distribution studies, dermatokinetic modeling & In-vitro and Ex-vivo correlation

2020 ◽  
Vol 18 ◽  
Author(s):  
Eranti Bhargav ◽  
Yiragamreddy Padmanabha Reddy ◽  
Koteshwara Kunnatur B
Keyword(s):  
Particle Size ◽  
Quality By Design ◽  
Fungal Infections ◽  
Ex Vivo ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
Fractional Factorial ◽  
Sonication Time ◽  
Drug Concentrations

Objective : The present study was aimed to improve the permeability of Luliconazole (LZ) and to localize high drug concentrations at skin layers by Quality by Design (QbD) based Nanostructured lipid carriers (NC) based gel. Methods: Quality Target Product Profile was set and Critical Quality attributes were identified. FT-IR and DSC studies confirmed compatibility. Risk assessment was carried out by screening the factors using 27-27-2 fractional factorial design and optimization by Box Behnken design. Cholesterol: Cetyl Palmitate, PEG 200 and probe sonication time were identified as factors, Particle size (<200 nm), PDI (0.4), % Entrapment efficiency (% EE, >80%) and % Cumulative Drug release (% CDR, >95%) as responses. Contour plots, Overlay plots and desirability were utilized to create design space. Results: The quadratic polynomial equations showed that increased lipid content, PEG 200 and optimum sonication time reduced Particle size, PDI, improved % EE and % CDR. The optimized formula was formulated into a gel. Ex-vivo permeation studies performed using pig ear pinna skin revealed that developed LZ NC gel exhibited greater permeation 272.98±8.57 (µg/cm2 ) and 32.11 ±4.7 (µg/cm2 /h) flux than plain drug dispersed gel. Dermatokinetic parameters of LZ NC gel revealed that highly significant amount of LZ was permeated, distributed and transported through the skin layers. The better linear correlations were obtained by LZ permeation through synthetic membrane (in-vitro) and pig ear pinna skin (ex-vivo). Conclusion: The above findings revealed that developed LZ NC gel exhibited better permeation and localization at skin layers in treating fungal infections.

Formulation and Evaluation of Nanosponges loaded Bifonazole for Fun-gal Infection

2020 ◽  
Vol 18 ◽  
Author(s):  
Amaravathi Murali Krishna ◽  
Venkatesh Dinnekere Putte Gowda ◽  
Roopa Karki
Keyword(s):  
Drug Release ◽  
Fungal Infections ◽  
Skin Irritation ◽  
In Vitro Release ◽  
Three Dimensional ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Model Stability ◽  
Novel Approach

Background: Nanosponges is a novel approach of topical drug delivery, especially for the fungal infections. Nanosponges are a unique class of nanoparticles with three-dimensional nanostructure in nanometers wide cavities, which can encapsulate both hydrophilic and lipophilic substances, will provide increased efficacy and safety. Objective: To formulate and evaluate Bifonazole loaded nanosponges in hydrogels for the treatment of fungal diseases. Methods: Bifonazole-loaded nanosponges to be formulated using emulsion solvent diffusion technique. Interaction of drugethyl cellulose polymer along with other excipients’ was done by using FTIR as well as DSC. The nanosponges formulations were evaluated with different parameters. Results: Bifonazole loaded nanosponges’ particle size and zeta potential for formulations were between the range of 183.7 to 560.2 nm and –17.77 to –21.9 mV, respectively. Surface morphology of nanosponges by SEM disclosed that it was spherical and porous in nature. Drug entrapment efficiency was found to be 45.44 to 79.71%. The drug release study was done by using phosphate buffer pH 6.8. Further in vitro release data is fitted in to kinetic models. The optimized formulation M6 has incorporated hydrogels, further evaluated skin irritation, in vitro drug release, viscosity and pH using a rat model. Stability studies of hydrogel formulation MH2 revealed that no changes in in-vitro drug release, pH and drug content study at the completion of 6 months. Conclusion: Thus, it indicated that the prepared Bifonazole loaded nanosponges into hydrogel was stable. Hence, it could be a suitable dosage form for the cure of fungal infections in the skin.

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF PIPER RETROFRACTUM EXTRACT LOADED MUCOADHESIVE NANOSTRUCTURED LIPID CARRIERS FOR TOPICAL ORAL DRUG DELIVERY

2017 ◽  
Vol 9 (9) ◽  
pp. 79
Author(s):  
Kavee Srichaivatana ◽  
Anan Ounaroon ◽  
Waree Tiyaboonchai
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
Oral Cavity ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
Oral Drug ◽  
Drug Entrapment Efficiency ◽  
Piper Retrofractum

Objective: To develop and characterize Piper retrofractum extract loaded nanostructured lipid carriers (PRE loaded NLCs) for topical oral cavity administration to enhance bioavailability and stability of piperine.Methods: PRE loaded NLCs were prepared with a hot high-pressure homogenization technique followed by coating the particle surface with mucoadhesive polymers; polyethene glycol 400 (PEG) and polyvinyl alcohol (PVA). The physicochemical properties in terms of particle size, polydispersity index, zeta potential, drug entrapment efficiency, in vitro drug release profile and antimicrobial activities were examined. In vitro, mucoadhesion studies were assessed by the wash-off test. The physicochemical stabilities of mouth spray containing PRE loaded NLCs were investigated by kept at room temperature and 4 °C for 6 mo.Results: The PRE loaded NLCs showed spherical shape with a mean particle size of ~100-120 nm and zeta potential of ~-24 mV. Up to 90% drug entrapment efficiency was achieved. PEG-NLCs and PVA-NLCs showed a strong interaction with porcine buccal mucosa than uncoated-NLCs. All PRE loaded NLCs formulations revealed fast release characteristics and effective against Streptococcus mutans and S. sanguinis. The mouth spray containing PRE loaded NLCs showed good physical stability without particle aggregation. In addition, the chemical stability of piperine in NLCs was significantly improved during storage at both storage conditions compared to its solution form.Conclusion: The developed PRE loaded polymer coated-NLCs showed high potential to use as a local drug delivery system for reducing the bacterial growth in the oral cavity.

Design of Caffeine-Loaded Nanostructured Lipid Carriers Containing Coconut Oil for Topical Application

2019 ◽  
Vol 819 ◽  
pp. 187-192 ◽  
Author(s):  
Somkamol Manchun ◽  
Sitthiphong Soradech ◽  
Krongkan Kingkaew ◽  
Parapat Sobharaksha ◽  
Pornsak Sriamornsak ◽  
...  
Keyword(s):  
Topical Application ◽  
Skin Permeation ◽  
Coconut Oil ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carriers ◽  
Pharmacological Agents ◽  
Solid Lipid ◽  
Glyceryl Behenate ◽  
Selection Of

Although caffeine was suggested as one of the pharmacological agents for the cellulite treatment, its skin permeation restricted. The present work was aimed at formulating caffeine loaded nanostructured lipid carriers (CAF-NLCs) containing coconut oil as a topical delivery system. CAF-NLCs were prepared by the ultrasonic emulsification method, using coconut oil as a liquid lipid. The proper selection of solid lipid and surfactants for these formulations were investigated. Subsequently, physicochemical properties, entrapment efficacy, stability, and in vitro drug release were evaluated. The CAF-NLCs containing coconut oil was successfully prepared using glyceryl behenate as a solid lipid and showed an interesting entrapment efficiency (62-99%). The obtained CAF-NLCs presented the nanosized range (≈ 60-390 nm), with a low polydispersity index and high negative zeta potential values (over ‐30 mV). However, the type and concentration of surfactant also affected these properties. These results suggested that CAF-NLCs containing coconut oil are the promising carrier for delivery of caffeine following topical application.

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