Evaluation of Skin Permeability of Resveratrol Loaded Liposomes and Nanostructured Lipid Carriers using a Skin Mimic Artificial Membrane (skin-PAMPA)

2019 ◽  
Vol 9 (2) ◽  
pp. 134-145 ◽  
Author(s):  
Marta Casamonti ◽  
Vieri Piazzini ◽  
Anna Rita Bilia ◽  
Maria Camilla Bergonzi
Keyword(s):  
Antioxidant Capacity ◽  
In Vitro Release ◽  
Topical Delivery ◽  
Delivery Systems ◽  
Nanostructured Lipid Carriers ◽  
Skin Permeability ◽  
Dpph Test ◽  
Release Studies ◽  
Vitro Release

Background: The skin-PAMPA test is a quick and relatively deep tool in the early stages of drug discovery and formulation of dermal and transdermal delivery systems. Objective: This study focused on the application of the skin-PAMPA test to evaluate the permeation of Resveratrol (RSV) and also of two formulations, Liposomes (LP) and Nanostructured Lipid Carriers (NLC), prepared to improve RSV topical delivery. Methods: LP and NLC were physically and chemically characterized. Stability and in vitro release studies were also assessed in different pH media. The release results were applied to define the kinetic and mechanism of RSV release from the LP and NLC formulations. In vitro permeability was estimated through the skin-PAMPA and the antioxidant capacity was evaluated by DPPH test. Results: Nanoparticles have a spherical shape, dimensions suitable for skin application, and narrow size distribution. Encapsulation efficiency was 96.5% ± 2.1 for LP and 86.0% ± 2.4 for NLC. The formulations increased RSV solubility. Nanoparticles showed excellent physical and chemical stability during storage at 4°C for two months. In vitro release studies were performed at pH 5.5 and 7.4. The nanoparticles achieved a prolonged release of RSV. Skin-PAMPA proved an increased cutaneous permeability of RSV when loaded into LP or NLC. Both formulations maintained the antioxidant capacity of RSV, as evidenced by DPPH test. Conclusion: LP and NLC could be applied as drug delivery systems suitable for the topical delivery of the RSV. Skin-PAMPA has proved to be an effective tool for studying the permeability not only of the RSV but also of its formulations.

scholarly journals Influence of Oleic Acid on the Rheology and in Vitro Release of Lumiracoxib from Poloxamer Gels

2010 ◽  
Vol 13 (2) ◽  
pp. 286 ◽  
Author(s):  
Tailane Sant´Anna Moreira ◽  
Valéria Pereira De Sousa ◽  
Maria Bernadete Riemma Pierre
Keyword(s):  
Oleic Acid ◽  
Rheological Behavior ◽  
Transdermal Delivery ◽  
In Vitro Release ◽  
Delivery Systems ◽  
Penetration Enhancer ◽  
Release Studies ◽  
Vitro Release ◽  
Gel Transition

Abstract PURPOSE: Transdermal delivery of anti-inflammatory lumiracoxib (LM) could be an interesting strategy to avoid the side effects associated with systemic delivery, but it is ineffective due to the drug poor skin penetration. We have investigated the effects of oleic acid (OA), a lipid penetration enhancer, on the in vitro release of LM from poloxamer-based delivery systems (PBDS). The rheological behavior (shear rate dependent viscosity) and gelation temperature through measurements of optimal sol-gel transition temperatures (Tsol-gel) were also carried out in these systems. METHODS: In vitro release studies of LM from PBDS were performed using cellulose acetate as artificial membrane mounted in a diffusion system. The amount of LM released was divided by exposition area (µg/cm2) and these values were plotted as function of the time (h). The flux of the drug across the membrane (J) was calculated from the slope of the linear portion of the plot and expressed as µg/cm2. h -1. The determination of viscosity was carried out at different shear rates (γ) between 0.1- 1000 S-1 using a parallel plate rheometer. Oscillatory measurements using a cone-plate geometry rheometer surrounded by a double jacket with temperature varying 4-40°C, was used in order to determine Tsol-gel. RESULTS: Increase of both polymer and OA concentrations increases the viscosity of the gels and consequently reduces the in vitro LM release from the PBDS, mainly for gels containing OA at 10.0% compared to other concentrations of the penetration enhancer. Tsol-gel transition temperature was decreased by increasing viscosity; in some cases the formulation was already a gel at room temperature. Rheological studies showed a pseudoplastic behavior, which facilitates the flow and improves the spreading characteristics of the formulations. CONCLUSIONS: Taken together, the results showed that poloxamer gels are good potential delivery systems for LM, leading to a sustained release, and also have appropriate rheological characteristics. Novelty of the work: A transdermal delivery of non-steroidal antinflammatory drugs like lumiracoxib (LM) can be an interesting alternative to the oral route of this drug, since it was recently withdraw of the market due to the liver damage when systemically administered in tablets as dosage form. There are no transdermal formulations of LM and it could be an alternative to treat inflammation caused by arthritis or arthrosis. Then, an adequate delivery system to LM is necessary in order to release the drug properly from the PBDS as well as have good characteristics related to semi-solid preparations for transdermal application, which were evaluated through in vitro release studies and rheological behavior in this paper, respectively.

scholarly journals Preparation, In Vitro characterization and stability studies of ropinirole lipid nanoparticles enriched hydrogel for treatment of neurodegeneration diseases

2021 ◽  
Vol 11 (2-S) ◽  
pp. 66-75
Author(s):  
Kumara Swamy Samanthula ◽  
Ramesh Alli ◽  
Thirupathi Gorre
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Nanostructured Lipid Carriers ◽  
Solid Lipid ◽  
Release Studies ◽  
Vitro Release

Ropinirole (RP), is a selective dopamine agonist that is used alone or with other medications to treat the symptoms of Parkinson’s disease (PD). RP has low bioavailability of only about 50% due to the first-pass metabolism, and it requires frequent dosing during oral administration. The objective of the current research was to develop RP loaded solid lipid nanoparticles (RP-SLNs), nanostructured lipid carriers (RP-NLCs), and their corresponding hydrogels (RP-SLN-C and RP-NLC-C) that might improve efficacy in PD treatment. RP nanoparticles were prepared by homogenization aided probe sonication method and optimized based on particle size, polydispersity index (PDI), zeta potential (ZP), assay, entrapment efficiency, and in vitro release studies. Optimized formulations were converted to hydrogel formulations using Carbopol 934 as a gelling polymer and optimized based on rheological and release characteristics. Optimized formulations were further evaluated using differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD), scanning electron microscopy (SEM), freeze-drying, and stability study at refrigerated and room temperatures. The optimized RP-SLN formulation showed particle size and entrapment efficiency of 213.5±3.8 nm and 77.9±3.1% compared to 190.6±3.7 nm and 85.7±1.7% for optimized RP-NLC formulation. PXRD supplemented and confirmed DSC results, RP was entrapped in a molecularly dispersed state inside the core of the lipid nanocarrier. Furthermore, RP loaded lipid nanocarriers revealed a spherical shape in SEM images. In vitro release studies demonstrated sustained release profiles for RP from SLNs, NLCs, and their hydrogels over 24 h and were stable over three months at 4ºC and 25ºC storage conditions. Keywords: Parkinson’s disease, Ropinirole, Solid lipid nanoparticles, Nanostructured lipid carriers, Hydrogel.

Preparation and Comparatively Evaluation of Phenylethyl Resorcinol-Loaded Nanocarriers: Nanoemulsions and Nanostructured Lipid Carriers

2015 ◽  
Vol 1118 ◽  
pp. 28-36 ◽  
Author(s):  
Chao Long Ma ◽  
Cai Biao Hu ◽  
Shi Lei Ni ◽  
Ai Rui Qian ◽  
Qiang Xia
Keyword(s):  
Encapsulation Efficiency ◽  
In Vitro Release ◽  
Correlation Spectroscopy ◽  
Nanostructured Lipid Carriers ◽  
Particle Sizes ◽  
Typical Application ◽  
Release Studies ◽  
Penetration Ability ◽  
Vitro Release

The aim of the present study was to prepare nanostructured lipid carriers (NLCs) and nanoemulsions (NEs) with different lipid compositions for delivery of phenylethyl resorcinol (PR) and investigate the effect of the lipid composition on the performance of lipid-based nanocarriers. The optimized nanocarriers were evaluated by photon correlation spectroscopy (PCS), Laser diffraction (LD), encapsulation efficiency, in vitro release and in vitro penetration studies. The particle sizes of all the freshly prepared nanocarriers were in the range of 70-200 nm. PR-NLCs showed higher encapsulation efficiency than PR-NEs. A controlled-release behavior of PR-NLCs was observed in in vitro release studies. In vitro penetration studies demonstrated nanocarriers with smaller particles possessed higher penetration ability. According to the present study, nanocarriers with small particle sizes can be considered as a potential drug delivery system for typical application.

scholarly journals FORMULATION AND EVALUATION OF TRANSDERMAL PATCHES OF PANTOPRAZOLE SODIUM

2021 ◽  
pp. 287-291
Author(s):  
M. R. SHIVALINGAM ◽  
ARUL BALASUBRAMANIAN ◽  
KOTHAI RAMALINGAM
Keyword(s):  
In Vitro Release ◽  
Skin Permeability ◽  
Release Mechanism ◽  
Content Uniformity ◽  
Prolonged Release ◽  
Peptic Ulcers ◽  
Transdermal Patches ◽  
Release Studies ◽  
Vitro Release

Objective: The present study was an attempt to develop an alternative dosage form for the existing conventional oral, parenteral proton pump inhibitor (PPI) as transdermal patches for treating peptic ulcers. Methods: Transdermal patches of PPI were prepared using HPMC E5 with PVP K 30 and HPMC E5 with Eudragit L100 polymers in different ratios by a solvent evaporation method. All the formulated patches were subjected to various evaluation parameters such as thickness, folding endurance, weight uniformity, content uniformity, swelling index, percentage moisture content, moisture uptake, surface pH and in vitro release studies. Results: All patches exhibited satisfactory characteristics regarding integrity, flexibility, dispersion of drug, and other quality control parameters. In the in vitro release studies of transdermal patches, formulation F1 showed the prolonged release of drug (98.99 %) for 24 h, which indicates the maximum availability of the drug, and the in vitro skin permeability studies also showed that 96.26 % of drug Pantoprazole sodium permeated through the rat abdominal skin in 24 h. The kinetic studies were carried out and it was found that all the formulations follow zero-order and the release mechanism of drugs was found to be diffusion rate-limited, Non-Fickian mechanism which was confirmed by Korsmeyer–Peppas model. Conclusion: This suggests the transdermal application of Pantoprazole sodium holds the promised controlled release of the drug for an extended period of time.

scholarly journals Thermosensitive Nanocomposite Hydrogels for Intravitreal Delivery of Cefuroxime

Nanomaterials ◽  
2019 ◽  
Vol 9 (10) ◽  
pp. 1461 ◽  
Author(s):  
Simona Sapino ◽  
Elena Peira ◽  
Daniela Chirio ◽  
Giulia Chindamo ◽  
Stefano Guglielmo ◽  
...  
Keyword(s):  
Cataract Surgery ◽  
Retinal Pigment ◽  
In Vitro Release ◽  
Delivery Systems ◽  
Experimental Investigations ◽  
Inflammatory Disorder ◽  
Nanocomposite Hydrogels ◽  
Release Studies ◽  
Vitro Release

Endophthalmitis is a rare, but serious, intravitreal inflammatory disorder that can arise after cataract surgery. The intracameral injection of 1 mg cefuroxime (CEF) followed by three-times daily antibiotic topical administration for a week is generally recognized as the routine method of prophylaxis after cataract surgery. This procedure is controversial because of both the low efficacy and the low adherence to therapy by elderly patients. A unique slow release antibiotic intravitreal injection could solve these problems. The objective of the present study was to design ophthalmic nanocomposite delivery systems based on in situ gelling formulations that undergo sol-to-gel transition upon change in temperature to prolong the effect of CEF. Oil in water (O/W) microemulsion (µE) and solid lipid nanoparticles (SLN), obtained with an innovative formulation technology called cold microemulsion dilution, were evaluated as ocular drug delivery systems for CEF. Drug entrapment efficiency up to 80% was possible by esterifying CEF with 1-dodecanol to obtain dodecyl-CEF (dCEF). Both dCEF-loaded SLN and µE were then added with Pluronic®F127 (20% w/v) to obtain a nanocomposite hydrogel-based long acting system. The prepared thermosensitive formulations were evaluated for their physical appearance, drug content, gelation temperature, injectability and rheological properties, in vitro release studies and stability studies. Moreover, cell proliferation assays on human retinal pigment epithelial ARPE-19 cells were performed to evaluate the influence of this innovative system on the cellular viability. In addition, minimal inhibitory concentration (MIC) was assessed for both CEF and dCEF, revealing the need of dCEF hydrolysis for the antimicrobial activity. Although further experimental investigations are required, the physico-chemical characterization of the nanocomposite hydrogels and the preliminary in vitro release studies highlighted the potential of these systems for the sustained release of CEF.

Preparation and in vitro Evaluation of Bioadhesive Microparticulate System

1970 ◽  
Vol 1 (3) ◽  
pp. 257-266
Author(s):  
Nagda C. D. ◽  
Chotai N. P. ◽  
Patel S. B. ◽  
Soni T. J ◽  
Patel U. L
Keyword(s):  
Drug Loading ◽  
In Vitro Release ◽  
Phenyl Acetic Acid ◽  
Solvent Evaporation Method ◽  
Elimination Half ◽  
Release Studies ◽  
Differential Scanning Colorimetry ◽  
Polymer Interactions ◽  
Vitro Release

Aceclofenac (ACE) is NSAIDs of a phenyl acetic acid class. It is indicated in arthritis and osteoarthritis, rheumatoid arthritis, ankylosing spondylitis. It has short elimination half life of 4 hours. The objective of the study is to design, characterize and evaluate bioadhesive microspheres of ACE employing carbopol (CP) as bioadhesive polymer. Bioadhesive microspheres of ACE were prepared by solvent evaporation method. The prepared microspheres were free flowing and spherical in shape and characterized for drug loading, mucoadhesion test, infrared spectroscopy (IR), differential scanning colorimetry (DSC) and scanning electron microscopy (SEM). The in-vitro release studies were performed using pH 6.8 phosphate buffer. The drug loaded microspheres in a ratio of 1:5 showed 47% of drug entrapment; percentage mucoadhesion was 81% and 89% release in 10 h. The infrared spectra and DSC showed stable character of aceclofenac in the drug loaded microspheres and revealed the absence of drug-polymer interactions. SEM studies showed that the microspheres are spherical and porous in nature. The in vitro release profiles from microspheres of different polymer-drug ratios followed Higuchi model.

scholarly journals Development of nitazoxanide-loaded colon-targeted formulation for intestinal parasitic infections: centre composite design-based optimization and characterization

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Charu Bharti ◽  
Upendra Nagaich ◽  
Jaya Pandey ◽  
Suman Jain ◽  
Neha Jain
Keyword(s):  
Particle Size ◽  
Desirability Function ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
Percentage Yield ◽  
Vitro Release ◽  
Selection Of

Abstract Background The current investigation is focused on the development and characterization of Eudragit S100 coated nitazoxanide-loaded microbeads as colon-targeted system utilizing central composite design (CCD) and desirability function. The study initiated with the selection of a BCS class II drug nitazoxanide and its preformulation screening with excipients, selection of polymer and identification of concentration for CCD, selection of optimized formulation based on desirability function, and in vitro release studies in simulated gastric and colonic media and stability studies. A two-factor, three-level CCD was employed with two independent variables, i.e. X1 (chitosan % w/v) and X2 (sodium tripolyphosphate % w/v), and three dependent variables, i.e. Y1 (particle size in micrometres), Y2 (percentage yield) and Y3 (percent entrapment efficiency), were chosen. Additionally, surface morphology, mucoadhesion and in vitro drug release studies were also conducted. Result Chitosan concentration showing maximum entrapment and optimum particle size was selected to formulate chitosan beads. The polynomial equation and model graphs obtained from the Design-Expert were utilized to examine the effect of independent variables on responses. The effect of formulation composition was found to be significant (p ˂ 0.05). Based on the desirability function, the optimized formulation was found to have 910.14 μm ± 1.03 particle size, 91.84% ± 0.64 percentage yield and 84.75% ± 0.38 entrapment efficiency with a desirability of 0.961. Furthermore, the formulations were characterized for in vitro drug release in simulated colonic media (2% rat caecal content) and have shown a sustained release of ∼ 92% up to 24 h as compared to in vitro release in simulated gastric fluid. Conclusion The possibility of formulation in enhancing percentage yield and entrapment efficiency of nitazoxanide and the utilization of CCD helps to effectively integrate nitazoxanide microbeads into a potential pharmaceutical dosage form for sustained release.

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