Cetyl palmitate-based NLC for topical delivery of Coenzyme Q10 – Development, physicochemical characterization and in vitro release studies

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.

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Preparation and in vitro Evaluation of Bioadhesive Microparticulate System

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2008.1.3.9 ◽

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.

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

Future Journal of Pharmaceutical Sciences ◽

10.1186/s43094-020-00130-1 ◽

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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Inclusion of hydroxytyrosol in ethyl cellulose microparticles: In vitro release studies under digestion conditions

Food Hydrocolloids ◽

10.1016/j.foodhyd.2018.06.009 ◽

2018 ◽

Vol 84 ◽

pp. 104-116 ◽

Cited By ~ 13

Author(s):

Filipa Paulo ◽

Lúcia Santos

Keyword(s):

Ethyl Cellulose ◽

In Vitro Release ◽

Release Studies ◽

Vitro Release

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Sodium alginate nanoparticles as a new transdermal vehicle of glucosamine sulfate for treatment of osteoarthritis

European Journal of Nanomedicine ◽

10.1515/ejnm-2017-0008 ◽

2017 ◽

Vol 9 (3-4) ◽

Cited By ~ 2

Author(s):

Asmaa S. El-Houssiny ◽

Azza A. Ward ◽

Dina M. Mostafa ◽

Salwa L. Abd-El-Messieh ◽

Kamal N. Abdel-Nour ◽

...

Keyword(s):

Side Effects ◽

Surface Charge ◽

Ex Vivo ◽

In Vitro Release ◽

Glucosamine Sulfate ◽

Suspension Stability ◽

Rat Skin ◽

Release Studies ◽

Vitro Release

AbstractGlucosamine sulfate (GS) has been used orally for the treatment of osteoarthritis (OA). However, it may be susceptible to the liver first pass phenomenon, which greatly affects its bioavailability, in addition to its side effects on the gastrointestinal tract. Alginate nanoparticles (Alg NPs) were investigated as a new drug carrier for transdermal delivery of GS to improve its effectiveness and reduce side effects. GS-Alg NPs were characterized by encapsulation efficiency, NP yield, particle size and surface charge properties. The in vitro release studies of GS and the ex vivo permeability through rat skin were determined using a UV-Vis spectrophotometer. GS-Alg NPs are within the nanometer range of size. High negative surface charge values are obtained and indicate the high suspension stability of the prepared formulation. The in vitro release studies showed that GS is released from Alg NPs in a sustained and prolonged manner. The ex vivo permeability of GS through rat skin is enhanced significantly after encapsulation in the negatively charged Alg NPs. We successfully reported a highly stable nanoparticlulate system using Alg NPs that permits the encapsulation of GS for topical administration, overcoming the disadvantages of oral administration.

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In Vitro Release Studies on Matrix Type Transdermal Drug Delivery Systems of Naltrexone and Its Acetyl Prodrug

Drug Development and Industrial Pharmacy ◽

10.1080/03639040500271944 ◽

2005 ◽

Vol 31 (9) ◽

pp. 871-877 ◽

Cited By ~ 15

Author(s):

Buchi N. Nalluri ◽

Caitlin Milligan ◽

Jianhong Chen ◽

Peter A. Crooks ◽

Audra L. Stinchcomb

Keyword(s):

Drug Delivery ◽

Transdermal Drug Delivery ◽

Drug Delivery Systems ◽

In Vitro Release ◽

Delivery Systems ◽

Matrix Type ◽

Release Studies ◽

Transdermal Drug Delivery Systems ◽

Vitro Release

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Synthesis, characterization and in vitro release studies of a new acetazolamide–HP-β-CD–TEA inclusion complex

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2007.03.037 ◽

2008 ◽

Vol 43 (3) ◽

pp. 464-470 ◽

Cited By ~ 40

Author(s):

Gladys E. Granero ◽

Marcos M. Maitre ◽

Claudia Garnero ◽

Marcela R. Longhi

Keyword(s):

Inclusion Complex ◽

In Vitro Release ◽

Release Studies ◽

Vitro Release

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Chitosan (Poly-(D) glucosamine) based solid lipid nanoparticles of dexibuprofen for topical delivery: Formulation development and characterizations

Main Group Chemistry ◽

10.3233/mgc-210055 ◽

2021 ◽

pp. 1-12

Author(s):

Irshadullah ◽

Shefaat Ullah Shah ◽

Muhammad Khalid Khan ◽

Kifayat Ullah Shah ◽

Barkat Ali Khan

Keyword(s):

Surface Morphology ◽

Solid Lipid Nanoparticles ◽

Active Drug ◽

In Vitro Release ◽

Topical Delivery ◽

Lipid Nanoparticles ◽

Solid Lipid ◽

Permeation Study ◽

Vitro Release

Chitosan a poly-(D) glucosamine is a polysaccharide made by treating shrimp and other crustacean shells with the alkali sodium hydroxide. It is a hydrophilic polymer that helps to retain the drug inside the solid lipid nanoparticles (SLN’s) and prolongs the release of drug from the carrier system. The purpose of the study was to formulate Chitosan decorated SLN’s for the topical delivery of dexibuprofen by hot pressure homogenization technique. Blank SLN’s, drug loaded SLN’s and Chitosan decorated SLN’s were prepared. Particle size, zeta potential and PDI were determined. FTIR study was conducted to evaluate the compatibility of excipients with the active drug. Surface morphology of SLN’s was determined by field emission scanning electron microscope. Drug content and entrapment efficiency of SLN’s were determined using indirect method. In vitro release and ex vivo permeation study of SLN’s were carried out using Franz diffusion cell. The droplet size fell into the nano range i.e. 132±7 to 424±2 nm which is effective for topical drug delivery system. The PDI of formulations range from 0.21 to 0.42 which depicts the homogeneity of all the SLN’s formulations. Vibrational analysis indicates that there is no interaction between active drug and excipient used in the formulation. The surface morphology revealed the spherical shape of Chitosan decorated SLN’s. The in vitro release of formulations showed 79.91±1.07 to 89.94±1.8 % drug release. The drug permeation study showed high permeation of drug into the skin. The percent drug permeation ranges from 64.15±0.93 to 71.80±0.88% indicating good permeation of drug across the skin. Overall, SLN’s are an effective carrier for topical delivery of dexibuprofen and thus bypasses side effects associated with oral delivery.

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In vitro Release Kinetics Study of Ranolazine from Swellable Hydrophilic Matrix Tablets

Dhaka University Journal of Pharmaceutical Sciences ◽

10.3329/dujps.v8i1.5333 ◽

1970 ◽

Vol 8 (1) ◽

pp. 31-38 ◽

Cited By ~ 1

Author(s):

Mohammad Nezab Uddin ◽

Ishtiaq Ahmed ◽

Monzurul Amin Roni ◽

Muhammad Rashedul Islam ◽

Mohammad Habibur Rahman ◽

...

Keyword(s):

Drug Release ◽

Sustained Release ◽

Release Kinetics ◽

In Vitro Release ◽

High Viscosity ◽

Matrix Tablets ◽

Release Studies ◽

The Matrix ◽

Vitro Release

The objective of this study was to design oral sustained release matrix tablets of Ranolazine usinghydroxypropyl methylcellulose (HPMC) as the retardant polymer and to study the effect of formulation factors suchas polymer proportion and polymer viscosity on the release of drug. In vitro release studies were performed usingUSP type II apparatus (paddle method) in 900 mL of 0.1N HCl at 100 rpm for 12 hours. The release kinetics wasanalyzed using the zero-order, first order, Higuchi and Korsmeyer-Peppas equations to explore and explain themechanism of drug release from the matrix tablets. In vitro release studies revealed that the release rate decreasedwith increase in polymer proportion and viscosity grade. Mathematical analysis of the release kinetics indicated thatthe nature of drug release from the matrix tablets was dependent on drug diffusion and polymer relaxation andtherefore followed non-Fickian or anomalous release. The developed controlled release matrix tablets of Ranolazineprepared with high viscosity HPMC extended release up to 12 hours.Key words: Ranolazine; Sustained release; Methocel E50 Premium LV; Methocel K100LV CR; Methocel K4M CR;Methocel K15M CR.DOI: 10.3329/dujps.v8i1.5333Dhaka Univ. J. Pharm. Sci. 8(1): 31-38, 2009 (June)

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