Cationic Nanoliposomes Efficiently Delivering Phenylethyl Resorcinol Produce Enhanced Skin Lightening Effect

Nano LIFE ◽  
2020 ◽  
Vol 10 (04) ◽  
pp. 2040009
Author(s):  
Tianbao Wei ◽  
Dan Chen ◽  
Hexiang Mei ◽  
Zheng Zhou ◽  
Jianyong Sheng ◽  
...  
Keyword(s):  
Drug Loading ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
B16f10 Cells ◽  
Noticeable Reduction ◽  
The Mean ◽  
Skin Lightening ◽  
Vitro Release ◽  
Transdermal Permeability

Phenylethyl resorcinol-loaded cationic nanoliposomes (PR-CLPs) were prepared and characterized. Moreover, their transdermal properties, cellular uptake, and inhibition of tyrosinase activity and melanin production in B16F10 cells were studied. The mean particle size, polydispersity index (PDI) and zeta potential of the PR-CLPs were [Formula: see text][Formula: see text]nm, [Formula: see text][Formula: see text]mV [Formula: see text][Formula: see text]mV, respectively. The drug loading efficiency (DLE) and entrapment efficiency (EE) of PR in the PR-CLPs were [Formula: see text]% and [Formula: see text]%, respectively. Sustained release of PR from the PR-CLPs was observed in vitro release experiments. The results of the in vitro transdermal experiments showed that PR-CLPs significantly improved both the retention of PR in the skin and its transdermal permeability ([Formula: see text]) in comparison with PR solution or traditional phenylethyl resorcinol nanoliposomes (PR-LPs). The uptake and accumulation of FITC-CLPs in B16F10 cells was significantly enhanced as compared with that of FITC-LPs. Furthermore, at a PR concentration of 20 or 30[Formula: see text][Formula: see text]g/mL, PR-CLPs displayed a high tyrosinase inhibitory activity and caused a noticeable reduction in the melanin content in B16F10 cells. Taken together, these results indicate that PR-CLPs can efficiently deliver phenylethyl resorcinol to produce an enhanced skin lightening effect.

Studies on Preparation of Artesunate-Loaded mPEG-PLGA-Nanoparticles and Its Inhibition on K562 cells

Blood ◽  
2010 ◽  
Vol 116 (21) ◽  
pp. 4712-4712
Author(s):  
Liu Xiaoli ◽  
Shuang Wang ◽  
Qingfeng Du ◽  
Na Xu ◽  
Jun Yang ◽  
...  
Keyword(s):  
Drug Loading ◽  
In Vitro Release ◽  
K562 Cells ◽  
Plga Nanoparticles ◽  
Leukemia Cells ◽  
Human Leukemia ◽  
The Mean ◽  
Poly Ethylene ◽  
Vitro Release

Abstract Abstract 4712 The aim of the present work was to investigate the characterization of Artesunate-loaded methoxy poly (ethylene glyeol) -poly (lactic-co- glycolic acid) copolymer (mPEG-PLGA) nanoparticles and the anti-tumoral activity of the Art-Nps on human leukemia cells K562. The Artesunate (Art) poly (ethylene glyeol-lactic-co-glycolic acid) nanoparticles (Art-Nps) were prepared by modified-Spontaneous emulsion solvent diffusion method. The shape of the nanoparticles was observed by SEM. The mean diameter and the size distribution of nanoparticles were determined by laser light scattering. The drug loading efficiency, encapsulation rate and releasing behavior of Art -NPs in vitro were examined by HPLC. The effects of Art-Nps on the proliferation of K562 cells were studied by MTT assay and Hoechst staining. Artesunate loaded mPEG-PLGA nanoparticles were spheric with the mean size of (156.7±1.01)nm, zeta potential was -(26.23±1.86) mV, and the average drug loading and encapsulation efficiency were (14.5±0.2)% and (86.5±0.5)%, respectively. In vitro release behavior could be described by the Higuchi equation: Q=4.11t1/2+27.05, r=0.983. MTT assay showed different concentrations. different times of Art-Nps could inhibit the proliferation of K562 cells (P<0.01), and both have a synergistic effect (P=0.002), it showed that concentration was dependented with time, and the inhibition rate after 72h was exceeded to the the control group (P<0.05), it was showed the Art-Nps had sustained-release effect. Art-NPs of the cells (treated by 12.5μ g/m. 25μ g/ml. 50μ g/ml) resulted in significantly higher apoptosis than blank groups. The Art-NP obtained were characted with a small size and high drug loading and entrapment efficiency, in vitro release showed a good sustained-release nature, and it can inhibit the proliferation of human leukemia K562 cells in vitro, extending the time on leukemia cells. This study was provide an experimental basis for develop a new intravenous artesunate formulations. Disclosures: No relevant conflicts of interest to declare.

Preparation and Controlled Release Analysis of Patchouli Oil Complex Microcapsules

2011 ◽  
Vol 236-238 ◽  
pp. 2669-2672 ◽  
Author(s):  
Yang Hu ◽  
Zi Ming Yang ◽  
Jia Yi Liu ◽  
Jian Hua Cheng ◽  
Zhuo Hong Yang
Keyword(s):  
Drug Loading ◽  
In Vitro Release ◽  
Gum Arabic ◽  
Entrapment Efficiency ◽  
Complex Coacervation ◽  
Release Property ◽  
Release Analysis ◽  
Uv Visible ◽  
Vitro Release

In this paper, the patchouli oil complex microcapsules were prepared by complex coacervation method, with chitosan (CTS), quaternary ammonium salt of chitosan (HACC) and gum arabic (GA) as the wall materials, patchouli oil as the core materials. The surface morphology of microcapsules was characterized by scanning electron microscopy (SEM).The in vitro release property of patchouli oil from microcapsules was measured by UV–visible spectrophotometer. The results showed that the shapes of microcapsules were spherical, and the diameters of microcapsules were mostly 3-9 μm. The entrapment efficiency and drug loading of microcapsules were 60.6%and 20.2% respectively. The release effect of microcapsules could be influenced by the temperature of the release medium.

Preparation and In-vitro Evaluation of Fe3O4 Encapsulated by Chitosan Loaded Capecitabine Nanoparticles for the Treatment of Breast Cancer

2016 ◽  
Vol 6 (3) ◽  
Author(s):  
Shanmuganathan S. ◽  
Nigma S. ◽  
Anbarasan B. ◽  
Harika B.
Keyword(s):  
Fe3o4 Nanoparticles ◽  
Polymer Concentration ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
In Vitro Evaluation ◽  
Sem Image ◽  
Therapeutic Molecules ◽  
Dialysis Method ◽  
Vitro Release

Nanoparticulate Carriers which is biodegradable, biocompatible and bio adhesive have significant feasible applications for administration of therapeutic molecules. The present study was aimed to formulate and optimise Capecitabine loaded Chitosan-Fe3O4 Nanoparticles and to study the in-vitro evaluation by sigma dialysis method. Capecitabine loaded chitosan – Fe3O4 nanoparticles batches with different ratios of drug: polymer (1:1, 1:2, 1:3, 1:4, 1:5, 1:6) were prepared by ionic gelation method. Increase in polymer concentration increases the nanoparticle drug content. Entrapment efficiency was 60.12% with drug to polymer ratio F3 (1:3). In-vitro release was found to be 65.20% for 12 hrs. Capecitabine from chitosanFe3O4 nanoparticles SEM image reveals discrete spherical structure and particles with size range of 100-500nm. FTIR studies represent the functional groups present with no characteristics change in formulations. Samples stored at refrigerator conditions showed better stability compared with samples kept at other conditions during 8 weeks of storage.

Formulation and Evaluation of Mefloquine Hydrochloride Nanoparticles

2014 ◽  
Vol 7 (1) ◽  
pp. 2377-2386
Author(s):  
Dilip Kumar Gupta ◽  
B K Razdan ◽  
Meenakshi Bajpai
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Taste Masking ◽  
Diffusion Method ◽  
Drug Entrapment Efficiency ◽  
Resistant Strains ◽  
Vitro Release

The present study deals with the formulation and evaluation of mefloquine hydrochloride nanoparticles. Mefloquine is a blood schizonticidal quinoline compound, which is indicated for the treatment of mild-to-moderate acute malarial infections caused by mefloquine-susceptible multi-resistant strains of P. falciparum and P. vivax. The purpose of the present work is to minimize the dosing frequency, taste masking toxicity and to improve the therapeutic efficacy by formulating mefloquine HCl nanoparticles. Mefloquine nanoparticles were formulated by emulsion diffusion method using polymer poly(ε-caprolactone) with six different formulations. Nanoparticles were characterized by determining its particle size, polydispersity index, drug entrapment efficiency, drug content, particle morphological character and drug release. The particle size ranged between 100 nm to 240 nm. Drug entrapment efficacy was >95%. The in-vitro release of nanoparticles were carried out which exhibited a sustained release of mefloquine HCl from nanoparticles up to 24 hrs. The results showed that nanoparticles can be a promising drug delivery system for sustained release of mefloquine HCl.

Formulation and Evaluation of Itopride Hydrochloride Floating Beads for Gastroretentive Delivery

2013 ◽  
Vol 6 (4) ◽  
pp. 2269-2280
Author(s):  
Nagratna Dhople ◽  
P N Dandag ◽  
A P Gadad ◽  
C K Pandey ◽  
Masthiholimath V S
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Sustained Release Formulation ◽  
Prokinetic Drug ◽  
Drug Entrapment Efficiency ◽  
Itopride Hydrochloride ◽  
Vitro Release

A gastroretentive sustained release system of itopride hydrochloride was formulated to increase the gastric residence time and modulate its release behavior. Itopride hydrochloride is a prokinetic drug used in the treatment of gastroeosophageal reflux disease, Non-ulcer dyspepsia and as an antiemetic. Hence, itopride hydrochloride beads were prepared by emulsion gelation method by employing low methoxy pectin and sodium alginate as sustained release polymers in three different ratios alone and in combination and sunflower oil was used to enable floating property to the beads. The effect of variation in polymer and their concentration was investigated. The beads were evaluated for production yield, particle size, swelling index, density measurement, buoyancy, drug content, drug entrapment efficiency, in vitro release characteristics and release kinetic study. Based on drug entrapment efficiency, buoyancy, swelling and in vitro release, F9 was selected as the optimized formulation. F9 was further subjected to surface morphology by SEM, in vitro release comparison with marketed formulation, in vivo floating study in rabbits and stability study for 90 days. In vitro release follows zero order and fitted in Korsmeyer peppas model (Non-Fickian release). Therefore, the rate of drug release is due to the combined effect of drug diffusion and polymer swelling. The in vivo X-ray studies revealed that the beads were floating in the rabbit stomach up to 10 hours. Thus, it was concluded that the sustained release formulation containing itopride hydrochloride was found to improve patient compliance, minimize the side effects and decrease the frequency of administration.

Preparation, Characterization and In-vitro release of Piroxicam-loaded Solid Lipid Nanoparticles

2010 ◽  
Vol 3 (3) ◽  
pp. 1136-1146
Author(s):  
V K Verma ◽  
Ram A
Keyword(s):  
Electron Microscopy ◽  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Diffusion Method ◽  
Solid Lipid ◽  
Vitro Release

 Solid lipid nanoparticles (SLNs) of piroxicam where produced by solvent emulsification diffusion method in a solvent saturated system. The SLNs where composed of tripamitin lipid, polyvinyl alcohol (PVAL) stabilizer, and solvent ethyl acetate. All the formulation were subjected to particle size analysis, zeta potential, drug entrapment efficiency, percent drug loading determination and in-vitro release studies. The SLNs formed were nano-size range with maximum entrapment efficiency. Formulation with 435nm in particle size and 85% drug entrapment was subjected to scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for surface morphology, differential scanning calorimetry (DSC) for thermal analysis and short term stability studies. SEM and TEM confirm that the SLNs are nanometric size and circular in shape. The drug release behavior from SLNs suspension exhibited biphasic pattern with an initial burst and prolong release over 24 h. 

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.

Preparation, evaluation, and in vitro release of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules

2020 ◽  
pp. 1-9
Author(s):  
Yunhong Wang ◽  
Rong Hu ◽  
Yanlei Guo ◽  
Weihan Qin ◽  
Xiaomei Zhang ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Orthogonal Design ◽  
Drug Loading ◽  
In Vitro Release ◽  
Core Material ◽  
Evaluation Indexes ◽  
Vitro Release

OBJECTIVE: In this study we explore the method to prepare tanshinone self-microemulsifying sustained-release microcapsules using tanshinone self-microemulsion as the core material, and chitosan and alginate as capsule materials. METHODS: The optimal preparation technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules was determined by using the orthogonal design experiment and single-factor analysis. The drug loading and entrapment rate were used as evaluation indexes to assess the quality of the drug, and the in vitro release rate was used to evaluate the drug release performance. RESULTS: The best technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules is as follows: the concentration of alginate is 1.5%, the ratio of tanshinone self-microemulsion volume to alginate volume to chitosan mass is 1:1:0.5 (ml: ml: g), and the best concentration of calcium chloride is 2.0%. To prepare the microcapsules using this technology, the drug loading will be 0.046%, the entrapment rate will be 80.23%, and the 24-hour in vitro cumulative release rate will be 97.4%. CONCLUSION: The release of the microcapsules conforms to the Higuchi equation and the first-order drug release model and has a good sustained-release performance.

scholarly journals Development and Evaluation of Rifampicin Loaded Alginate–Gelatin Biocomposite Microfibers

Polymers ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1514
Author(s):  
Ameya Sharma ◽  
Vivek Puri ◽  
Pradeep Kumar ◽  
Inderbir Singh ◽  
Kampanart Huanbutta
Keyword(s):  
Wound Healing ◽  
Xanthan Gum ◽  
In Vitro Release ◽  
Antimicrobial Properties ◽  
Entrapment Efficiency ◽  
Tissue Proliferation ◽  
Naturally Occurring ◽  
Reinforcing Material ◽  
Vitro Release

Various systematic phases such as inflammation, tissue proliferation, and phases of remodeling characterize the process of wound healing. The natural matrix system is suggested to maintain and escalate these phases, and for that, microfibers were fabricated employing naturally occurring polymers (biopolymers) such as sodium alginate, gelatin and xanthan gum, and reinforcing material such as nanoclay was selected. The fabrication of fibers was executed with the aid of extrusion-gelation method. Rifampicin, an antibiotic, has been incorporated into a biopolymeric solution. RF1, RF2, RF3, RF4 and RF5 were coded as various formulation batches of microfibers. The microfibers were further characterized by different techniques such as SEM, DSC, XRD, and FTIR. Mechanical properties and physical evaluations such as entrapment efficiency, water uptake and in vitro release were also carried out to explain the comparative understanding of the formulation developed. The antimicrobial activity and whole blood clotting of fabricated fibers were additionally executed, hence they showed significant results, having excellent antimicrobial properties; they could be prominent carriers for wound healing applications.

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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