Development of lauroyl sulfated chitosan for enhancing hemocompatibility of chitosan

The present study deals with the encapsulation of vegetable organogels in alginate microparticles (MPs). Mango butter (MB) and cocoa butter (CB) are natural organogels, which are being used in the preparation of pharmaceutical formulations. In addition to these, mustard oil (MO) was used as the control. The thermal stability of MB and CB can be enhanced by encapsulating them and can be used in oral drug-delivery formulations. Double emulsification method was followed for the preparation of MPs. By this method, spherical MPs were synthesized and the sphericity was confirmed by doing light microscopy and scanning electron microscopy. The size range of MPs was 107 ± 53 μm, 79 ± 43 μm, and 112 ± 78 μm for MPs encapsulating MO, MB, and CB, respectively. The melting endotherms of MPs with MB and CB were in exact match with the melting points of MB and CB. This confirmed the existence of MB and CB within the MPs. The encapsulation of the vegetable organogels altered the release pattern of the drug, metronidazole. The drug release kinetics suggested that the release pattern followed the non-Fickian kinetics. The MPs were found to be hemocompatible in nature and have shown good mucoadhesive and swelling properties. Based on the preliminary results, it was suggested that the vegetable organogels can be encapsulated in alginate MPs and used as drug-delivery vehicles.

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“…The study was conducted for 10 min. The % swelling of MPs was calculated from the equation 1 [30,31]. The measurements were done at RT.…”

Section: Swelling Studiesmentioning

confidence: 99%

“…The MPs were analyzed for hemolysis by incubating them in the presence of goat blood at 37 ± 1°C, as described elsewhere [30]. The method calculates the extent of hemolysis in the presence of the samples.…”

Section: Hemocompatibility Studiesmentioning

confidence: 99%

Encapsulation of vegetable organogels for controlled delivery applications

Sagiri

Sethy

Pal

et al. 2012

Designed Monomers and Polymers

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“…[60][61][62][63] To assess the in vivo utility of a nanoformulation as a carrier for curcumin, the hemolytic potential in human blood needs to be tested. 64,65 Therefore, we evaluated a direct nanoparticle-erythrocyte membrane interaction in which the extent of disruption of the erythrocyte membrane was a direct measure of nanoparticle toxicity (Figure 4).…”

Section: Hemolysismentioning

confidence: 99%

Interaction of curcumin nanoformulations with human plasma proteins and erythrocytes

Yallapu¹,

Ebeling²,

Chauhan³

et al. 2011

IJN

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Background Recent studies report curcumin nanoformulation(s) based on polylactic- co -glycolic acid (PLGA), β-cyclodextrin, cellulose, nanogel, and dendrimers to have anticancer potential. However, no comparative data are currently available for the interaction of curcumin nanoformulations with blood proteins and erythrocytes. The objective of this study was to examine the interaction of curcumin nanoformulations with cancer cells, serum proteins, and human red blood cells, and to assess their potential application for in vivo preclinical and clinical studies. Methods The cellular uptake of curcumin nanoformulations was assessed by measuring curcumin levels in cancer cells using ultraviolet-visible spectrophotometry. Protein interaction studies were conducted using particle size analysis, zeta potential, and Western blot techniques. Curcumin nanoformulations were incubated with human red blood cells to evaluate their acute toxicity and hemocompatibility. Results Cellular uptake of curcumin nanoformulations by cancer cells demonstrated preferential uptake versus free curcumin. Particle sizes and zeta potentials of curucumin nanoformulations were varied after human serum albumin adsorption. A remarkable capacity of the dendrimer curcumin nanoformulation to bind to plasma protein was observed, while the other formulations showed minimal binding capacity. Dendrimer curcumin nanoformulations also showed higher toxicity to red blood cells compared with the other curcumin nanoformulations. Conclusion PLGA and nanogel curcumin nanoformulations appear to be very compatible with erythrocytes and have low serum protein binding characteristics, which suggests that they may be suitable for application in the treatment of malignancy. These findings advance our understanding of the characteristics of curcumin nanoformulations, a necessary component in harnessing and implementing improved in vivo effects of curcumin.

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“…The phase-transition temperature of a bilayer lipid membrane directly determines its liquidity, which in turn affects the release of CU from liposomes. Under the experimental temperature conditions, the lower film liquidity of the bilayer lipid membrane in CU-HSPC-C was less than in CU-SPC-C, which slowed down the release of CU from the CU-HSPC-C. Hemolysis is a type of acute toxicity assay used to evaluate the hemocompatibility of the complexes and to detect hemolyzation of red blood cells (Koziara et al, 2005;Ciochina et al, 2009;Mayer et al, 2009;Shelma & Sharma, 2011). To evaluate the in vivo utility of a CU-PC-C and CU-HSPC-C as a carrier for CU, the hemolytic potential in human blood needs to be tested (Fischer & Chan, 2007;Grainger, 2009).…”

Section: Discussionmentioning

confidence: 99%

Development, characterization and toxicological evaluations of phospholipids complexes of curcumin for effective drug delivery in cancer chemotherapy

et al. 2014

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The purpose of this study was to prepare and characterize the complexes between curcumin (CU) phosphatidylcholine (PC) and hydrogenated soya phosphatidylcholine (HSPC) and to evaluate their anticancer activity. These CU-PC and CU-HSPC complexes (CU-PC-C and CU-HSPC-C) were evaluated for various physical parameters like Fourier transform infrared spectroscopy, melting point, solubility, scanning electron microscopy and the in vitro drug release study. These data confirmed the formation of phospholipids complexes. The in vitro hemolysis study showed that the complex was non-hemolytic. The anti-cancer potential of the complexes was demonstrated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay in MCF-7 cell line. This increase may be due to the amphiphilic nature of the complexes, which significantly enhances the water and lipid solubility of the CU. Unlike the free CU (which showed a total of only 90% drug release at the end of 8 h), complex showed around 40-60% release at the end of 8 h in dissolution studies. It showed that (when given in equimolar doses) complexes have significantly decreased the amount of CU available for absorption as compared with CU-free drug. Both CU-PC-C and CU-HSPC-C were found to be non-toxic at the dose equivalent to 2000 mg/kg of body weight of CU in the toxicity study. Acute and subacute toxicity studies confirmed the oral safety of the formulation. A series of genotoxicity studies was conducted, which revealed the non-genotoxicity potential of the developed complexes. Thus, it can be concluded that the phospholipid complexes of CU may be a promising candidate in cancer therapy.

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Development of lauroyl sulfated chitosan for enhancing hemocompatibility of chitosan

Cited by 97 publications

References 26 publications

Encapsulation of vegetable organogels for controlled delivery applications

Encapsulation of vegetable organogels for controlled delivery applications

Interaction of curcumin nanoformulations with human plasma proteins and erythrocytes

Development, characterization and toxicological evaluations of phospholipids complexes of curcumin for effective drug delivery in cancer chemotherapy

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