Novel Spray-Dried Genipin-Crosslinked Casein Nanoparticles for Prolonged Release of Alfuzosin Hydrochloride

Elzoghby, Ahmed O.; Samy, Wael M.; Elgindy, Nazik A.

doi:10.1007/s11095-012-0897-z

Cited by 89 publications

(19 citation statements)

References 40 publications

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“…2 In our previous study we used a spraydrying technique to generate genipin-crosslinked CAS nanoparticles for prolonged release of alfuzosin hydrochloride. 12 Prostate cancer has the highest incidence of all kinds of cancers and is the second most deadly cancer in men, after lung cancer. 13 Flutamide (FLT) is an antiandrogenic agent presently used for monotherapy of androgen-dependent prostate cancer.…”

Section: Introductionmentioning

confidence: 99%

Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics

Elzoghby¹,

Helmy²,

Samy³

et al. 2013

IJN

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A novel particulate delivery matrix based on ionically crosslinked casein (CAS) nanoparticles was developed for controlled release of the poorly soluble anticancer drug flutamide (FLT). Nanoparticles were fabricated via oil-in-water emulsification then stabilized by ionic crosslinking of the positively charged CAS molecules below their isoelectric point, with the polyanionic crosslinker sodium tripolyphosphate. With the optimal preparation conditions, the drug loading and incorporation efficiency achieved were 8.73% and 64.55%, respectively. The nanoparticles exhibited a spherical shape with a size below 100 nm and a positive zeta potential (+7.54 to +17.3 mV). FLT was molecularly dispersed inside the nanoparticle protein matrix, as revealed by thermal analysis. The biodegradability of CAS nanoparticles in trypsin solution could be easily modulated by varying the sodium tripolyphosphate crosslinking density. A sustained release of FLT from CAS nanoparticles for up to 4 days was observed, depending on the crosslinking density. After intravenous administration of FLT-CAS nanoparticles into rats, CAS nanoparticles exhibited a longer circulation time and a markedly delayed blood clearance of FLT, with the half-life of FLT extended from 0.88 hours to 14.64 hours, compared with drug cosolvent. The results offer a promising method for tailoring biodegradable, drug-loaded CAS nanoparticles as controlled, long-circulating drug delivery systems of hydrophobic anticancer drugs in aqueous vehicles.

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Section: Introductionmentioning

confidence: 99%

Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics

Elzoghby¹,

Helmy²,

Samy³

et al. 2013

IJN

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“…Alfuzosin hydrochloride was dissolved directly in casein solution, and genipin in ethanol was added to achieve cross-linking. Nanoparticles were obtained by spray-drying [95, 96]. Powdered nanoparticles were then tableted using a single-punch tablet press.…”

Section: Casein Delivery Particlesmentioning

confidence: 99%

“…Casein-based tablets floated much faster than marketed ones. Both formulations prolonged alfuzosin release for 24 h [95], whereas drug release could be modulated by altering the cross-linking degree in the case of the casein tablets [95, 96]. …”

Section: Casein Delivery Particlesmentioning

confidence: 99%

Potential of Casein as a Carrier for Biologically Active Agents

2017

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Casein is the collective name for a family of milk proteins. In bovine milk, casein comprises four peptides: αS1, αS2, β, and κ, differing in their amino acid, phosphorus and carbohydrate content but similar in their amphiphilic character. Hydrophilic and hydrophobic regions of casein show block distribution in the protein chain. Casein peptides carry negative charge on their surface as a result of phosphorylation and tend to bind nanoclusters of amorphous calcium phosphate. Due to these properties, in suitable conditions, casein molecules agglomerate into spherical micelles. The high content of casein in milk (2.75 %) has made it one of the most popular proteins. Novel research techniques have improved understanding of its properties, opening up new applications. However, casein is not just a dietary protein. Its properties promise new and unexpected applications in science and the pharmaceutical and functional food industries. One example is an encapsulation of health-related substances in casein matrices. This review discusses gelation, coacervation, self-assembly and reassembly of casein peptides as means of encapsulation. We highlight information on encapsulation of health-related substances such as drugs and dietary supplements inside casein micro- and nanoparticles.

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“…The atomized aqueous extract was then fed into LabPlant Mini-Spray dryer SD-06AG (Lab-Plant, UK). Where, the inlet-temperature was adjusted at 165 °C and the feed rate was adjusted keeping the outlet-temperature at 75-80 °C [6]. The spray dried extract (HS-sd) was collected and kept in a desiccator till further testing.…”

Section: Ultrasound-assisted Spray Drying Versus Conventional Rotary-mentioning

confidence: 99%

Phytochemical and Biological Evaluation of Ultrasound-Assisted Spray Dried Lonicera etrusca for Potential Management of Diabetes

Raafat¹,

Samy²

2018

Rec.Nat.Prod.

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Honeysuckle or Lonicera etrusca is one of the important medicinal-plants that is traditionally-used as a potential antioxidant. The aim of this work was to make a phytochemical-evaluation of Lonicera etrusca ultrasound-assisted spray-dried extract versus conventional-method utilizing RP-HPLC aided-method in the potential management of diabetes. Ultrasound-assisted spray-drying (US-SD) is a new productive-technique aiming at increasing the efficiency and extract-yield in addition to short time of exposure to elevated temperature thus improving product stability. A bio-guided study utilizing RP-HPLC, 1 H and 13 C NMR methods indicated that the most active antidiabetic-compound was isochlorogenic acid (ICA). Diabetes measurement utilizing glucometers and HbA1c methods was applied. Serum-insulin levels and serum-catalase (CAT) was also monitored. The US-SD preserved time by 4 folds and with higher yield (ca. 20%) than the conventional method. The US-SD also had higher quality in US-SD honeysuckle (HS-sd) constituents than the conventional method as supported by RP-HPLC analysis. Rotary evaporated honeysuckle (HS-r) major peaks identified were; chlorogenic acid (38.6%), caffeic acid (5.8%), isochlorogenic acid (36.1%), luteolin-7-O-glucoside (3.3%), and quercetin (3.0%). HS-sd major peaks identified were; chlorogenic acid (40.5%), caffeic acid (6.4%), isochlorogenic acid (43.3%), luteolin-7-O-glucoside (3.5%), and quercetin (3.2%). HS-sd had significant (p˂0.05, n=7/group) antidiabetic-activity more than HS-r. HS-sd had more-significant dose-dependent increase in serum-insulin, CATlevels and body-weights more prominent than HS-r. Compared to conventional-methods, US-SD has shown to be time-conserving, efficient, and active-ingredients preserving method. The antidiabetic-potentials of HS-sd and ICA were probably mediated via the significant insulin-secretagogue effect and the attenuation glucose-provoked oxidative-stress.

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Novel Spray-Dried Genipin-Crosslinked Casein Nanoparticles for Prolonged Release of Alfuzosin Hydrochloride

Abstract: These results demonstrated that genipin-crosslinking combined with spray-drying technique could be used as a promising tool to develop solid redispersible casein nanoparticles with sustained drug release properties.

Cited by 89 publications

References 40 publications

Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics

Novel ionically crosslinked casein nanoparticles for flutamide delivery: formulation, characterization, and in vivo pharmacokinetics

Potential of Casein as a Carrier for Biologically Active Agents

Phytochemical and Biological Evaluation of Ultrasound-Assisted Spray Dried Lonicera etrusca for Potential Management of Diabetes

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