Modifying the release of leuprolide from spray dried OED microparticles

Alcock, Robert; Blair, J. A.; O’Mahony, Donagh; Raoof, Araz; Quirk, Alan V.

doi:10.1016/s0168-3659(02)00165-7

Cited by 26 publications

(14 citation statements)

References 9 publications

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“…Reverse phase chromatography (Alcock et al, 2002) (Phenomenex-Luna ® C18-5 column mm, 5 µm) running at a flow rate of 1.0 ml min -1 with UV detection (254 nm) was used. A mobile phase elution gradient was established, comprising two solvent mixtures (solvent A 0.1% TFA in acetonitrile; solvent B 0.1% TFA in water).…”

Section: Determination Of Peptide Loading Encapsulation Efficiency Amentioning

confidence: 99%

Nano-encapsulation of a novel anti-Ran-GTPase peptide for blockade of regulator of chromosome condensation 1 (RCC1) function in MDA-MB-231 breast cancer cells

Haggag

Matchett

Dakir

et al. 2017

International Journal of Pharmaceutics

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Section: Determination Of Peptide Loading Encapsulation Efficiency Amentioning

confidence: 99%

Nano-encapsulation of a novel anti-Ran-GTPase peptide for blockade of regulator of chromosome condensation 1 (RCC1) function in MDA-MB-231 breast cancer cells

Haggag

Matchett

Dakir

et al. 2017

International Journal of Pharmaceutics

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“…Insulin release from such microparticles is governed by the crystallization of the matrix upon contact with water (156). OEDs have also been employed to prepare spray-dried leuprolide acetate particles via hydrophobic ion pairing with sodium docusate (157). Pulmonary administration of such leuprolide microspheres shows controlled release of the drug with limited initial burst, which may be explained by the high glass transition temperature of OEDs (157).…”

Section: Sustained/controlled Release Formulationsmentioning

confidence: 99%

“…OEDs have also been employed to prepare spray-dried leuprolide acetate particles via hydrophobic ion pairing with sodium docusate (157). Pulmonary administration of such leuprolide microspheres shows controlled release of the drug with limited initial burst, which may be explained by the high glass transition temperature of OEDs (157). However, the safety profiles of OEDs for use in pulmonary drug delivery have yet to be established.…”

Section: Sustained/controlled Release Formulationsmentioning

confidence: 99%

Particle Engineering for Pulmonary Drug Delivery

et al. 2007

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With the rapidly growing popularity and sophistication of inhalation therapy, there is an increasing demand for tailor-made inhalable drug particles capable of affording the most efficient delivery to the lungs and the most optimal therapeutic outcomes. To cope with this formulation demand, a wide variety of novel particle technologies have emerged over the past decade. The present review is intended to provide a critical account of the current goals and technologies of particle engineering for the development of pulmonary drug delivery systems. These technologies cover traditional micronization and powder blending, controlled solvent crystallization, spray drying, spray freeze drying, particle formation from liquid dispersion systems, supercritical fluid processing and particle coating. The merits and limitations of these technologies are discussed with reference to their applications to specific drug and/or excipient materials. The regulatory requirements applicable to particulate inhalation products are also reviewed briefly.

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“…[9][10] Also, techniques such as spray drying the drug with phospholipid composites in a suitable range for pulmonary delivery 11 or the dissolution of lecithin in chlorofluorohydrocarbon and the formation of liposomes in situ 12 or nebulization of the preformed liposomes 13 can be attempted for liposomal drug delivery to lungs. Recently, many microparticle systems have been reported to be used for pulmonary drug delivery such as oligosaccharide ester derivative (OED), [14][15] biodegradable ether-anhydride polymer, 16 sodium hyaluronate, 17 and poly(lactic-co-glycolic acid) (PLGA). [18][19] We have studied the delivery of liposomal ketotifen and liposomal budesonide DPI by blending the lactose carrier with preformed liposomes as described previously and found the fine particle fraction (FPF) to be not more than 21%.…”

Section: Introductionmentioning

confidence: 99%

Liposomal amikacin dry powder inhaler: Effect of fines on in vitro performance

Shah

Misra

2004

AAPS PharmSciTech

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The aim of the present investigation was to prepare and evaluate the influence of adding fines on the in vitro performance of liposomal amikacin dry powder inhaler (AMK LDPI) formulations. Liposomes composed of hydrogenated soyaphosphatidylcholine, cholesterol and saturated soyaphosphatidylglycerol (AMK 1), or stearylamine (AMK 2) were prepared by a reverse phase evaporation technique, extruded to reduce size and separated from unentrapped drug. Purified liposomal dispersion was subjected to lyophilization using optimized cryoprotectant to achieve maximum percentage drug retention (PDR). Lactose carrier in varying mass ratios with or without addition of fines in different mixing sequences was used to formulate AMK LDPI formulations. AMK LDPI formulations were characterized for angle of repose, compressibility index, dispersibility index, scanning electron microscopy, and fine particle fraction (FPF). PDR was found to be 97.6% ± 2.2% for AMK1 and 98.5% ± 1.9% for AMK2 using sucrose as optimized cryoprotectant in lipid:sucrose ratio of 1:4. Lactose carrier containing 10% fines (wt/wt) was found to be the optimum blend at 1:5 mass ratio of liposome:lactose. The addition of fines and the order of mixing of fines were found to influence the FPF with significantly different device fractions. FPF of AMK LDPI formulations using Rotahaler as the delivery device at 30, 60, and 90 L/min were found to be 21.85% ± 2.2% and 24.6% ± 2.4%, 25.9% ± 1.8% and 29.2% ± 2.1%, and 29.5% ± 2.6% and 34.2% ± 2.0% for AMK1 and AMK2, respectively. From the studies performed in this investigation, it was observed that liposomal charge, addition of fines and order of mixing fines, has a significant effect (P < .05) on in vitro deposition of drug from LDPI formulation.KEYWORDS: liposomes, dry powder inhalers, amikacin, lactose, fines, fine particle fraction INTRODUCTIONAmikacin sulfate (AMK) is a broad-spectrum and potent aminoglycoside with limited clinical use owing to a high dose requirement and renal and audio-vestibular apparatus toxicity. 1-2 Major drawbacks associated with the use of earlier or conventional liposomal formulations are the tendency of liposomes to leak drug while in circulation, the extensive uptake of these liposomes by tissues of reticuloendothelial systems (RES), and the inability of liposomes to extravasate into infected tissue. 3-4 Therefore, localized liposomal AMK delivery was considered for the treatment of cystic fibrosis infections in the lungs. Liposomal encapsulation of AMK will give the required release of drug for a longer time duration at the localized site, thereby reducing both the chances of systemic side effects and the frequency of dosing.Improving drug delivery to the lungs from a dry powder inhaler (DPI) formulation is possible by various techniques such as smoothing the carrier surface, 5 reducing the particle size of the carrier, 6-7 and using a ternary powder mix formulation. 8 Addition of micronized lactose to coarse lactose carrier was found to improve the dispersion and deaggregation o...

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Modifying the release of leuprolide from spray dried OED microparticles

Cited by 26 publications

References 9 publications

Nano-encapsulation of a novel anti-Ran-GTPase peptide for blockade of regulator of chromosome condensation 1 (RCC1) function in MDA-MB-231 breast cancer cells

Nano-encapsulation of a novel anti-Ran-GTPase peptide for blockade of regulator of chromosome condensation 1 (RCC1) function in MDA-MB-231 breast cancer cells

Particle Engineering for Pulmonary Drug Delivery

Liposomal amikacin dry powder inhaler: Effect of fines on in vitro performance

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