Amphiphilic amino acid copolymers as stabilizers for the preparation of nanocrystal dispersion

Lee, Jonghwi; Lee, Soo Jeong; Choi, Ji-Yeun; Yoo, Ji Youn; Ahn, Cheol‐Hee

doi:10.1016/j.ejps.2004.12.010

Cited by 111 publications

(60 citation statements)

References 27 publications

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“…The stabilization effects on the nanosuspensions were attributed to two factors. Firstly, adsorption of protein onto the drug particles produced effective steric stabilization, 3,25 and secondly, the surface charge from submit your manuscript | www.dovepress.com…”

Section: Results and Discussion Preparation And Characterization Of Nmentioning

confidence: 99%

Formulating food protein-stabilized indomethacin nanosuspensions into pellets by fluid-bed coating technology: physical characterization, redispersibility, and dissolution

Lü²,

Qi³

et al. 2013

IJN

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Background: Drug nanosuspensions are very promising for enhancing the dissolution and bioavailability of drugs that are poorly soluble in water. However, the poor stability of nanosuspensions, reflected in particle growth, aggregation/agglomeration, and change in crystallinity state greatly limits their applications. Solidification of nanosuspensions is an ideal strategy for addressing this problem. Hence, the present work aimed to convert drug nanosuspensions into pellets using fluid-bed coating technology. Methods: Indomethacin nanosuspensions were prepared by the precipitation-ultrasonication method using food proteins (soybean protein isolate, whey protein isolate, β-lactoglobulin) as stabilizers. Dried nanosuspensions were prepared by coating the nanosuspensions onto pellets. The redispersibility, drug dissolution, solid-state forms, and morphology of the dried nanosuspensions were evaluated. Results: The mean particle size for the nanosuspensions stabilized using soybean protein isolate, whey protein isolate, and β-lactoglobulin was 588 nm, 320 nm, and 243 nm, respectively. The nanosuspensions could be successfully layered onto pellets with high coating efficiency. Both the dried nanosuspensions and nanosuspensions in their original amorphous state and not influenced by the fluid-bed coating drying process could be redispersed in water, maintaining their original particle size and size distribution. Both the dried nanosuspensions and the original drug nanosuspensions showed similar dissolution profiles, which were both much faster than that of the raw crystals. Conclusion: Fluid-bed coating technology has potential for use in the solidification of drug nanosuspensions.

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Section: Results and Discussion Preparation And Characterization Of Nmentioning

confidence: 99%

Formulating food protein-stabilized indomethacin nanosuspensions into pellets by fluid-bed coating technology: physical characterization, redispersibility, and dissolution

Lü²,

Qi³

et al. 2013

IJN

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“…For example, Lee et al (2005) synthesized amino acid block copolymers based on various combinations of lysine, phenylalanine, leucine and alanine via ring opening polymerization. Various compositional and morphological effects of block copolymers were investigated in this study.…”

Section: Theorymentioning

confidence: 99%

Solid Nanosuspensions: The Emerging Technology and Pharmaceutical Applications as Nanomedicine

Verma

Burgess

2009

Pharmaceutical Suspensions

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One of the foremost reasons for such a widespread interest in nanosuspensions as drug delivery systems is their ability to provide formulations of poorly soluble drugs with increased saturation solubility and higher dissolution rates. Nanosuspensions manifest these properties because of their small size and high surface area. The unique properties of the nanosuspensions along with their fast development times, low production costs, ease of manufacture and scale-up as well as their ability to extend the lifecycle of off-patent drugs have resulted in rapid commercialization. Nanosuspensions provide us with a useful tool for formulating an ever-increasing number of poorly water soluble drugs in pharmaceutical development programs.

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“…[15] The instability of the finely divided particles and their tendency to agglomerate is due to increase the effective surface of the drug particles, which is associated with a proportional vast increase of the surface energy. [16] Among the preparation methods of nanoparticles, nano-comminution has conveniently been utilized to prepare solid nanoparticles due to simplicity and cost-effectiveness. [17,18] Furthermore, an additional advantage of using wet comminution is that no organic solvent or harsh environment is needed and scaling-up to industrial level is easy.…”

Section: Introductionmentioning

confidence: 99%

Untitled

Nada

2017

AJP

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Introduction: Ibuprofen (IBU), a well-known drug with dissolution rate-limited bioavailability was formulated as nanoparticles and nanosuspensions by ultra-homogenization technique, employing a series of hydrophilic polymers/surfactants. Materials and Methods: Various nanosuspensions were prepared using different hydrophilic polymers, freeze-dried into nano-particles and evaluated for relevant physicochemical characteristics. Based on the in vitro dissolution and particle size, the optimized drug: Polymer ratio was re-formulated into nanosuspensions using Tween-80 to study any further reduction in particle size and enhancement in dissolution as compared with marketed suspensions. Results and Discussion: All the suspensions prepared with the different drugs: Polymer ratio (1:1, 1:2 and 1:3) showed a significant decrease in particle size with increase in the number of homogenization cycles and pressure. Polyvinyl pyrrolidone K30 (PVP-K30) served as the best polymer to enhance the aqueous solubility of IBU, based on stability constant (K) and Gibbsfree energy (ΔG o ) values. IBU: PVP-K30 (1:2 w/w) nanosuspensions gave the least particle size (527 ± 31.04 nm) with a narrow polydispersibility index and high negative zeta potential value. Nanoparticles produced by freeze drying the nano-suspension were amorphous in nature as confirmed by differential scanning calorimetry and Fourier transform infrared and also showed enhanced release rate than the pure drug. Furthermore, a combination of IBU: PVP-K30:Tween 80 (T80) (1:2:2 w/w) homogenized nanosuspensions exhibited much smaller particle size (127 ± 6.18 nm) and two-fold faster release compared to the marketed products (DP 15 min = 95%). Other polymer combinations either did not show any significant change in particle size or exhibited agglomeration and crystal growth. Conclusion: IBU/ PVP-K30/T80 nanosuspensions were successfully prepared by high-pressure homogenization technique, with enhanced solubility and dissolution properties which could reduce the required dose and gastrointestinal side effects of the pure drug. This, in turn, is expected to increase the therapeutic benefits of IBU and other similar drugs belonging to Class II of Biopharmaceutics Classification System system, as well as to decrease/abolish the ulcerative effect. The proposed technique also has the potential of commercial scale-up to formulate safe products with higher bioavailability.

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Amphiphilic amino acid copolymers as stabilizers for the preparation of nanocrystal dispersion

Cited by 111 publications

References 27 publications

Formulating food protein-stabilized indomethacin nanosuspensions into pellets by fluid-bed coating technology: physical characterization, redispersibility, and dissolution

Formulating food protein-stabilized indomethacin nanosuspensions into pellets by fluid-bed coating technology: physical characterization, redispersibility, and dissolution

Solid Nanosuspensions: The Emerging Technology and Pharmaceutical Applications as Nanomedicine

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