Improving solubility and chemical stability of natural compounds for medicinal use by incorporation into liposomes

Coimbra, Maria; Isacchi, Benedetta; Bloois, Louis van; Toraño, Javier Sastre; Ket, Aldo; Wu, Xing‐De; Broere, Femke; Metselaar, Josbert M.; Rijcken, Cristianne J.F.; Storm, Gert; Bilia, Anna Rita; Schiffelers, Raymond M.

doi:10.1016/j.ijpharm.2011.01.056

Cited by 284 publications

(162 citation statements)

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“…The preservation of the antioxidant activity after three months storage in nanoencapsulated form suggests that lipidic nanoemulsions can present a solution to the problem of instability of resveratrol, which was reported to be easily oxidized (Frozza et al, 2011). This also came in accordance with several other authors (Lucas-Abellán et al, 2007;Caddeo et al, 2008;Coimbra et al, 2011;Sessa et al, 2014), who declared that encapsulation of resveratrol in carriers, such as cyclodextrin complexes, liposomes and lecithin-based nanoemulsions were able to improve the stability of resveratrol. Similarly, this could be applied to curcumin, in which authors reported that its encapsulation in nanoformulations improves its stability (Rachmawati et al, 2015).…”

Section: Stability Of the Selected Nanoemulsion Formulasupporting

confidence: 86%

Development of an optimized hyaluronic acid-based lipidic nanoemulsion co-encapsulating two polyphenols for nose to brain delivery

Nasr

2015

Drug Delivery

164

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RESEARCH ARTICLEDevelopment of an optimized hyaluronic acid-based lipidic nanoemulsion co-encapsulating two polyphenols for nose to brain delivery Maha NasrDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt AbstractThe development of mucoadhesive lipidic nanoemulsion based on hyaluronic acid, co-encapsulating two polyphenols (resveratrol and curcumin) for the transnasal treatment of neurodegenerative diseases was attempted in the current manuscript. Nanoemulsions were prepared by the spontaneous emulsification method, and were characterized for their particle size, zeta potential, mucoadhesive strength and morphology. The selected formula was tested for its antioxidant potential, in vitro and ex vivo release of the two polyphenols, safety on nasal mucosa and in vivo quantification of the two drugs in rat brains. Its stability was tested by monitoring the change in particle size, zeta potential, drugs' content and antioxidant potential upon storage for 3 months. The optimized hyaluronic acid based nanoemulsion formula displayed a particle size of 115.2 ± 0.15 and a zeta potential of À23.9 ± 1.7. The formula displayed a spherical morphology and significantly higher mucoadhesive strength compared to its non mucoadhesive counterpart. In addition, the nanoemulsion was able to preserve the antioxidant ability of the two polyphenols and protect them from degradation. Diffusion controlled release of the two drugs was achievable till 6 hours, with an ex vivo flux across sheep nasal mucosa of 2.86 and 2.09 mg/cm 2 hr for resveratrol and curcumin, respectively. Moreover, the mucoadhesive nanoemulsion was safe on nasal mucosa and managed to increase the amounts of the two polypehnols in the brain (about 7 and 9 folds increase in AUC 0-7 h for resveratrol and curcumin, respectively). Hyaluronic acid based lipidic nanoemulsion proved itself as a successful carrier enhancing the solubility, stability and brain targetability of polyphenols.

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Section: Stability Of the Selected Nanoemulsion Formulasupporting

confidence: 86%

Development of an optimized hyaluronic acid-based lipidic nanoemulsion co-encapsulating two polyphenols for nose to brain delivery

Nasr

2015

Drug Delivery

164

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“…To address this issue, researchers have 27 developed multiple techniques, e.g. salt formation [2], solubilization [3], 28 complexation [4], liposome [5,6], nanoparticles [7], nanoemulsion [8]and so on. But 29 these formulation techniques can only be used to a certain number of drugs exhibiting A c c e p t e d M a n u s c r i p t 5 ultra-pure water and mixed under magnetic stirring.…”

Section: Introductionmentioning

confidence: 99%

The construction of puerarin nanocrystals and its pharmacokinetic and in vivo–in vitro correlation (IVIVC) studies on beagle dog

et al. 2015

Colloids and Surfaces B: Biointerfaces

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“…They can be nontoxic, long-lasting, slow-release, biocompatible with drugs, and inert toward many drugs. Additionally, they can decrease the toxicity of drugs, target lymph tissue, and increase the solubility and stability of drugs (Coimbra et al, 2011). Such properties make liposomes a suitable biomaterial for controlled drug release systems.…”

Section: Discussionmentioning

confidence: 99%

Retinoic acid liposome-hydrogel: preparation, penetration through mouse skin and induction of F9 mouse teratocarcinoma stem cells differentiation

Xia

Cheng

Xu³

et al. 2015

Braz. J. Pharm. Sci.

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Retinoic acid (RA), a metabolite of retinol, is one of the most biologically active forms of retinoid and plays vital roles in embryonic development and in the regulation of cell proliferation and differentiation.Knowing that liposomes simulate cell membranes and that hydrogel is an ideal delivery vehicle for topical medicine, liposome-hydrogel is a novel preparation that has synergistic advantages over each component separately. Our objective was to investigate the characteristics of RA liposome-hydrogel. For quality control of the RA-loaded liposomes, we measured their morphology, particle size, Zeta-potential, and entrapment efficiency. Then we determined the viscosity of RA liposome-hydrogel. Next, the diffusion through mouse skin was explored, followed by investigation of the mRNA expression levels of Ker18, REX1, and α-FP using Q-PCR. The results showed that RA liposome-hydrogel penetrates the mouse skin effectively. The permeation rates were: Q n (%) of RA liposome-hydrogel < Q n (%) of RA-loaded liposome < Q n (%) of RA. The mRNA expression levels were dose-dependent and the effective dose decreased between vehicles due to their different release rates. F9 mouse teratocarcinoma stem cells were an ideal model to explore the mechanism of RA liposome-hydrogel in stem cell differentiation.Uniterms: Retinoic acid (RA). RA liposome-hydrogel/characteristics. RA liposome-hydrogel/preparation. RA liposome-hydrogel/diffusion/experimental study. F9 cell/differentiation. O ácido retinóico (RA) é um metabolito de retinol. Ele também é uma das formas mais biologicamente ativas de retinóide. Desempenha papel vital no desenvolvimento embrionário e na regulação da proliferação e diferenciação celular. Sabendo-se que lipossomas simulam a membrana das células e que hidrogel é um sistema ideal para o medicamento tópico, o lipossoma-hidrogel é uma nova preparação, que apresenta vantagens sinérgicas em relação a cada um dos componentes separados. Nosso objetivo foi investigar as características de RA lipossoma-hidrogel. A fim de controlar a qualidade do lipossoma carregado com RA, medimos morfologia, tamanho das partículas, potencial zeta e eficiência de retenção. Em seguida, determinou-se a viscosidade de RA lipossoma-hidrogel. Em seguida, avaliou-se a sua difusão através da pele de camundongos, seguida da investigação dos níveis da expressão de mRNA de Ker18, REX e de α-FP, utilizando-se Q-PCR. Os resultados mostraram que RA lipossoma-hidrogel pode penetrar na pele do camundongo de forma eficaz. As taxas de permeação foram: Qn (%) de RA lipossoma-hidrogel

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Improving solubility and chemical stability of natural compounds for medicinal use by incorporation into liposomes

Cited by 284 publications

References 50 publications

Development of an optimized hyaluronic acid-based lipidic nanoemulsion co-encapsulating two polyphenols for nose to brain delivery

Development of an optimized hyaluronic acid-based lipidic nanoemulsion co-encapsulating two polyphenols for nose to brain delivery

The construction of puerarin nanocrystals and its pharmacokinetic and in vivo–in vitro correlation (IVIVC) studies on beagle dog

Retinoic acid liposome-hydrogel: preparation, penetration through mouse skin and induction of F9 mouse teratocarcinoma stem cells differentiation

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