Effect of Polymer Characteristics on the Thermal Stability of Retinol Encapsulated in Aliphatic Polyester Nanoparticles

Cho, Eun Chul

doi:10.5012/bkcs.2012.33.8.2560

Cited by 8 publications

(7 citation statements)

References 42 publications

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“…As for the crystalline structures, as discussed in section , the amount of crystallites in the PCL10K14-PCG6-Drug2 nanoparticles were a little lower than the PCL10K7-PCG3-Drug1 nanoparticles. Although the melting temperature of PCL10K14-PCG6-Drug2 was higher by 1–2 °C, the temperatures were far away from the storage temperatures, which would negligibly affect the formation of drug crystals . Putting these factors together, it was suggested that the nanoparticle size is the dominant factor influencing the formation of the drug crystals for the two crystalline nanoparticles in these media.…”

Section: Resultsmentioning

confidence: 99%

Internal Structure and Size Matters of Polyester Nanoparticles Encapsulating a Bioactive Hydrophobic Drug for the Prevention of Drug Crystals in Aqueous Systems

Cho

2012

Ind. Eng. Chem. Res.

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This study presents a way of preventing a highly hydrophobic bioactive drug encapsulated in polycaprolactone (PCL) nanoparticles from forming drug crystals aqueous systems. Thymol trimethoxycinnamate was selected as a hydrophobic bioactive model drug. Four PCL-drug nanoparticles were prepared: their internal structures and sizes were regulated by introducing different types of PCL or by changing polymer compositions during the preparation of the nanoparticles. The formation of drug crystals from the PCL-drug nanoparticles was observed by optical microscopy at two temperatures (25 and 40 °C) and in three aqueous mediums (deionized water or aqueous solutions containing 5 wt % butylene glycol or ethanol). In deionized water, the formation of drug crystals could be prevented if PCL-drug nanoparticles have highly crystalline cores. In aqueous solutions containing butylene glycol or ethanol, both the internal crystalline core and the size of the nanoparticles could be important in preventing the drug crystal formation. The present study provides both scientific and practical information to those who involve the drug delivery system and pharmaceutical sciences where drugs are engineered to increase the therapeutic efficiency through polymeric nanoparticles.

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Section: Resultsmentioning

confidence: 99%

Internal Structure and Size Matters of Polyester Nanoparticles Encapsulating a Bioactive Hydrophobic Drug for the Prevention of Drug Crystals in Aqueous Systems

Cho

2012

Ind. Eng. Chem. Res.

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“…RET as terpene alcohol has already been applied as the initiator of the ring-opening polymerization (ROP) of ethylene oxide [3] or lactide [4] resulting in welldefined biohybrid polymers with potential applications as liquid crystalline materials, amphiphilies, or conjugate systems targeted to stellate liver cells. However, according to the literature the delivery of RET is supported by encapsulation strategy, mostly into chitozan [5][6][7], and polyester (polyadipates, polycaprolactone) [8] nanoparticles. Moreover, spherical inorganic particles containing RET have been fabricated using silica in combination with surfactants and hydroxypropyl cellulose [9], tetraethyl orthosilicate sol-gel systems [10], or polyphosphates with calcium ions [11].…”

Section: Introductionmentioning

confidence: 99%

Retinol derivative as bioinitiator in the synthesis of hydroxyl-functionalized polymethacrylates for micellar delivery systems

Odrobińska¹,

Neugebauer²

2019

Express Polym. Lett.

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Amphiphilic copolymers containing 2-hydroxyethyl methacrylate (HEMA) and methyl methacrylate (MMA) units were synthesized by controlled atom transfer radical polymerization (ATRP) applying bromoester modified retinol (RETBr) as a novel initiator. Analogous series of copolymers with adjustable hydrophilic-hydrophobic balance was obtained with the use of a standard initiator, i.e. ethyl α-bromoisobutyrate (EBriB). The self-assembling particles, prepared by the solvent evaporation, were loaded with vitamin C (VitC) or ferulic acid (FA). The hydrophilic/hydrophobic ratio in the copolymer was indicated as a crucial factor to regulate efficiencies of encapsulation processes in the range of 53-98%. In vitro release of bioactive substance was carried out in phosphate buffer solution (PBS) at pH 7.4 with the maximum amount of VitC after 1h (27-62%) or FA within 2 h (71-97%). The polymeric systems with satisfactory encapsulation characteristics and release profiles are attractive micellar carriers of antioxidants, which, due to their activities could be also delivered using the popular approaches in cosmetology like masks, under-eye patches, or wraps.

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“…With regard to enhanced stability, it has been previously demonstrated that the water vapor permeability of BMC (51) is lower than what is commonly used for preservation of fruits and vegetables (52); thus, it is likely that the known moisture barrier properties of BMC provide protection against humidity and small-molecule diffusion by acting as a physical barrier between the payload and the environment. The UV-protective abilities of BMC can likely be attributed to the increased refractive index due to encapsulation in BMC (53), which will lower light exposure to encapsulated micronutrients. BMC is soluble at low pH in aqueous solutions and in non-aqueous solvents; hence, the solubility of BMC enabled rapid dissolution and release in stomach conditions, thus providing the versatility to facilitate encapsulation of 11 distinct micronutrients.…”

Section: Discussionmentioning

confidence: 99%

“…5A). Cooking the encapsulated ferrous sulfate had no effect on its bioavailability [FIA, 1.41 (0.91, 2.19)%; RBV, 42 (34,53)%] (Fig. 5A).…”

Section: Bioavailability Of Iron In Humans and Iron Transport In An I...mentioning

confidence: 99%

A heat-stable microparticle platform for oral micronutrient delivery

Anselmo

Buerkli

et al. 2019

Sci. Transl. Med.

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Micronutrient deficiencies affect up to 2 billion people and are the leading cause of cognitive and physical disorders in the developing world. Food fortification is effective in treating micronutrient deficiencies; however, its global implementation has been limited by technical challenges in maintaining micronutrient stability during cooking and storage. We hypothesized that polymer-based encapsulation could address this and facilitate micronutrient absorption. We identified poly(butylmethacrylate-co-(2-dimethylaminoethyl)methacrylate-co-methylmethacrylate) (1:2:1) (BMC) as a material with proven safety, offering stability in boiling water, rapid dissolution in gastric acid, and the ability to encapsulate distinct micronutrients. We encapsulated 11 micronutrients (iron; iodine; zinc; and vitamins A, B2, niacin, biotin, folic acid, B12, C, and D) and co-encapsulated up to 4 micronutrients. Encapsulation improved micronutrient stability against heat, light, moisture, and oxidation. Rodent studies confirmed rapid micronutrient release in the stomach and intestinal absorption. Bioavailability of iron from microparticles, compared to free iron, was lower in an initial human study. An organotypic human intestinal model revealed that increased iron loading and decreased polymer content would improve absorption. Using process development approaches capable of kilogram-scale synthesis, we increased iron loading more than 30-fold. Scaled batches tested in a follow-up human study exhibited up to 89% relative iron bioavailability compared to free iron. Collectively, these studies describe a broad approach for clinical translation of a heat-stable ingestible micronutrient delivery platform with the potential to improve micronutrient deficiency in the developing world. These approaches could potentially be applied toward clinical translation of other materials, such as natural polymers, for encapsulation and oral delivery of micronutrients.

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Effect of Polymer Characteristics on the Thermal Stability of Retinol Encapsulated in Aliphatic Polyester Nanoparticles

Cited by 8 publications

References 42 publications

Internal Structure and Size Matters of Polyester Nanoparticles Encapsulating a Bioactive Hydrophobic Drug for the Prevention of Drug Crystals in Aqueous Systems

Internal Structure and Size Matters of Polyester Nanoparticles Encapsulating a Bioactive Hydrophobic Drug for the Prevention of Drug Crystals in Aqueous Systems

Retinol derivative as bioinitiator in the synthesis of hydroxyl-functionalized polymethacrylates for micellar delivery systems

A heat-stable microparticle platform for oral micronutrient delivery

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