Protein encapsulation into biodegradable microspheres by a novel S/O/W emulsion method using poly(ethylene glycol) as a protein micronization adjuvant

Morita, Takahiro; Sakamura, Yumi; Horikiri, Yuji; Suzuki, Takehiko; Yoshino, Hideaki

doi:10.1016/s0168-3659(00)00326-6

Cited by 141 publications

(102 citation statements)

References 23 publications

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“…The rhEPO-loaded PLGA microspheres were prepared using a modified s/o/w method [11] . Briefly, 10 mg of the rhEPO-HSA mixture microparticles was suspended in 2.5 mL of dichloromethane solution containing 180 mg/mL of PLGA.…”

Section: Preparation Of the Rhepo-loaded Plga Microspheresmentioning

confidence: 99%

Pharmacokinetic and pharmacodynamic profiles of recombinant human erythropoietin-loaded poly(lactic-co-glycolic acid) microspheres in rats

Zhou

et al. 2011

Acta Pharmacol Sin

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Aim: To characterize the pharmacokinetic and pharmacodynamic profiles of the recombinant human erythropoietin (rhEPO)-loaded poly(lactic-co-glycolic acid) (PLGA) microspheres in rats. Methods: The rhEPO-loaded microspheres were prepared using a solid-in-oil-in-water emulsion method. Pharmacokinetics and pharmacodynamics of the rhEPO-loaded microspheres were evaluated in male Sprague-Dawley rats. The serum rhEPO level was determined with ELISA. The level of anti-rhEPO antibody in the serum was measured to assess the immunogenicity of rhEPO released from the microspheres. Results: rhEPO was almost completely released from the PLGA microspheres in vitro, following zero-order release kinetics over approximately 30 d. After intramuscular injection (10 000 or 30 000 IU rhEPO/kg) in the rats, the serum rhEPO concentration reached maximum levels on d 1, then decreased gradually and was maintained at nearly steady levels for approximately 4 weeks. Furthermore, the release of rhEPO from the PLGA microspheres was found to be controlled mainly by a dissolution/diffusion mechanism. A good linear correlation (R 2 =0.98) was obtained between the in vitro and in vivo release data. A single intramuscular injection of the rhEPOloaded PLGA microspheres (10 000 or 30 000 IU rhEPO/kg) in the rats resulted in elevated hemoglobin and red blood cell concentrations for more than 28 d. Moreover, the immunogenicity of rhEPO released from the PLGA microspheres was comparable with that of the unencapsulated rhEPO. Conclusion:The results prove the feasibility of using the PLGA-based microspheres to deliver rhEPO for approximately 1 month.

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Section: Preparation Of the Rhepo-loaded Plga Microspheresmentioning

confidence: 99%

Pharmacokinetic and pharmacodynamic profiles of recombinant human erythropoietin-loaded poly(lactic-co-glycolic acid) microspheres in rats

Zhou

et al. 2011

Acta Pharmacol Sin

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“…The particle size in case of S/O/W emulsion is dependent on several factors such as the size of drug particles, the polymer to drug ratio, etc. [26]. Hence, a small microsponge size may be obtained by using a drug of small particle size or through using high polymer to drug ratio.…”

Section: Fig 1: Images Of Different Formulations Of Microsponges Takmentioning

confidence: 99%

Preparation of Ascorbic Acid and Cholecalciferol Microsponges for Topical Application

Zia

Nazir

Khan

et al. 2017

Int J Pharm Pharm Sci

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Objective: Apart from having various physiological functions in the body, ascorbic acid (vitamin C) and cholecalciferol (vitamin D3) also have a key role in skin protection. However, their bioavailability is quite limited in the skin, and therefore, many cosmetic products are supplemented with these vitamins, which are usually associated with stability issues. To avoid these issues, here we report on the preparation of microsponges of these vitamins for topical application. Methods:The microsponges were prepared through various emulsification-solvent evaporation methods involving singleThe organic internal phase was consisted of Eudragit ® RS 100 polymer dissolved in an organic solvent such as acetone or dichloromethane, at a constant polymer to drug ratio of 2:1. The prepared microsponges were characterized for their entrapment efficiency, droplet size and uniformity, core to wall interaction, and surface morphology.Results: It was found that the W/O/W and S/O/W are suitable methods for the preparation of vitamin C microsponges and O/W is a suitable method for the preparation of vitamin D3 microsponges; ensuring an encapsulation efficiency of around 56-59% and 93%, respectively. The average diameter of vitamin C and D3 microsponges was typically around 56-68 μm and 48 μm, respectively. Conclusion:It is possible to encapsulate both water and oil soluble vitamins in a microsponge system at an appreciable entrapment efficiency. The findings of the present study are expected to play a vital role in the development of cosmeceuticals.

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“…12,13,29 Protein loadings were set to less than 1 wt% of the final microparticle weight, as shown previously to be ideal for loaded electrospraying particles, in terms of release and protein distribution. 23 Aqueous solutions were prepared, containing SA and PEG, with and without GF and with and without trehalose addition.…”

Section: Particle Fabricationmentioning

confidence: 99%

“…4 By using dry encapsulation, such as in spray-drying or with solid emulsions, the bioactivity of proteins can be improved or maintained. 10,11 Stabilizers can also be used to protect proteins, 12 by increasing the energy barrier between the native and denatured states of protein molecules, for example. 4 Size reduction of protein aggregates (or micronization) with poly(ethylene glycol) (PEG) upon colyophilization 13 can also effectively lead to a more favorable state of the protein, 5,14,15 as seen for nerve growth factor (GF) 16 and albumin, 14 and may also reduce protein adsorption to the polymer matrix.…”

mentioning

confidence: 99%

Growth Factor-Loaded Microparticles for Tissue Engineering: The Discrepancies of In Vitro Characterization Assays

Bock

Dargaville

Kirby

et al. 2016

Tissue Engineering Part C: Methods

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Protein encapsulation into biodegradable microspheres by a novel S/O/W emulsion method using poly(ethylene glycol) as a protein micronization adjuvant

Cited by 141 publications

References 23 publications

Pharmacokinetic and pharmacodynamic profiles of recombinant human erythropoietin-loaded poly(lactic-co-glycolic acid) microspheres in rats

Pharmacokinetic and pharmacodynamic profiles of recombinant human erythropoietin-loaded poly(lactic-co-glycolic acid) microspheres in rats

Preparation of Ascorbic Acid and Cholecalciferol Microsponges for Topical Application

Growth Factor-Loaded Microparticles for Tissue Engineering: The Discrepancies of In Vitro Characterization Assays

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