Magnetically responsive polymeric microparticles for oral delivery of protein drugs

Jianjun Cheng, Benjamin A. Teply, Seok Yoon Jeong, Christopher H. Yim, Dennis Ho, Ines Sherifi, Sangyong Jon, Omid C. Farokhzad, Ali Khademhosseini, Robert S. Langer

Research output: Contribution to journalArticle

100 Citations (Scopus)

Abstract

Purpose. Protein drugs cannot be delivered efficiently through oral routes. To address this challenge, we evaluated the effect of prolonged gastrointestinal transit on the bioavailability of insulin carried by magnetically responsive microparticles in the presence of an external magnetic field. Methods. Magnetite nanocrystals and insulin were coencapsulated into poly(lactide-co-glycolide) (PLGA) microparticles and their effects on hypoglycemia were evaluated in mice in the presence of a circumferentially applied external magnetic field. Results. A single administration of 100 U/kg of insulin-magnetite-PLGA microparticles to fasted mice resulted in a reduction of blood glucose levels of up to 43.8% in the presence of an external magnetic field for 20 h (bioavailability = 2.77 ± 0.46 and 0.87 ± 0.29% based on glucose and ELISA assay, respectively), significantly higher than similarly dosed mice without a magnetic field (bioavailability = 0.66 ± 0.56 and 0.30 ± 0.06%, based on glucose and ELISA assay, respectively). Conclusions. A substantially improved hypoglycemic effect was observed in mice that were orally administered with insulin-magnetite-PLGA microparticles in the presence of an external magnetic field, suggesting that magnetic force can be used to improve the efficiency of orally delivered protein therapeutics.

Original languageEnglish (US)
Pages (from-to)557-564
Number of pages8
JournalPharmaceutical Research
Volume23
Issue number3
DOIs
StatePublished - Mar 1 2006

Fingerprint

Magnetic Fields
Ferrosoferric Oxide
Magnetic fields
Insulin
Biological Availability
Pharmaceutical Preparations
Proteins
Assays
Enzyme-Linked Immunosorbent Assay
Gastrointestinal Transit
Polyglactin 910
Glucose
Hypoglycemia
Hypoglycemic Agents
Nanoparticles
Nanocrystals
Blood Glucose
polylactic acid-polyglycolic acid copolymer

Keywords

  • Insulin
  • Magnetic particles
  • Microparticles
  • Oral delivery
  • Protein drugs

ASJC Scopus subject areas

  • Biotechnology
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry
  • Pharmacology (medical)

Cite this

Magnetically responsive polymeric microparticles for oral delivery of protein drugs. / Cheng, Jianjun; Teply, Benjamin A.; Jeong, Seok Yoon; Yim, Christopher H.; Ho, Dennis; Sherifi, Ines; Jon, Sangyong; Farokhzad, Omid C.; Khademhosseini, Ali; Langer, Robert S.

In: Pharmaceutical Research, Vol. 23, No. 3, 01.03.2006, p. 557-564.

Research output: Contribution to journalArticle

Cheng, J, Teply, BA, Jeong, SY, Yim, CH, Ho, D, Sherifi, I, Jon, S, Farokhzad, OC, Khademhosseini, A & Langer, RS 2006, 'Magnetically responsive polymeric microparticles for oral delivery of protein drugs', Pharmaceutical Research, vol. 23, no. 3, pp. 557-564. https://doi.org/10.1007/s11095-005-9444-5
Cheng, Jianjun ; Teply, Benjamin A. ; Jeong, Seok Yoon ; Yim, Christopher H. ; Ho, Dennis ; Sherifi, Ines ; Jon, Sangyong ; Farokhzad, Omid C. ; Khademhosseini, Ali ; Langer, Robert S. / Magnetically responsive polymeric microparticles for oral delivery of protein drugs. In: Pharmaceutical Research. 2006 ; Vol. 23, No. 3. pp. 557-564.
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abstract = "Purpose. Protein drugs cannot be delivered efficiently through oral routes. To address this challenge, we evaluated the effect of prolonged gastrointestinal transit on the bioavailability of insulin carried by magnetically responsive microparticles in the presence of an external magnetic field. Methods. Magnetite nanocrystals and insulin were coencapsulated into poly(lactide-co-glycolide) (PLGA) microparticles and their effects on hypoglycemia were evaluated in mice in the presence of a circumferentially applied external magnetic field. Results. A single administration of 100 U/kg of insulin-magnetite-PLGA microparticles to fasted mice resulted in a reduction of blood glucose levels of up to 43.8{\%} in the presence of an external magnetic field for 20 h (bioavailability = 2.77 ± 0.46 and 0.87 ± 0.29{\%} based on glucose and ELISA assay, respectively), significantly higher than similarly dosed mice without a magnetic field (bioavailability = 0.66 ± 0.56 and 0.30 ± 0.06{\%}, based on glucose and ELISA assay, respectively). Conclusions. A substantially improved hypoglycemic effect was observed in mice that were orally administered with insulin-magnetite-PLGA microparticles in the presence of an external magnetic field, suggesting that magnetic force can be used to improve the efficiency of orally delivered protein therapeutics.",
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AU - Sherifi, Ines

AU - Jon, Sangyong

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