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Formulation Study of Chitosan Microparticles Loaded with Lactoferrin

Published on Jan 1, 2014in Journal of Molecular and Genetic Medicine
· DOI :10.4172/1747-0862.1000166
Hiraku Onishi24
Estimated H-index: 24
,
Yoshiharu Machida38
Estimated H-index: 38
+ 1 AuthorsKen-ichi Watanabe1
Estimated H-index: 1
Abstract
Lactoferrin (LF) is known to show various useful biological features such as antimicrobial, antiviral, antitumor and anti-inflammatory effects. However, orally administered LF undergoes enzymatic degradation in the gastrointestinal tract, resulting in extensive decrease of such functions. The purpose of this study is to develop a useful oral delivery system of LF. Also, chitosan (Ch) was adopted as a carrier because it is yielded abundantly and a safe polymer. LF-loaded Ch microparticles were produced by the emulsification-evaporation technique using sorbitan sesquioleate (SO-15) and sorbitan trioleate (SO-30) as surfactants. The resultant LF-loaded Ch microparticles were evaluated from the viewpoints of particle size, shape, drug content and in vitro release in the gastric and intestinal pHs. The selected LF-loaded microparticles (MS4) were coated with an enteric coating polymer, Eudragit L100 (EL-100). The resultant microparticles (E/MS4) were protected from the deformation in the gastric pH, and exhibited fairly appropriate release profiles of LF. Thus, enteric-coated MS4 was suggested to be possibly useful as an orally-taken delivery system of LF.
  • References (34)
  • Citations (1)
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References34
Newest
Introduction: Recently, pharmacotherapy has advanced extensively, but there are still many refractory diseases which cannot be solved fully by existing therapeutic agents. Therefore, alternative medicine and health foods are now attracting much attention, for example, lactoferrin (LF): a multifunctional glycoprotein. As LF is non-toxic and low-cost, its application in healthcare and therapeutics is expected to be widespread. Areas covered: In this review, LF's general basic features are describe...
17 CitationsSource
#1Hiraku Onishi (Hoshi University)H-Index: 24
#2Kennichi Koyama (Hoshi University)H-Index: 1
Last. Yoshiharu Machida (Hoshi University)H-Index: 38
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Background: Although lactoferrin (LF) possesses useful functions such as antitumor, antiviral, and anti-inflammatory acitivities, it is subject to gastric digestion, resulting in the reduction of efficacy. Therefore, it is important to develop a system delivering LF efficiently to intestinal mucosa or gut-associated lymphoid tissue. Method: Chitosan/alginate/calcium complex microparticles containing LF at a high loading were prepared using alginate, LF, and calcium chloride at the ratio of 6:3:8...
20 CitationsSource
#2Adrian Canizalez-Roman (Autonomous University of Sinaloa)H-Index: 17
Last. Jan G. M. Bolscher (UvA: University of Amsterdam)H-Index: 15
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Increased prevalence of antibiotic-resistant bacteria has become a major threat to the health sector worldwide due to their virulence, limited therapeutic options and distribution in both hospital and community settings. Discovery and development of new agents to combat antibiotic-resistant bacteria is thus needed. This study therefore aimed to evaluate the ability of bovine lactoferrin (LF), peptides from two antimicrobial domains lactoferricin B (LFcin17-30) and lactoferrampin (LFampin265-284)...
71 CitationsSource
#1Yasuhiro Nojima (Tokyo University of Technology)H-Index: 4
#2Yosuke Suzuki (Tokyo University of Technology)H-Index: 3
Last. Atsushi Sato (Tokyo University of Technology)H-Index: 7
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Purpose We developed a lactoferrin conjugate by modifying bovine lactoferrin (bLF) with a 40-kDa branched poly(ethylene glycol) (PEG) molecule (designated 40 k-PEG-bLf), and we evaluated its in vitro activities and pharmacokinetic properties.
32 CitationsSource
#1Yasuhiro NojimaH-Index: 4
#2Yosuke SuzukiH-Index: 3
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Lactoferrin (LF) is an iron-binding glycoprotein that possesses multifunctional biological activities. Recent reports from clinical trials suggest that LF is potentially effective as a therapeutic protein against cancer and gangrene. However, pharmaceutical proteins such as LF are unstable in vivo. Therefore, to improve stability, we developed mono-PEGylated bovine LF (20k-PEG-bLf) with branched 20 kDa (2 × 10 kDa) poly(ethylene glycol) (PEG). We examined in vitro activities such as iron binding...
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#1Hiraku Onishi (Hoshi University)H-Index: 24
#2Yoshiharu Machida (Hoshi University)H-Index: 38
Last. Ken-ichi Koyama (Memorial Hospital of South Bend)H-Index: 3
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ABSTRACTIn order to achieve the delivery and controlled release of lactoferrin (LF), a biologically multifunctional protein, chitosan microparticles loaded with LF were prepared. Several types of chitosan microparticles containing LF were prepared by the w/o emulsification-solvent evaporation method, and the particle characteristics and release properties in JP 2nd fluid, pH 6.8, were examined. All kinds of microparticles were obtained at a yield of more than 75% (w/w). LF-loaded microparticles ...
17 CitationsSource
#1Takashi Takeuchi (Tottori University)H-Index: 22
#2Takahiro Jyonotsuka (Tottori University)H-Index: 1
Last. Etsumori Harada (Rakuno Gakuen University)H-Index: 2
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We have previously demonstrated that intestinally infused bovine lactoferrin (bLF) is transported into the blood circulation via the lymphatic pathway, not via the portal circulation. Therefore, in the present study, we further investigated whether intragastrically infused enteric-formulated bLF (EF-bLF) was more efficiently absorbed than bLF from the intestine in adult rats. The rats were randomly divided into three groups: 30 and 300 mg kg−1 non-enteric-formulated bLF (non-EF-bLF) groups and a...
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#1Dominique Legrand (CNRS: Centre national de la recherche scientifique)H-Index: 36
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Last. Joël Mazurier (CNRS: Centre national de la recherche scientifique)H-Index: 42
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The antimicrobial activities of lactoferrin (Lf) depend on its capacity to bind iron and on its direct interaction with the surface of microorganisms. Its protective effect also extends to the regulation of the host response to infections. Depending on the immune status of an individual, Lf can have anti-inflammatory properties that downregulate the immune response and prevent septic shock and damage to tissues. It also acts as a promoter of the activation, differentiation, and (or) proliferatio...
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#1Håvard Jenssen (UBC: University of British Columbia)H-Index: 34
One of the most common viral infections in humans is caused by the herpes simplex virus (HSV). It was first effectively treated in the 1970s with the introduction of acyclovir, which is still the most commonly used treatment. Naturally occurring antimicrobial proteins and peptides have also been shown to possess antiviral activity against HSV. This review will focus on the anti-HSV activity of one such protein, lactoferrin, and a small peptide fragment from its N-terminal domain, lactoferricin. ...
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Mammalian lactoferrin (Lf) receptors are sug- gested to have pivotal roles for mediating multiple func- tions of Lf. In this review, we focus on current knowledge of the structure and function of mammalian Lf receptors, mainly the fi rst cloned Lf receptor that has been shown to be expressed in the infant small intestine at high levels but also in virtually all other tissues. The small intestinal Lf receptor takes up iron from Lf into cells and presumably exerts other physiological functions. Ot...
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Colostrumis can be defined as ‘the early milk which is secreted at the time of parturition’, which works as an immune booster in post-natal health, and additionally is rich in antibodies. It provides passive immunity to the newborn, also called as “foremilk”. Bovine Colostrum (BC) contains high amount of proteins, immunoglobulin, lactoferrin and growth factors which are essential for specific functions. Many studies have suggested that colostrum components like antimicrobial factors, immunoglobu...