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Development of Microspheres Based on Thiol-Modified Sodium Alginate for Intestinal-Targeted Drug Delivery
journal contribution
posted on 2019-11-21, 14:03 authored by Xinyan Mao, Xinying Li, Wenjie Zhang, Lun Yuan, Lei Deng, Liming Ge, Changdao Mu, Defu LiBioactive peptide drugs are mostly delivered by parenteral
administration,
which brings great pain and risks to patients. Oral administration
is an acceptable alternative form. However, peptide drugs are extremely
sensitive to the strong acidic environment in the stomach after oral
administration. They would be degraded by pepsin and trypsin in the
gastrointestinal tract. Herein, we present microspheres for intestinal-targeted
peptides drug delivery through oral administration. Sodium alginate
was reacted with l-cysteine to bring it into thiol groups.
Then sodium alginate-l-cysteine conjugates were mixed with
native sodium alginate and emulsified by an improved method. Ca2+ was used to fix the emulsion to get the microspheres. Bovine
serum albumin was used as the simulating drug to assess the feasibility
of microspheres as intestinal delivery carriers. The results showed
that the microspheres exhibited spherical properties and narrow size
distribution. The drug-loading capacity of microspheres was not compromised
after thiol-modification. It is interesting that the microspheres
can maintain structural integrity and hold drugs in the strong acidic
environment in the stomach. Conversely, the microspheres presented
sustained intestinal-targeted drugs release ability as expected. Moreover,
thiol-modification further improved the adherence ability of microspheres
on the inner walls of the small intestine, which is good for enhancing
drug permeability. In sum, the microspheres based on thiol-modified
sodium alginate have promising applications as intestinal-targeted
macromolecular drug carriers.
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thiol-modified sodium alginatemicrosphereintestinal-targeted peptides drug deliveryadministrationIntestinal-Targeted Drug Delivery Bioactive peptide drugsBovine serum albuminThiol-Modified Sodium Alginateintestinal-targeted drugs release abilityacidic environmentsodium alginate-l-cysteine conjugates
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