Antifungal and Mucoadhesive Properties of an Orally Administered Chitosan-Coated Amphotericin B Nanostructured Lipid Carrier (NLC)

Janet Tan Sui Ling; Clive J. Roberts; Nashiru Billa

doi:10.1208/s12249-019-1346-7

Antifungal and Mucoadhesive Properties of an Orally Administered Chitosan-Coated Amphotericin B Nanostructured Lipid Carrier (NLC)

Janet Tan Sui Ling, Clive J. Roberts, Nashiru Billa

Research output: Contribution to journal › Article › Research › peer-review

29 Citations (Scopus)

Abstract

Surface-modified nanostructured lipid carriers (NLC) represent a promising mode of drug delivery used to enhance retention of drugs at absorption site. Formulated chitosan-coated amphotericin-B-loaded NLC (ChiAmp NLC) had a size of 394.4 ± 6.4 nm, encapsulation and loading efficiencies of 86.0 ± 3% and 11.0 ± 0.1% respectively. Amphotericin-B release from NLCs was biphasic with no changes in physical properties upon exposure to simulated gastrointestinal conditions. Antifungal properties of Amphotericin-B and ChiAmpB NLC were comparable but ChiAmpB NLC was twice less toxic to red blood cells and ten times safer on HT-29 cell lines. In vitro mucoadhesion data were observed ex vivo, where ChiAmpB NLC resulted in higher retention within the small intestine compared to the uncoated formulation. The data strongly offers the possibility of orally administering a non-toxic, yet effective Amphotericin-B nanoformulation for the treatment of systemic fungal infections.

Original language	English
Article number	136
Number of pages	11
Journal	AAPS PharmSciTech
Volume	20
Issue number	3
DOIs	https://doi.org/10.1208/s12249-019-1346-7
Publication status	Published - Apr 2019
Externally published	Yes

Keywords

amphotericin B
antifungal
chitosan
mucoadhesion
toxicity

Access to Document

10.1208/s12249-019-1346-7

Cite this

@article{afb687cb1e8e47349495358257257327,

title = "Antifungal and Mucoadhesive Properties of an Orally Administered Chitosan-Coated Amphotericin B Nanostructured Lipid Carrier (NLC)",

abstract = "Surface-modified nanostructured lipid carriers (NLC) represent a promising mode of drug delivery used to enhance retention of drugs at absorption site. Formulated chitosan-coated amphotericin-B-loaded NLC (ChiAmp NLC) had a size of 394.4 ± 6.4 nm, encapsulation and loading efficiencies of 86.0 ± 3% and 11.0 ± 0.1% respectively. Amphotericin-B release from NLCs was biphasic with no changes in physical properties upon exposure to simulated gastrointestinal conditions. Antifungal properties of Amphotericin-B and ChiAmpB NLC were comparable but ChiAmpB NLC was twice less toxic to red blood cells and ten times safer on HT-29 cell lines. In vitro mucoadhesion data were observed ex vivo, where ChiAmpB NLC resulted in higher retention within the small intestine compared to the uncoated formulation. The data strongly offers the possibility of orally administering a non-toxic, yet effective Amphotericin-B nanoformulation for the treatment of systemic fungal infections.",

keywords = "amphotericin B, antifungal, chitosan, mucoadhesion, toxicity",

author = "Ling, {Janet Tan Sui} and Roberts, {Clive J.} and Nashiru Billa",

note = "Publisher Copyright: {\textcopyright} 2019, American Association of Pharmaceutical Scientists.",

year = "2019",

month = apr,

doi = "10.1208/s12249-019-1346-7",

language = "English",

volume = "20",

journal = "AAPS PharmSciTech",

issn = "1530-9932",

publisher = "Springer",

number = "3",

}

TY - JOUR

T1 - Antifungal and Mucoadhesive Properties of an Orally Administered Chitosan-Coated Amphotericin B Nanostructured Lipid Carrier (NLC)

AU - Ling, Janet Tan Sui

AU - Roberts, Clive J.

AU - Billa, Nashiru

PY - 2019/4

Y1 - 2019/4

N2 - Surface-modified nanostructured lipid carriers (NLC) represent a promising mode of drug delivery used to enhance retention of drugs at absorption site. Formulated chitosan-coated amphotericin-B-loaded NLC (ChiAmp NLC) had a size of 394.4 ± 6.4 nm, encapsulation and loading efficiencies of 86.0 ± 3% and 11.0 ± 0.1% respectively. Amphotericin-B release from NLCs was biphasic with no changes in physical properties upon exposure to simulated gastrointestinal conditions. Antifungal properties of Amphotericin-B and ChiAmpB NLC were comparable but ChiAmpB NLC was twice less toxic to red blood cells and ten times safer on HT-29 cell lines. In vitro mucoadhesion data were observed ex vivo, where ChiAmpB NLC resulted in higher retention within the small intestine compared to the uncoated formulation. The data strongly offers the possibility of orally administering a non-toxic, yet effective Amphotericin-B nanoformulation for the treatment of systemic fungal infections.

AB - Surface-modified nanostructured lipid carriers (NLC) represent a promising mode of drug delivery used to enhance retention of drugs at absorption site. Formulated chitosan-coated amphotericin-B-loaded NLC (ChiAmp NLC) had a size of 394.4 ± 6.4 nm, encapsulation and loading efficiencies of 86.0 ± 3% and 11.0 ± 0.1% respectively. Amphotericin-B release from NLCs was biphasic with no changes in physical properties upon exposure to simulated gastrointestinal conditions. Antifungal properties of Amphotericin-B and ChiAmpB NLC were comparable but ChiAmpB NLC was twice less toxic to red blood cells and ten times safer on HT-29 cell lines. In vitro mucoadhesion data were observed ex vivo, where ChiAmpB NLC resulted in higher retention within the small intestine compared to the uncoated formulation. The data strongly offers the possibility of orally administering a non-toxic, yet effective Amphotericin-B nanoformulation for the treatment of systemic fungal infections.

KW - amphotericin B

KW - antifungal

KW - chitosan

KW - mucoadhesion

KW - toxicity

UR - http://www.scopus.com/inward/record.url?scp=85062585890&partnerID=8YFLogxK

U2 - 10.1208/s12249-019-1346-7

DO - 10.1208/s12249-019-1346-7

M3 - Article

C2 - 30838459

AN - SCOPUS:85062585890

SN - 1530-9932

VL - 20

JO - AAPS PharmSciTech

JF - AAPS PharmSciTech

IS - 3

M1 - 136

ER -

Antifungal and Mucoadhesive Properties of an Orally Administered Chitosan-Coated Amphotericin B Nanostructured Lipid Carrier (NLC)

Abstract

Keywords

Access to Document

Other files and links

Cite this