Characteristics and Bioactivities of Carrageenan/Chitosan Microparticles Loading Α-mangostin

doi:10.21203/rs.3.rs-457618/v1

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Characteristics and Bioactivities of Carrageenan/Chitosan Microparticles Loading Α-mangostin

https://doi.org/10.21203/rs.3.rs-457618/v1

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published 05 Jul, 2021

Read the published version in Journal of Polymers and the Environment →

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This study attempted to develop carrageenan/chitosan based microparticles loading α-mangostin which was extracted from Vietnamese mangosteen skin. The carrageenan/chitosan/α-mangostin microparticles were prepared by ionic gelation method by mixing chitosan, carrageenan with α-mangostin and subsequently cross-linking the mixtures with sodium tripolyphosphate crosslinking agent. The content of α-mangostin in microparticles was changed to evaluate the effect of α-mangostin content on physical, morphological properties, particles size and bioactivities of the carrageenan/chitosan/α-mangostin microparticles. The obtained results showed that carrageenan, chitosan was interacted together and with α-mangostin. The presence of polymers matrix improved the release ability of α-mangostin into ethanol/pH buffer solutions. The carrageenan/chitosan/ α-mangostin microparticles have antibacterial (gram (+) strains) and anti-oxidant activities. The results suggested that combination of chitosan and carrageenan in the microparticles can enhance the control release of α-mangostin into solutions as well as keep the bioactivities of α-mangostin.

Polymer Science

Environmental Policy

α-Mangostin

carrageenan/chitosan drug delivery

solubility

anti-oxidant

antimicrobial activity

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Table I. Component ratio and designation of carrageenan/chitosan/MGS samples

No.	Chitosan (mg)	Carrageenan (mg)	MGS (mg)	STPP (mg)	KCl (mg)	Designation
1	100	50	0	0.5	20	CCG0
2	100	50	7.5	0.5	20	CCG5
3	100	50	15	0.5	20	CCG10
4	100	50	22.5	0.5	20	CCG15
5	100	50	30	0.5	20	CCG20

Table II. Average particle size of CCG microparticles

Sample	Size range (nm)	Peak size (nm)	Z-average particle size (nm)	PDI
CCG0	295-712	482.7 ± 35.40	1282.0	0.411
CCG5	164 - 295	228 ± 8.78	437.7	0.406
CCG10	43 - 91 141 - 295	61.33 ± 4.09 (14.8) 232.1 ± 18.71 (85.2)	595.1	0.588
CCG15	246 - 356	267.3 ± 13.25	641.6	0.513
CCG20	91 - 295 396 - 1106	166.7 ± 18.35 (34.8) 730.8 ± 78.95 (65.2)	756.8	0.632

Table III. DSC parameters of CCG microparticles

Sample	Melting temperature (^oC)	Heat flow at melting point (mW/mg)	Melting enthalpy (J/g)
MGS	172.8	2.26	90.33
CCG0	90.8	2.427	396.7
CCG10	88.1	3.612	238.7
CCG20	95.8	2.738	284.4

Table IV. Comparison of several release kinetic models for CCG microparticles

Kinetic model	Stage	R² of kinetic models
		MGS	CCG5	CCG10	CCG15	CCG20
		Ethanol/pH 1.2 buffer solution
ZO	Fast release (first 120 min of testing)	0.8409	0.5588	0.9455	0.7368	0.8633
FO		0.4791	0.2278	0.9125	0.5706	0.7911
HG		0.8780	0.6799	0.9815	0.8339	0.9327
HC		0.2773	0.5588	0.9455	0.7368	0.8633
KMP		0.9751	0.9108	0.9903	0.8056	0.9362
n		0.5243	0.7644	0.2814	0.6051	0.2920
ZO	Slow release (following time)	0.6785	0.6761	0.9899	0.6356	0.9923
FO		0.9920	0.9523	0.9996	0.9507	0.9814
HG		0.6367	0.7989	0.9949	0.6079	0.9862
HC		0.6785	0.7613	0.9899	0.6356	0.9923
KMP		0.5943	0.8332	0.9981	0.5736	0.9758
n		0.7094	0.7513	0.6979	0.6820	0.3831
		Ethanol/pH 4.5 buffer solution
ZO	Fast release (first 120 min of testing)	0.9356	0.6506	0.6973	0.9698	0.5146
FO		0.8610	0.6613	0.8959	0.7349	0.4624
HG		0.9799	0.7885	0.7164	0.8001	0.7277
HC		0.2943	0.5271	0.5535	0.6549	0.4729
KMP		0.9887	0.8262	0.4360	0.5723	0.7685
n		0.1040	0.2743	0.6276	0.6275	0.2038
ZO	Slow release (following time)	0.9200	0.9661	0.9071	0.9812	0.9527
FO		0.7175	0.2650	0.4723	0.6242	0.9617
HG		0.8978	0.9776	0.8771	0.9832	0.9287
HC		0.9200	0.4966	0.9071	0.9812	0.9527
KMP		0.8764	0.9833	0.8484	0.9805	0.9023
n		0.4485	0.5009	0.3775	0.3130	0.2913
		Ethanol/pH 6.8 buffer solution
ZO	Fast release (first 120 min of testing)	0.5919	0.5919	0.7570	0.7746	0.7091
FO		0.5369	0.5369	0.7242	0.9010	0.6680
HG		0.4273	0.4273	0.7197	0.7316	0.7277
HC		0.3470	0.3470	0.6355	0.6164	0.4729
KMP		0.8167	0.8167	0.8800	0.8776	0.8796
n		0.1250	0.1250	0.1873	0.1855	0.2194
ZO	Slow release (following time)	0.9919	0.9919	0.9730	0.9230	0.8219
FO		0.9852	0.9852	0.8914	0.9646	0.3985
HG		0.9958	0.9958	0.9561	0.9384	0.7833
HC		0.9919	0.9919	0.9730	0.9230	0.8219
KMP		0.9953	0.9953	0.9382	0.9507	0.7411
n		0.2922	0.2922	0.5155	0.6683	0.3478
		Ethanol/pH 7.4 buffer solution
ZO	Fast release (first 120 min of testing)	0.6948	0.7985	0.7889	0.6944	0.6188
FO		0.5690	0.7508	0.7281	0.3988	0.4423
HG		0.5450	0.8069	0.7889	0.7794	0.7278
HC		0.6700	0.5198	0.5715	0.5781	0.8439
KMP		0.8851	0.9519	0.9739	0.8708	0.9381
n		0.1864	0.1766	0.3514	0.2510	0.2113
ZO	Slow release (following time)	0.4736	0.8205	0.9341	0.7627	0.9816
FO		0.9459	0.9852	0.4559	0.119	0.9945
HG		0.4598	0.7949	0.9403	0.8039	0.6151
HC		0.4736	0.8205	0.9341	0.7627	0.5679
KMP		0.4432	0.7633	0.9414	0.8409	0.9481
n		0.4712	0.4851	0.3845	0.2563	0.4049

n is diffusion constant obtained from KMP model

Table V. Antimicrobial activity of MGS and CCG microparticles

Sample	Value (µg/mL)	Inhibitory percentage
		Gram (+)			Gram (-)			Yeast
		Staphylococcus aureus	Bacillus subtilis	Lactobacillus fermentum	Salmonella enterica	Escherichia coli	Pseudomonas aeruginosa	Candida albicans
CCG5	128	100	100	100	0	0	0	0
	32	40	0	5	0	0	0	0
	8	0	0	0	0	0	0	0
	2	0	0	0	0	0	0	0
	IC₅₀	48.00	80.00	77.47	>128	>128	>128	>128
	MIC	128	128	128	>128	>128	>128	>128
CCG 10	128	100	100	100	0	0	0	0
	32	100	50	0	0	0	0	0
	8	30	0	0	0	0	0	0
	2	0	0	0	0	0	0	0
	IC₅₀	14.86	32.00	80.0	>128	>128	>128	>128
	MIC	32	128	128	>128	>128	>128	>128
CCG 15	128	100	100	95	0	0	0	0
	32	95	100	0	0	0	0	0
	8	0	0	0	0	0	0	0
	2	0	0	0	0	0	0	0
	IC₅₀	20.63	20.00	82.53	>128	>128	>128	>128
	MIC	128	32	>128	>128	>128	>128	>128
CCG 20	128	100	100	98	0	0	0	0
	32	92	74	0	0	0	0	0
	8	10	25	0	0	0	0	0
	2	0	0	0	0	0	0	0
	IC₅₀	19.71	20.25	80.98	>128	>128	>128	>128
	MIC	128	128	>128	>128	>128	>128	>128
MGS	256	100	100	100	0	10	20	0
	64	100	100	100	0	0	0	0
	16	100	100	100	0	0	0	0
	4	100	100	100	0	0	0	0
	1	55	40	0	-	-	-	-
	0.33	20	0	0	-	-	-	-
	IC₅₀	0.89	1.5	2.5	>256	>256	>256	>256
	MIC	4	4	4	>256	>256	>256	>256

Table VI. Anti-oxidant activity of MGS and CCG microparticles

Sample	Scavenging capacity (SC, %)	SC₅₀ (mg/mL)
Control (+) [Ascorbic acid]	86.53 ± 0.3	0.0126
Control (-) [DPPH/EtOH+ DMSO]	0.0 ± 0.0	-
CCG5	14.55 ± 0.0	>5
CCG 10	15.45 ± 0.5	4.87
CCG 15	19.59 ± 0.4	4.51
CCG 20	20.99 ± 0.6	4.35
MGS	76.89 ± 0.8	0.49

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Journal Publication

published 05 Jul, 2021

Read the published version in Journal of Polymers and the Environment →

Editorial decision: Major Revisions Needed
03 Jun, 2021
Reviews received at journal
11 May, 2021
Editor assigned by journal
26 Apr, 2021
First submitted to journal
22 Apr, 2021

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Characteristics and Bioactivities of Carrageenan/Chitosan Microparticles Loading Α-mangostin

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