Preparation of a stable amiodarone hydrochloride formulation using various nanotechnology methods and pharmaceutical studies

Xinyu You; Xianghua Gao; Bingbing Wu; Rongqiang Li; Luoting Yu; Qijie Xu

doi:10.2478/pjct-2026-0006

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Preparation of a stable amiodarone hydrochloride formulation using various nanotechnology methods and pharmaceutical studies

Green Sciences

Volume 28 (2026): Issue 1 (March 2026)

By: Xinyu You, Xianghua Gao, Bingbing Wu, Rongqiang Li, Luoting Yu and Qijie Xu

Open Access

|Jun 2026

Figures & Tables

Chemical structure of amiodarone hydrochloride.

TEM images of the wet-milling nanosuspension (a) and the EPAS nanosuspension (b).

DSC spectra of (a) physical mixture (PM) powder, (b) the NS-A powders, (c) NS-B powders, and (d) AD.

XRPD spectra of (a) NS-B, (b) NS-A, and (c) AD powders.

Dissolution profiles for raw AD (AD), physical mixture of AD (PM), the EPAS dried powder (NS-A) and wet-milling dried powder (NS-B) at 37°C and 100 rpm (n = 3).

Plasma concentration-time profiles of AD after intravenous AD coarse suspension (20 mg/kg), oral nanosuspension and AD coarse suspension administrations of 50 mg/kg in the rats. Two different oral formulations were tested: nanosuspension and coarse suspension. Data are expressed as mean ± SD (n = 6).

Cytotoxicity of normal saline, NS-A, and NS-B without AD, at different concentrations to HEK293 (a) and CT26 (b) cells was measured by MTT assay. Cells were treated with normal saline, NS-A, and NS-B without AD for 3 days. Each column represented the mean ± SD for three independent experiments (*p < 0.05, **p < 0.01 vs. control). Cytotoxicity of PM, NS-A, and NS-B at different concentrations to HEK293 (c) and CT26 (d) cells was measured by MTT assay. Cells were treated with PM, NS-A, or NS-B for 3 days. Each column represented the mean ± SD for three independent experiments (*p < 0.05, **p < 0.01 vs. control).

Pharmacokinetic parameters in three groups: coarse suspension of oral AD (50 mg/kg), nanosuspension of oral AD (50 mg/kg), and intravenous AD (20 mg/kg)

Parameter	Intravenous	Coarse suspensions	NS-A	NS-B
Dose (mg/kg)	20	50	50	50
C _max (μg/mL)	3.503 ± 0.329	1.217 ± 0.225	1.873 ± 0.31**	2.049 ± 0.29**
T _max (h)	—	12 ± 0	8 ± 0.765*	8 ± 1.155*
AUC_0–∞ (μg h/mL)	37.446 ± 7.076	31.19 ± 4.594	60.59 ± 3.375*	70.304 ± 4.563*
T _1/2 (h)	23.20 ± 9.867	11.98 ± 0.11	18.98 ± 2.15*	20.013 ± 3.25*
F _r	—	33.31%	64.72%	75.91%

Effect of the ratio of steric stabilizers to drug, the ratio of electrostatic stabilizers to drug, milling time, and milling speed on mean particle size d (90) and PDI

Run	Ration of steric stabilizers to drug (mg)	Ration of electrostatic stabilizers to drug (mg)	Milling time (h)	Milling speed (Hz)	MPS d (90) nm	PDI
1	300	150	8	30	279.1	0.317
2	300	80	8	30	215.3	0.221
3	300	50	8	30	221.9	0.298
4	300	80	6	30	228.0	0.271
5	300	80	12	30	205.6	0.214
6	350	80	8	30	246.4	0.230
7	400	80	8	30	288.7	0.252
8	300	80	8	35	210.1	0.197
9	300	80	8	40	195.7	0.248
10	300	80	6	35	204.5	0.217
11	350	80	6	35	224.9	0.247
12	350	80	8	35	212.4	0.235
13	400	80	8	35	237.1	0.217
14	400	50	8	35	255.3	0.240
15	400	150	8	35	287.0	0.371
16	350	150	8	35	321.9	0.298
17	300	150	8	35	390.7	0.383
18	300	50	8	35	226.7	0.224
19	350	50	8	35	217.0	0.222
20	350	50	8	40	195.4	0.256
21	350	50	12	40	189.6	0.247
22	350	80	12	40	225.3	0.295
23	350	80	8	40	243.4	0.276
24	350	150	8	40	289.5	0.354
25	300	150	8	40	274.5	0.342

The stability of the EPAS dried powder (NS-A)

Time month	Physical appearance	Colour change	MPS d (90) nm	PDI
0 month	Homogenous	No change	226 ± 0.32	0.223 ± 0.005
1 month	Homogenous	No change	233 ± 0.86	0.237 ± 0.008
2 month	Homogenous	No change	252 ± 1.12	0.248 ± 0.014
3 month	Homogenous	No change	259 ± 1.35	0.265 ± 0.017

Composition of AD nanosuspensions by the EPAS method

Formulation	AD (mg)	PF-127 (mg)	PEG-6000 (mg)	PVPK30 (mg)	SDS (mg)	T-80 (mg)	Ethanol (mL)
1	100	0	0	50	20	0	10
2	100	0	0	50	0	0	10
3	100	0	0	0	50	0	10
4	100	0	0	0	20	0	8
5	100	0	0	50	10	0	10
6	100	50	0	0	0	0	8
7	100	50	0	0	10	0	10
8	100	50	0	0	20	0	8
9	100	80	0	0	0	0	10
10	100	80	0	0	10	0	10
11	100	0	0	50	0	10	8
12	100	0	0	0	0	80	10
13	100	0	50	0	10	0	10
14	100	0	50	0	0	0	10
15	100	50	0	0	10	0	10
16	100	50	0	0	15	0	10
17	100	50	0	0	10	0	8
18	100	50	0	20	20	0	10
19	100	50	0	0	10	0	8
20	100	50	0	0	10	0	8
21	100	0	0	0	0	0	10

The stability of the wet-milling dried powder (NS-B)

Time month	Physical appearance	Colour change	MPS d (90) nm	PDI
0 month	Homogenous	No change	205 ± 0.57	0.217 ± 0.004
1 month	Homogenous	No change	223 ± 1.07	0.235 ± 0.008
2 month	Homogenous	No change	235 ± 1.31	0.257 ± 0.016
3 month	Homogenous	No change	255 ± 1.62	0.268 ± 0.018

References

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DOI: https://doi.org/10.2478/pjct-2026-0006 | Journal eISSN: 3072-0389 | Journal ISSN: 1509-8117

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Language: English

Page range: 88 - 101

Submitted on: Jul 24, 2025

Accepted on: May 11, 2026

Published on: Jun 12, 2026

Published by: West Pomeranian University of Technology, Szczecin

In partnership with: Paradigm Publishing Services

Publication frequency: Volume open

Keywords:

Amiodarone hydrochloride,

Evaporative precipitation into aqueous solution,

Pharmacokinetic studies,

Nanosuspensions,

Wet-milling

Related subjects:

Industrial chemistry,

Biotechnology,

Chemical engineering,

Process engineering

© 2026 Xinyu You, Xianghua Gao, Bingbing Wu, Rongqiang Li, Luoting Yu, Qijie Xu, published by West Pomeranian University of Technology, Szczecin
This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 License.

Volume 28 (2026): Issue 1 (March 2026)

Preparation of a stable amiodarone hydrochloride formulation using various nanotechnology methods and pharmaceutical studies

Figures & Tables

Figure 1

Figure 2

Figure 3

Figure 4

Figure 5

Figure 6

Figure 7

Pharmacokinetic parameters in three groups: coarse suspension of oral AD (50 mg/kg), nanosuspension of oral AD (50 mg/kg), and intravenous AD (20 mg/kg)

Effect of the ratio of steric stabilizers to drug, the ratio of electrostatic stabilizers to drug, milling time, and milling speed on mean particle size d (90) and PDI

The stability of the EPAS dried powder (NS-A)

Composition of AD nanosuspensions by the EPAS method

The stability of the wet-milling dried powder (NS-B)

Paradigm

My account

Formulation	AD (mg)	PF-127 (mg)	PEG-6000 (mg)	PVPK30 (mg)	SDS (mg)	T-80 (mg)	Ethanol (mL)
1	100	0	0	50	20	0	10
2	100	0	0	50	0	0	10
3	100	0	0	0	50	0	10
4	100	0	0	0	20	0	8
5	100	0	0	50	10	0	10
6	100	50	0	0	0	0	8
7	100	50	0	0	10	0	10
8	100	50	0	0	20	0	8
9	100	80	0	0	0	0	10
10	100	80	0	0	10	0	10
11	100	0	0	50	0	10	8
12	100	0	0	0	0	80	10
13	100	0	50	0	10	0	10
14	100	0	50	0	0	0	10
15	100	50	0	0	10	0	10
16	100	50	0	0	15	0	10
17	100	50	0	0	10	0	8
18	100	50	0	20	20	0	10
19	100	50	0	0	10	0	8
20	100	50	0	0	10	0	8
21	100	0	0	0	0	0	10

Formulation	AD (mg)	PF-127 (mg)	PEG-6000 (mg)	PVPK30 (mg)	SDS (mg)	T-80 (mg)	Ethanol (mL)
1	100	0	0	50	20	0	10
2	100	0	0	50	0	0	10
3	100	0	0	0	50	0	10
4	100	0	0	0	20	0	8
5	100	0	0	50	10	0	10
6	100	50	0	0	0	0	8
7	100	50	0	0	10	0	10
8	100	50	0	0	20	0	8
9	100	80	0	0	0	0	10
10	100	80	0	0	10	0	10
11	100	0	0	50	0	10	8
12	100	0	0	0	0	80	10
13	100	0	50	0	10	0	10
14	100	0	50	0	0	0	10
15	100	50	0	0	10	0	10
16	100	50	0	0	15	0	10
17	100	50	0	0	10	0	8
18	100	50	0	20	20	0	10
19	100	50	0	0	10	0	8
20	100	50	0	0	10	0	8
21	100	0	0	0	0	0	10

Formulation	AD (mg)	PF-127 (mg)	PEG-6000 (mg)	PVPK30 (mg)	SDS (mg)	T-80 (mg)	Ethanol (mL)
1	100	0	0	50	20	0	10
2	100	0	0	50	0	0	10
3	100	0	0	0	50	0	10
4	100	0	0	0	20	0	8
5	100	0	0	50	10	0	10
6	100	50	0	0	0	0	8
7	100	50	0	0	10	0	10
8	100	50	0	0	20	0	8
9	100	80	0	0	0	0	10
10	100	80	0	0	10	0	10
11	100	0	0	50	0	10	8
12	100	0	0	0	0	80	10
13	100	0	50	0	10	0	10
14	100	0	50	0	0	0	10
15	100	50	0	0	10	0	10
16	100	50	0	0	15	0	10
17	100	50	0	0	10	0	8
18	100	50	0	20	20	0	10
19	100	50	0	0	10	0	8
20	100	50	0	0	10	0	8
21	100	0	0	0	0	0	10