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. 2019 Spring;18(2):556-568.
doi: 10.22037/ijpr.2019.1100651.

Preparation of Ethyl Cellulose Microspheres for Sustained Release of Sodium Bicarbonate

Jia-Hui Wu  1 , Xiao-Juan Wang  1 , Shu-Juan Li  1 , Xiao-Ying Ying  1 , Jing-Bo Hu  1 , Xiao-Ling Xu  1 , Xu-Qi Kang  1 , Jian You  1 , Yong-Zhong Du  1
Affiliations

Preparation of Ethyl Cellulose Microspheres for Sustained Release of Sodium Bicarbonate

Jia-Hui Wu et al. Iran J Pharm Res. 2019 Spring.

Abstract

Sustained release of thermal-instable and water-soluble drugs with low molecule weight is a challenge. In this study, sodium bicarbonate was encapsulated in ethyl cellulose microspheres by a novel solid-in-oil-in-oil (S/O/O) emulsification method using acetonitrile/soybean oil as new solvent pairs. Properties of the microspheres such as size, recovery rate, morphology, drug content, and drug release behavior were evaluated to investigate the suitable preparation techniques. In the case of that the ratio of the internal and external oil phase was 1: 9, Tween 80 as a stabilizer resulted in the highest drug content (2.68%) and a good spherical shape of microspheres. After the ratio increased to 1: 4, the microspheres using Tween 80 as the stabilizer also had high drug content (1.96%) and exhibited a sustained release behavior, with 70% of drug released within 12 h and a sustained release of more than 40 h. Otherwise, different emulsification temperatures at which acetonitrile was evaporated could influence the drug release behaviour of microspheres obtained. This novel method is a potential and effective method to achieve the encapsulation and the sustained release of thermal-instable and water-soluble drugs with low molecule weight.

Keywords: Encapsulation; Microspheres; Sodium bicarbonate; Stabilizer; Sustained release.

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Figures

Figure 1
Figure 1
(A) SEM images of particles of sodium bicarbonate centrifuged from the corresponding nanosuspensions. (B) Number average particle size of sodium bicarbonate nanosuspensions
Figure 2
Figure 2
Size distribution of nanosuspensions of sodium bicarbonate (mean ± SD, n = 3)
Figure 3
Figure 3
(A) SEM images and (B) number average particle size of M1 to M6
Figure 4
Figure 4
In-vitro release of M1 to M6 (mean ± SD, n = 3). **P < 0.01 indicated the accumulative release of M1 compared with that of other groups (M2 to M6) at 48 h
Figure 5
Figure 5
(A) SEM images and (B) number average particle size of M7 to M10
Figure 6
Figure 6
In-vitro release of M7 to M10 (mean ± SD, n = 3). **P < 0.01 indicated the accumulative release of M7 compared with that of other groups (M8 to M10) at 48 h
Figure 7
Figure 7
(A) SEM images and (B) number average particle size of M4, M11, M12 and M13
Figure 8
Figure 8
In-vitro release of M4, M11, M12 and M13 (mean ± SD, n = 3)
See this image and copyright information in PMC

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