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. 2022 Feb 20;15(4):1586.
doi: 10.3390/ma15041586.

The Advances and Challenges of Liposome-Assisted Drug Release in the Presence of Serum Albumin Molecules: The Influence of Surrounding pH

Danuta Pentak  1 , Anna Ploch-Jankowska  1 , Andrzej Zięba  2 , Violetta Kozik  3
Affiliations

The Advances and Challenges of Liposome-Assisted Drug Release in the Presence of Serum Albumin Molecules: The Influence of Surrounding pH

Danuta Pentak et al. Materials (Basel). .

Abstract

The aim of this study is to prepare a liposomal delivery system for 5-methyl-12 (H)-quino[3,4-b]-1,4-benzothiazine chloride (5-MBT) and study the in vitro release characteristics. The release of 5-MBT from a liposomal complex with human serum albumin (HSA) [LDPPC/5-MBT]:HSA was examined using the spectrophotometric method and differential scanning calorimetry (DSC). Electronic paramagnetic resonance was used to assess the influence of the pH of the environment on the conformation of phospholipids, the latter determining the degree of release of the encapsulated compound. The applied mathematical models made it possible to determine the necessary analytical parameters to facilitate the process of potential drug release from liposomes. The complexes formed by liposomal 5-MBT with serum albumin (HSA) particles allowed for the description of the Fick process. The change in the polarity of the phospholipid membrane resulting from the changes in the pH of the surroundings, significantly influenced the percentage of 5-MBT entrapment in the liposomes. It also affected the release percentage.

Keywords: biological systems; controlled drug delivery; nanoparticles; release mechanism.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Chloride-5-methyl-12(H)-chino[3,4-b]-1,4-benzothiazine.
Figure 2
Figure 2
Typical EPR spectrum of spin marker 5-DOXYL located in the liposome membrane.
Figure 3
Figure 3
Drug release profiles of chloride-5-methyl-12(H)-chino[3,4-b]-1,4-benzothiazine (5-MBT) loaded in the liposomes obtained in different pH.
Figure 4
Figure 4
Schematic representation of the polar conformation of the phosphatidylcholine group. (A) Conformation with a perpendicular arrangement of the phospholipid heads to the membrane surface, and (B) conformation with a parallel arrangement of the phospholipid heads to the membrane surface.
Figure 5
Figure 5
Effect of the pH and temperature on the polarity and the motion of spin marker 5-DOXYL along the perpendicular to the surface of membrane.
Figure 6
Figure 6
Effect of the temperature on maximum hyperfine splitting 2AII of 5-DOXYL in liposome vesicles.
Figure 7
Figure 7
The release kinetics of 5-MBT from the LDPPC/5-MBT liposomes (A1–C1) and their complexes with HSA [LDPPC/5-MBT]:HSA (A2–C2). (A) pH 4.47, (B) pH 5.59, (C) pH 6.10. Colored lines corresponding to the fits of the mathematical models. Black dot lines corresponding to the experimental data. (-) Korsmeyer–Peppas model; (-) first-order model; (-) Bhaskas model; (-) Higuchi model; (-) Ritger–Peppas model.
Figure 8
Figure 8
Release profile of 5-MBT from the LDPPC/5-MBT liposomes (A,B) and them complexes with albumin [LDPPC/5-MBT]:HSA (C), at 37 °C, at initial time. Error bars represent standard deviation.
Figure 9
Figure 9
The influence of the pH environment on the temperature of LDPPC/5-MBT liposomes phase transitions. (A) pH 4.47; (B) pH 5.59; (C) pH 6.10.
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