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. 2024 Nov 13;10(23):e40374.
doi: 10.1016/j.heliyon.2024.e40374. eCollection 2024 Dec 15.

Development and characterization of gastro-floating sustained-release granules for enhanced bioavailability of patchouli oil

Chen Liu  1   2 , Yanan Wu  2 , Yeli Zou  2 , Jiao Wang  3 , Boli Li  2 , Yanni Ma  1 , Xia Zhang  2 , Wenping Wang  3
Affiliations

Development and characterization of gastro-floating sustained-release granules for enhanced bioavailability of patchouli oil

Chen Liu et al. Heliyon. .

Abstract

Patchouli oil (PO), extracted from Pogostemon cablin Benth., a prominent aromatic plant of the Lamiaceae family, has shown considerable protective effects against gastrointestinal infections, particularly those induced by Helicobacter pylori. This study aimed to develop a gastro-floating multi-unit system for PO to enhance its gastric retention and oral bioavailability.

Methods: The oil-laden granules were prepared using colloidal silicon dioxide (CSD) for oil adsorption and to provide buoyancy, along with ethyl cellulose (EC) and hydroxypropyl methyl cellulose (HPMC) to form a sustained-release matrix. The CSD exhibited favorable characteristics for oil adsorption and floating. Compatibility between PO and CSD was affirmed through DSC thermograms and FTIR spectra. The obtained granules demonstrated a sustained release profile, achieving over 90 % release within 10 h without an initial burst. After oral administration, the granules were observed to remain in the gastric region of rats for over 7 h. The bioavailability of patchouli alcohol from the optimized granules was significantly higher than that from of the PO-loaded powders. The gastro-floating sustained-release granules, based on a CSD/EC/HPMC matrix, offer a simple yet effective strategy to improve the delivery efficacy of PO against Helicobacter pylori infections in the gastric region.

Keywords: Adsorption; Bioavailability; Colloidal silicon dioxide; Gastroretentive granules; Patchouli oil; Sustained release.

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Conflict of interest statement

The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Figures

Fig. 1
Fig. 1
Appearance of different adsorbents before (upper) and after (lower) mixed with Patchouli Oil.
Fig. 2
Fig. 2
In vitro floating performance of oil-loaded powders (A,B) and granules (C,D) of MCC (A,C) or CSD (B,D).
Fig. 3
Fig. 3
DSC thermograms (A) and FTIR spectra (B) of (a) patchouli oil, (b) CSD and (c) their mixture.
Fig. 4
Fig. 4
In vitro drug release profiles of MCC powder and gastro floating CSD granules loaded with patchouli oil (n = 3).
Fig. 5
Fig. 5
Appearance of rat stomach before (A) and after (B) gastric dissection after oral administration for 7 h.
Fig. 6
Fig. 6
Radiographic images of BaSO4-loaded granules in rat stomach before (fasting state) and after oral administration.
Fig. 7
Fig. 7
Plasma concentration-time curves of patchouli alcohol(A) and patchouli ketone(B) in SD rats after oral administration (mean ± S.D, n = 6).
See this image and copyright information in PMC

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