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Open AccessArticle

Encapsulation of Black Seed Oil in Alginate Beads as a pH-Sensitive Carrier for Intestine-Targeted Drug Delivery: In Vitro, In Vivo and Ex Vivo Study

1
Advanced Drug Delivery Laboratory, Department of Pharmaceutical Technology, Faculty of Pharmacy, International Islamic University Malaysia, Kuantan 25200, Malaysia
2
Dentistry College, Al-Kitab University, Kirkuk 36010, Iraq
3
Department of Pharmaceutics, SPPSPTM, SVKM’s NMIMS (Deemed to be University), Mumbai 400056, India
4
Naib Canselor, PICOMS International University College, Batu Muda, Batu Caves, Kuala Lumpur 68100, Malaysia
5
Department of Pharmaceutics, Faculty of Pharmacy, Sinai University, Arish 16020, Egypt
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2020, 12(3), 219; https://doi.org/10.3390/pharmaceutics12030219
Received: 27 January 2020 / Revised: 23 February 2020 / Accepted: 24 February 2020 / Published: 2 March 2020
(This article belongs to the Special Issue Natural Products in Drug Delivery Systems )
Black seed oil (BSO) has been used for various therapeutic purposes around the world since ancient eras. It is one of the most prominent oils used in nutraceutical formulations and daily consumption for its significant therapeutic value is common phenomena. The main aim of this study was to develop alginate-BSO beads as a controlled release system designed to control drug release in the gastrointestinal tract (GIT). Electrospray technology facilitates formulation of small and uniform beads with higher diffusion and swelling rates resulting in process performance improvement. The effect of different formulation and process variables was evaluated on the internal and external bead morphology, size, shape, encapsulation efficiency, swelling rate, in vitro drug release, release mechanism, ex vivo mucoadhesive strength and gastrointestinal tract qualitative and quantitative distribution. All the formulated beads showed small sizes of 0.58 ± 0.01 mm (F8) and spherical shape of 0.03 ± 0.00 mm. The coefficient of weight variation (%) ranged from 1.37 (F8) to 3.93 (F5) ng. All formulations (F1–F9) were studied in vitro for release characteristics and swelling behaviour, then the release data were fitted to various equations to determine the exponent (ns), swelling kinetic constant (ks), swelling rate (%/h), correlation coefficient (r2) and release kinetic mechanism. The oil encapsulation efficiency was almost complete at 90.13% ± 0.93% in dried beads. The maximum bead swelling rate showed 982.23 (F8, r2 = 0.996) in pH 6.8 and the drug release exceeded 90% in simulated gastrointestinal fluid (pH 6.8). Moreover, the beads were well distributed throughout various parts of the intestine. This designed formulation could possibly be advantageous in terms of increased bioavailability and targeted drug delivery to the intestine region and thus may find applications in some diseases like irritable bowel syndrome. View Full-Text
Keywords: black seed oil; alginate; beads; electrospray; microencapsulation black seed oil; alginate; beads; electrospray; microencapsulation
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Azad, A.K.; Al-Mahmood, S.M.A.; Chatterjee, B.; Wan Sulaiman, W.M.A.; Elsayed, T.M.; Doolaanea, A.A. Encapsulation of Black Seed Oil in Alginate Beads as a pH-Sensitive Carrier for Intestine-Targeted Drug Delivery: In Vitro, In Vivo and Ex Vivo Study. Pharmaceutics 2020, 12, 219.

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