Development of curcumin floating beads with low density materials and solubilizers

Treesinchai, Sakonjan; Puttipipatkhachorn, Satit; Pitaksuteepong, Tasana; Sungthongjeen, Srisagul

doi:10.1016/j.jddst.2019.03.002

Cited by 10 publications

(8 citation statements)

References 42 publications

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“…As shown in Figure 10 , the SEM image of the optimized formulation of TEL-loaded oil-entrapped floating alginate beads have an almost spherical shape with rough and porous exterior surfaces, which assisted in the controlled release of the drug from the floating beads with good buoyancy. The results were in agreement with the findings obtained by Treesinchai et al in 2019 [ 54 ].…”

Section: Resultssupporting

confidence: 93%

“…The emulsification of the sesame oil in the alginate solution and the rapid gelation within the alginate gel matrices resulted in the formation of tiny oil pockets either deep within the matrices or on the surfaces of the beads. These oily pockets offered buoyancy to the beads, allowing them to float for longer periods and providing a safety margin over premature sedimentation [ 54 ].…”

Section: Resultsmentioning

confidence: 99%

“…An additional property of buoyancy was observed in the oil-entrapped beads; this was due to the incorporation of oil, which has less density than water. The lower the density of the oil, the lower the amount of oil required to give it a buoyant nature [ 54 ]. Thus, it is evident that the oil-entrapped beads exhibited satisfactory gastro-retention and improved the solubility and drug release within the gastric region [ 58 ].…”

Section: Resultsmentioning

confidence: 99%

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Optimization and In Vitro Characterization of Telmisartan Loaded Sodium Alginate Beads and Its In Vivo Efficacy Investigation in Hypertensive Induced Animal Model

et al. 2023

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Background: Antihypertensive drug telmisartan (TEL) belongs to BCS class II, which is characterized by low water solubility and, consequently, low oral bioavailability. Gastroretentive systems may overcome the problems associated with low solubility of TEL and incomplete absorption by localizing the drug release in the stomach. The purpose of this study was to prepare TEL-loaded, oil-entrapped, floating alginate beads with the intent of enhancing the oral bioavailability of TEL for the treatment of hypertension. Methods: For the formulation and optimization of seventeen formulations of TEL-loaded oil-entrapped floating alginate beads, a central composite design was utilized. The concentration of sodium alginate (X1), the concentration of cross-linker (X2), and the concentration of sesame oil (X3) served as independent variables, whereas the entrapment efficiency (Y1), in vitro buoyancy (Y2), and drug release Q6h (Y3) served as dependent variables. Using the emulsion gelation method and calcium chloride as the cross-linking agent, different formulations of TEL alginate beads were produced. All formulations were evaluated for their entrapment efficiency percentage, in vitro buoyancy, and in vitro drug release. The optimal formulation of TEL alginate beads was prepared with and without oil and evaluated for entrapment efficiency percentage, in vitro buoyancy, swelling ratio, average size, and in vitro drug release. Using scanning electron microscopes, the surface morphology was determined. Using IR spectroscopy, the compatibility between the ingredients was determined. In vivo evaluation of the optimized formulation in comparison to the free TEL was done in hypertension-induced rats, and the systolic blood pressure and all pharmacokinetic parameters were measured. Results: The prepared beads exhibited a high entrapment efficiency percentage, in vitro buoyancy, and prolonged drug release. TEL was compatible with other ingredients, as approved by IR spectroscopy. The prepared TEL beads were spherical, as shown by the SEM. The relative bioavailability of TEL-loaded oil-entrapped beads was 222.52%, which was higher than that of the pure TEL suspension. The prepared TEL beads formulation exhibited a higher antihypertensive effect for a prolonged time compared to pure TEL suspension. Conclusions: It can be concluded that this innovative delivery method of TEL-loaded oil-entrapped beads is a promising tool for enhancing drug solubility and, thus, oral bioavailability and therapeutic efficacy, resulting in enhanced patient compliance. Furthermore, the in vivo study confirmed the formulation’s extended anti-hypertensive activity in animal models.

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Section: Resultssupporting

confidence: 93%

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

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Optimization and In Vitro Characterization of Telmisartan Loaded Sodium Alginate Beads and Its In Vivo Efficacy Investigation in Hypertensive Induced Animal Model

et al. 2023

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“…The percentage swelling index of all bead formulations (F1-F9) were at first lower in SGF, in contrast with that of SIF, demonstrating a pH-sensitive swelling behaviour. This might have occurred due to shrinkage of alginate at acidic pH [46]. Therefore, higher percentage of swelling index of these beads were noticed at 30-90 min in SIF (pH 6.8).…”

Section: Bead Swelling Behaviourmentioning

confidence: 90%

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

et al. 2020

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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.

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“…In another effort, for treating peptic ulcer, CUR is formulated with low density material such as polypropylene foam powder, oils and various solubilizers. This biocomposite has prolonged gastro-retention time and improve insufficient CUR release [184]. This composite is a promising carrier for drug targeted at stomach using CUR formulation.…”

Section: Curcumin Based Biocomposite Formulationmentioning

confidence: 99%

Therapeutic Applications of Curcumin Nanomedicine Formulations in Cardiovascular Diseases

Salehi

Prado-Audelo

Cortés

et al. 2020

JCM

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Cardiovascular diseases (CVD) compromises a group of heart and blood vessels disorders with high impact on human health and wellbeing. Curcumin (CUR) have demonstrated beneficial effects on these group of diseases that represent a global burden with a prevalence that continues increasing progressively. Pre-and clinical studies have demonstrated the CUR effects in CVD through its anti-hypercholesterolemic and anti-atherosclerotic effects and its protective properties against cardiac ischemia and reperfusion. However, the CUR therapeutic limitation is its bioavailability. New CUR nanomedicine formulations are developed to solve this problem. The present article aims to discuss different studies and approaches looking into the promising role of nanotechnology-based drug delivery systems to deliver CUR and its derivatives in CVD treatment, with an emphasis on their formulation properties, experimental evidence, bioactivity, as well as challenges and opportunities in developing these systems.

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Development of curcumin floating beads with low density materials and solubilizers

Cited by 10 publications

References 42 publications

Optimization and In Vitro Characterization of Telmisartan Loaded Sodium Alginate Beads and Its In Vivo Efficacy Investigation in Hypertensive Induced Animal Model

Optimization and In Vitro Characterization of Telmisartan Loaded Sodium Alginate Beads and Its In Vivo Efficacy Investigation in Hypertensive Induced Animal Model

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

Therapeutic Applications of Curcumin Nanomedicine Formulations in Cardiovascular Diseases

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