Buspirone Hydrochloride Loaded In Situ Nanovesicular Gel as an Anxiolytic Nasal Drug Delivery System: In Vitro and Animal Studies

Abdelnabi, Dina M.; Abdallah, Marwa H.; Elghamry, Hanaa A.

doi:10.1208/s12249-018-1211-0

Cited by 21 publications

(15 citation statements)

References 31 publications

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“…The second endothermic peak, at 204.45 °C, was due to the melting of the recrystallized polymorph-2 of the drug. These results were in accordance with the data obtained in the literature [ 14 , 15 ]. The thermogram of the Na alg.…”

Section: Resultssupporting

confidence: 93%

“…From the obtained data, it was concluded that the relative bioavailability of the BH-loaded in situ gel was higher than the drug solution by more than 1.5-fold. The enhanced relative bioavailability of the BH may have been due to the decreased release of the drug from the in situ gel, which led to a more sustained release and absorption of the drug compared to the free-solution form [ 15 , 24 ].…”

Section: Resultsmentioning

confidence: 99%

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Response Surface Methodology for Optimization of Buspirone Hydrochloride-Loaded In Situ Gel for Pediatric Anxiety

Abdallah

Abdelnabi

Elghamry

2022

Gels

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The purpose of the current investigation was to formulate, assess, and optimize oral in situ gels of buspirone hydrochloride (BH) with the specific end goal of expanding the time the medication spends in the stomach, thereby ensuring an extended medication discharge. This would allow the use of a once-a-day dose of liquid BH formulations, which is ideal for the treatment of pediatric anxiety. In situ gels loaded with BH were prepared using various concentrations of sodium alginate (Na alg.), calcium chloride (CaCl2), and hydroxypropyl methylcellulose (HPMC K15M). The in situ gels exhibited the desired consistency, drug distribution, pH, ability to form gel, and prolonged drug release in vitro. The (33) full factorial design was utilized for the revealing of the ideal figures for the selected independent variables, Na alg. (X1), HPMC (X2), and CaCl2 (X3) based on measurements of the viscosity (Y1) and percentage drug release after 6 h (Y2). A pharmacokinetic study of the optimum formulation on rabbits was also performed. The formulation containing 2% of Na alg., 0.9% of HPMC-K15M, and 0.1125% of CaCl2 was selected as the ideal formulation, which gave the theoretical values of 269.2 cP and 44.9% for viscosity and percentage of drug released after 6 h, respectively. The pharmacokinetic study showed that the selected oral Na alg. in situ gel formulation displayed a prolonged release effect compared to BH solution and the marketed tablet (Buspar®), which was confirmed by the low Cmax and high Tmax values. The optimum oral Na alg. in situ gel showed a 1.5-fold increment in bioavailability compared with the drug solution.

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Section: Resultssupporting

confidence: 93%

Section: Resultsmentioning

confidence: 99%

Response Surface Methodology for Optimization of Buspirone Hydrochloride-Loaded In Situ Gel for Pediatric Anxiety

Abdallah

Abdelnabi

Elghamry

2022

Gels

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“…At definite time intervals (0.25, 0.5, 1, 2, 4 and 6 h), 2 mL samples were withdrawn and substituted with the fresh buffer. Samples were analyzed for drug content spectroscopically at λ max 287 nm [ 28 ].…”

Section: Methodsmentioning

confidence: 99%

Experimental Design and Optimization of Nano-Transfersomal Gel to Enhance the Hypoglycemic Activity of Silymarin

et al. 2022

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Current advancements in the research investigations focused at using natural products to generate novel dosage forms with a potential therapeutic impact. Silymarin is a natural product obtained from the herb Silybum marianum that has been shown to have remarkable hypoglycemic activity. Owing to the low enteral absorption, instability in stomach secretion, and poor solubility of Silymarin, it was better to be produced as a topical dosage form. A three-factor, three-level Box Behnken (33 BB) design was constructed to develop 15 formulations using three independent variables (phospholipid concentration, surfactant concentration, and sonication time) and two dependent variables (encapsulation efficiency and in vitro drug release). The optimized formula was added to HPMC gel and the resulting transfersomal gel was investigated for its characteristics, in vitro, ex vivo and hypoglycemic behaviors. The pH of the Silymarin-loaded transfersomal gel was 7.05, the spreadability was 55.35 mm, and the viscosity was 6.27 Pa. Furthermore, Silymarin loaded transfersomal gel had the greatest transdermal flux (92.41 µg/cm2·h), which was much greater than all other formulations. In vivo observations revealed that Silymarin loaded transfersomal gel significantly reduced blood glucose levels, compared to either Silymarin gel or oral Silymarin suspension. The findings show that the developed transfersomal gel could be an effective carrier for Silymarin transdermal delivery.

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“…The study was performed according to the guidelines of the International Conference on Harmonization (ICH) to evaluate different criteria of the formulation such as pH, viscosity, spreadability, and in vitro drug release. The study was conducted after storing the formulation at 4 ± 1 °C and at 25 ± 1 °C for a period of 1 and 3 months [ 45 ].…”

Section: Methodsmentioning

confidence: 99%

Tea Tree Oil Nanoemulsion-Based Hydrogel Vehicle for Enhancing Topical Delivery of Neomycin

Elsewedy

Shehata

Soliman

2022

Life

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The present investigation aims to improve the antimicrobial influence of certain antibacterial drugs, namely, neomycin (NEO), exploiting the benefits of natural oils such as tea tree oil (TTO). Therefore, a distinctive nanolipid formulation, namely, a nanoemulsion (NE), was developed using a Central Composite Factorial Design (CCD) approach depending on the amount of TTO and tween 80 as surfactant. The optimized NEO-NE formula exhibiting minimum globular size and maximum in vitro release was selected. For efficient topical delivery, NEO-NE was incorporated into a pre-formulated hydrogel. The developed NEO-NE-hydrogel was characterized by its physical characteristics such as pH, viscosity, and spreadability. Next, it was tested for stability under different conditions for 3 months. Ultimately, an irritation test was conducted followed by an antibacterial examination. The preparation demonstrated acceptable properties to be successfully applied topically. It showed non-significant changes in stability in both conditions up to 3 months storage when compared to a fresh preparation. It exhibited no irritation when applied on hairless animal skin. Finally, TTO revealed a good inhibition for the bacterial growth that could improve the influence of NEO antibacterial activity, indicating the efficiency of NE containing NEO prepared with TTO to be a promising antibacterial nanocarrier.

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Buspirone Hydrochloride Loaded In Situ Nanovesicular Gel as an Anxiolytic Nasal Drug Delivery System: In Vitro and Animal Studies

Cited by 21 publications

References 31 publications

Response Surface Methodology for Optimization of Buspirone Hydrochloride-Loaded In Situ Gel for Pediatric Anxiety

Response Surface Methodology for Optimization of Buspirone Hydrochloride-Loaded In Situ Gel for Pediatric Anxiety

Experimental Design and Optimization of Nano-Transfersomal Gel to Enhance the Hypoglycemic Activity of Silymarin

Tea Tree Oil Nanoemulsion-Based Hydrogel Vehicle for Enhancing Topical Delivery of Neomycin

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