Enhanced Viability of Probiotics against Gastric Acid by One-Step Coating Process with Poly-L-Lysine: In Vitro and In Vivo Evaluation

Due to their low acid tolerance, a majority of probiotics face diculties with regard tosurviving in the gastric environment long enough to reach the intestinal surfaces where they colonizeand provide health benefits. We prepared a probiotic delivery system that can enhance their viabilityin acidic conditions by developing a one-step poly-L-lysine (PLL) coating process. We determinedwhether the coating process was successful by measuring the zeta potential and observing it withconfocal scanning microscopy. PLL-coated L. plantarum (PLL-LP), incubated in a solution of pH 2 for2 h, exhibited a higher viability (6.86 0.12 log CFU/mL of viable cells) than non-coated L. plantarum(non-coated LP), which exhibited only 2.7 1.23 log CFU/mL of viable cells. In addition, a higheramount of L. plantarum was detected in the feces of mice orally administered PLL-LP (6.2 0.4 logCFU/g of feces) than in the feces of the control groups. In addition to enhancing probiotic viability inpH 2 solution, the PLL coating showed no eect on the probiotic growth pattern and the viability ofeither freeze-dried L. plantarum or L. plantarum, stored at ?20 C and 4 C, respectively. Overall, theseresults indicated that the PLL coating is a promising potential probiotic delivery system.

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Freeze-Dried Clopidogrel Loaded Lyotropic Liquid Crystal: Box-Behnken Optimization, In-Vitro and In-Vivo Evaluation

Current Drug Delivery ◽

10.2174/1567201817666200122161433 ◽

2020 ◽

Vol 17 (3) ◽

pp. 207-217

Author(s):

Eman A. Hakeem ◽

Galal M. El-Mahrouk ◽

Ghada Abdelbary ◽

Mahmoud H. Teaima

Keyword(s):

Statistical Analysis ◽

Oral Bioavailability ◽

Quadratic Model ◽

Lipid Phase ◽

Individual Response ◽

In Vivo Evaluation ◽

Freeze Dried ◽

Suggested Formula

Background: Clopidogrel (CLP) suffers from extensive first pass metabolism results in a negative impact on its oral systemic bioavailability. Cubosomes are Lyotropic Liquid Crystalline (LLC) nano-systems comprising monoolein, a steric stabilizer and an aqueous system, it considered a promising carrier for different pharmaceutical compounds. Box-Behnken Design (BBD) is an efficient tool for process analysis and optimization skipping forceful treatment combinations. Objective: The study was designed to develop freeze-dried clopidogrel loaded LLC (cubosomes) for enhancement of its oral bioavailability. Methods: A 33 BBD was adopted, the studied independent factors were glyceryl monooleate (GMO lipid phase), Pluronic F127 (PL F127steric stabilizer) and polyvinyl alcohol powder (stabilizer). Particle Size (PS), Polydispersity Index (PDI) and Zeta Potential (ZP) were set as independent response variables. Seventeen formulae were prepared in accordance with the bottom up approach and in-vitro evaluated regarding PS, PDI and ZP. Statistical analysis and optimization were achieved using design expert software®, then the optimum suggested formula was prepared, in-vitro revaluated, freeze-dried with 3% mannitol (cryoprotectant), solid state characterized and finally packed in hard gelatin capsule for comparative in-vitro release and in-vivo evaluation to Plavix®. Results: Results of statistical analysis of each individual response revealed a quadratic model for PS and PDI where a linear model for ZP. The optimum suggested formula with desirability factor equal 0.990 consisting of (200 mg GMO, 78.15 mg PL F127 and 2% PVA). LC/MS/MS study confirmed significant higher C>max, AUC>0-24h and AUC>0-∞ than that of Plavix®. Conclusion: The results confirm the capability of developed carrier to overcome the low oral bioavailability.

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A Novel Intravaginal Delivery System for Itraconazole: In Vitro and In Vivo Evaluation

Current Drug Delivery ◽

10.2174/156720109787846289 ◽

2009 ◽

Vol 6 (2) ◽

pp. 151-158 ◽

Cited By ~ 2

Author(s):

N. Dobaria ◽

R. Mashru ◽

A. Badhan ◽

A. Thakkar

Keyword(s):

Delivery System ◽

In Vivo Evaluation ◽

Intravaginal Delivery

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Development of Triamcinolone Acetonide-Loaded Microemulsion as a Prospective Ophthalmic Delivery System for Treatment of Uveitis: In Vitro and In Vivo Evaluation

Pharmaceutics ◽

10.3390/pharmaceutics13040444 ◽

2021 ◽

Vol 13 (4) ◽

pp. 444

Author(s):

Alaa Mahran ◽

Sayed Ismail ◽

Ayat A. Allam

Keyword(s):

Triamcinolone Acetonide ◽

Delivery System ◽

Histopathological Examination ◽

Rabbit Model ◽

Subconjunctival Injection ◽

In Vivo Evaluation ◽

Ternary Phase Diagrams ◽

Ophthalmic Delivery

Treatment of uveitis (i.e., inflammation of the uvea) is challenging due to lack of convenient ophthalmic dosage forms. This work is aimed to determine the efficiency of triamcinolone acetonide (TA)-loaded microemulsion as an ophthalmic delivery system for the treatment of uveitis. Water titration method was used to construct different pseudo-ternary phase diagrams. Twelve microemulsion formulations were prepared using oleic acid, Cremophor EL, and propylene glycol. Among all tested formulations, Formulation F3, composed of oil: surfactant-co-surfactant (1:1): water (15:35:50% w/w, respectively), was found to be stable and showed acceptable pH, viscosity, conductivity, droplet size (211 ± 1.4 nm), and zeta potential (−25 ± 1.7 mV) and almost complete in vitro drug release within 24 h. The in vivo performance of the optimized formulation was evaluated in experimentally uveitis-induced rabbit model and compared with a commercial TA suspension (i.e., Kenacort®-A) either topically or by subconjunctival injection. Ocular inflammation was evaluated by clinical examination, white blood cell count, protein content measurement, and histopathological examination. The developed TA-loaded microemulsion showed superior therapeutic efficiency in the treatment of uveitis with high patient compliance compared to commercial suspension. Hence, it could be considered as a potential ocular treatment option in controlling of uveitis.

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