scholarly journals Self-Nanoemulsifying Drug Delivery System (SNEDDS) for Improved Oral Bioavailability of Chlorpromazine: In Vitro and In Vivo Evaluation

Medicina ◽  
2019 ◽  
Vol 55 (5) ◽  
pp. 210 ◽  
Author(s):  
Jeand Baloch ◽  
Muhammad Farhan Sohail ◽  
Hafiz Shaib Sarwar ◽  
Maria Hassan Kiani ◽  
Gul Majid Khan ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Oral Bioavailability ◽  
Drug Loading ◽  
Antipsychotic Agent ◽  
In Vivo Evaluation ◽  
Promising Alternative ◽  
Long Chain Triglycerides ◽  
Long Chain

Background and Objectives: Lipid-based self-nanoemulsifying drug delivery systems (SNEDDS) have resurged the eminence of nanoemulsions by modest adjustments and offer many valuable opportunities in drug delivery. Chlorpromazine, an antipsychotic agent with poor aqueous solubility—with extensive first-pass metabolism—can be a suitable candidate for the development of SNEDDS. The current study was designed to develop triglyceride-based SNEDDS of chlorpromazine to achieve improved solubility, stability, and oral bioavailability. Materials and Methods: Fifteen SNEDDS formulations of each short, medium, and long chain, triglycerides were synthesized and characterized to achieve optimized formulation. The optimized formulation was characterized for several in vitro and in vivo parameters. Results: Particle size, zeta potential, and drug loading of the optimized SNEDDS (LCT14) were found to be 178 ± 16, −21.4, and 85.5%, respectively. Long chain triglyceride (LCT14) showed a 1.5-fold increased elimination half-life (p < 0.01), up to 6-fold increased oral bioavailability, and 1.7-fold decreased plasma clearance rate (p < 0.01) compared to a drug suspension. Conclusion: The findings suggest that SNEDDS based on long-chain triglycerides (LCT14) formulations seem to be a promising alternative for improving the oral bioavailability of chlorpromazine.

scholarly journals Encapsulated Escitalopram and Paroxetine Intranasal Co-Administration: In Vitro/In Vivo Evaluation

2021 ◽  
Vol 12 ◽  
Author(s):  
Soraia Silva ◽  
Joana Bicker ◽  
Carla Fonseca ◽  
Nuno R. Ferreira ◽  
Carla Vitorino ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Selective Serotonin Reuptake Inhibitors ◽  
Common Mental Disorder ◽  
Drug Loading ◽  
Pharmacokinetic Studies ◽  
Brain Delivery ◽  
In Vivo Evaluation ◽  
The Brain

Depression is a common mental disorder. Its treatment with selective serotonin reuptake inhibitors (SSRIs) is effective only in a fraction of patients, and pharmacoresistance is increasing steadily. Intranasal (IN) drug delivery to the brain stands out as a promising strategy to improve current therapeutic approaches by operating as a shuttle to overcome the blood–brain barrier. This work aimed to simultaneously administer escitalopram and paroxetine by IN route to mice. For this purpose, three nanostructured lipid carriers (NLC1, NLC2, and BorNLC) and one nanoemulsion (NE) were tested for drug loading. After their characterization, investigation of their impact on nasal cell viability and SSRI permeability assays were performed, using a human nasal RPMI 2650 cell line in air–liquid interface. In vitro assays demonstrated that NLCs, including borneol (BorNLC), significantly increased escitalopram permeability (p &lt; 0.01) and paroxetine recovery values (p &lt; 0.05) in relation to the other formulations and non-encapsulated drugs. IN and intravenous (IV) pharmacokinetic studies performed in vivo with a single dose of 2.38 mg/kg demonstrated similar results for escitalopram brain-to-plasma ratios. IN administrations delayed escitalopram peak concentrations in the brain for 15–60 min and no direct nose-to-brain delivery was detected. However, encapsulation with BorNLC considerably decreased escitalopram exposure in the lungs (124 μg min/g) compared with free escitalopram by IN (168 μg min/g) and IV (321 μg min/g) routes. Surprisingly, BorNLC IN instillation increased concentration levels of paroxetine in the brain by five times and accelerated brain drug delivery. Once again, lung exposure was considerably lower with BorNLC (AUCt = 0.433 μg min/g) than that with IV administration (AUCt = 1.01 μg min/g) and non-encapsulated IN formulation (AUCt = 2.82 μg min/g). Direct nose-to-brain delivery was observed for paroxetine IN administration with a direct transport percentage (DTP) of 56.9%. If encapsulated, it increases to 74.2%. These results clearly emphasize that nose-to-brain delivery and lung exposure depend on the formulation and on the characteristics of the drug under investigation. NLCs seem to be an advantageous strategy for nose-to-brain delivery of lipophilic molecules, since they reduce systemic and lung exposure, thereby decreasing adverse effects. For hydrophilic compounds, NLCs are particularly important to decrease lung exposure after IN administration.

scholarly journals Development of Solid Self – Nanoemulsified Drug Delivery System Containing Rosuvastatin

2020 ◽  
Vol 36 (3) ◽  
Author(s):  
Tran Thi Hai Yen ◽  
Nguyen Thi Yen ◽  
Nguyen Canh Hung ◽  
Phan Thi Nghia ◽  
Pham Bao Tung ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Promising Alternative ◽  
Atorvastatin Calcium ◽  
Study Results ◽  
Rosuvastatin Calcium

This study aims to solidify the self-nanoemulsifying drug delivery system with rosuvastatin (SNEDDS Ros) for application in solid dosage forms. The liquid SNEDDS Ros system is solidified by granulation and spray drying methods. Solid SNEDDS Ros was evaluated on the drug content, the Carr index, nanoemulsification efficiency and several criteria of nanoemulsion, formed after emulsification of solid SNEDDS Ros, such as droplet size, polydispersion index (PDI), the drug proportion in the oil phase. The study results show that solid SNEDDS Ros, prepared by granulation method using Prosolv SMCC 90 as an adsorbent, had good flowability with the Carr index of about 15. The nanoemulsion, obtained after emulsification of the solid SNEDDS, had an average particle size of 15 nm, PDI less than 0.2, drug nanoemulsified efficiency of 94 % and drug proportion in the oil phase of 84%. Keywords Rosuvastatin, SNEDDS, Solid SNEDDS, solidification. References [1] A.G. Olsson, F. McTaggart, and A. Raza, Rosuvastatin: A Highly Effective New HMG-CoA Reductase Inhibitor. Cardiovasc. Drug Rev., 20 (2006) 303–328. https://doi.org/10.1111/j.1527-3466.2002.tb00099.x[2] A.M. Kassem, H.M. Ibrahim, and A.M. Samy, Development and optimisation of atorvastatin calcium loaded self-nanoemulsifying drug delivery system (SNEDDS) for enhancing oral bioavailability: in vitro and in vivo evaluation. J. Microencapsul 34 (2017) 319–333. https://doi.org/10.1080/02652048.2017.1328464[3] M.N. Ahsan and P.R. Prasad Verma, Solidified self nano-emulsifying drug delivery system of rosuvastatin calcium to treat diet-induced hyperlipidemia in rat: in vitro and in vivo evaluations. Ther. Deliv 8 (2017) 125–136. https://doi.org/10.4155/tde-2016-0071[4] S. Verma, S.K. Singh, P. R. P. Verma, and M. N. Ahsan, Formulation by design of felodipine loaded liquid and solid self nanoemulsifying drug delivery systems using Box-Behnken design. Drug Dev. Ind. Pharm. 40 (2014) 1358–1370. https://doi.org/10.3109/03639045.2013.819884[5] M.S. Reddy, Formulation and In Vitro Characterization of Solid-self Nanoemulsifying Drug Delivery System of Atorvastatin Calcium. Asian J. Pharm. 11 (2018) 991-999. https://dx.doi.org/10.22377/ajp.v11i04.1771.[6] N. Kulkarni, N. Ranpise, and G. Mohan, Development and evaluation of solid self nano-emulsifying formulation of rosuvastatin calcium for improved bioavailability. Trop. J. Pharm. Res. 14 (2015) 575–582. https://doi.org/10.4314/tjpr.v14i4.3[7] A.O. Kamel and A.A. Mahmoud, Enhancement of human oral bioavailability and in vitro antitumor activity of rosuvastatin via spray dried self-nanoemulsifying drug delivery system. J. Biomed. Nanotechnol. 9 (2013) 26–39. https://doi.org 10.1166/jbn.2013.1469.[8] H.A. Abo Enin and H.M. Abdel-Bar, Solid super saturated self-nanoemulsifying drug delivery system (sat-SNEDDS) as a promising alternative to conventional SNEDDS for improvement rosuvastatin calcium oral bioavailability. Expert Opin. Drug Deliv. 13 (2016) 1513–1521. https://doi.org/10.1080/17425247.2016.1224845            

scholarly journals Enhancement of Oral Bioavailability of Ibandronate Through Gastroretentive Raft Forming Drug Delivery System: In Vitro and In Vivo Evaluation

2020 ◽  
Vol Volume 15 ◽  
pp. 4847-4858
Author(s):  
Muhammad Hanif ◽  
Shahid Shah ◽  
Akhtar Rasul ◽  
Ghulam Abbas ◽  
Muhammad Zaman ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
In Vivo Evaluation

Solid self-nanoemulsifying drug delivery system (S-SNEDDS) of darunavir for improved dissolution and oral bioavailability: In vitro and in vivo evaluation

2015 ◽  
Vol 74 ◽  
pp. 1-10 ◽  
Author(s):  
Spandana Inugala ◽  
Basanth Babu Eedara ◽  
Sharath Sunkavalli ◽  
Rajeshri Dhurke ◽  
Prabhakar Kandadi ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
In Vivo Evaluation

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

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