Development of self emulsifying drug delivery system of itraconazole for oral delivery: formulation and pharmacokinetic consideration

We present a non-immunogenic, injectable, low molecular weight, amphiphilic hydrogel-based drug delivery system (TB-Gel) that can entrap a cocktail of four front-line antitubercular drugs isoniazid, rifampicin, pyrazinamide, and ethambutol. We...

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Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation

Nanomaterials ◽

10.3390/nano11112920 ◽

2021 ◽

Vol 11 (11) ◽

pp. 2920

Author(s):

Ameeduzzafar Zafar ◽

Syed Sarim Imam ◽

Nabil K. Alruwaili ◽

Omar Awad Alsaidan ◽

Mohammed H. Elkomy ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Oral Delivery ◽

Ex Vivo ◽

In Vitro Release ◽

System Optimization ◽

Globule Size

Hypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and transcutol HP as oil, surfactant, and co-surfactant, respectively. The formulation was optimized by three-factor, three-level Box-Behnken design. PE-SNEDDs were characterized for globule size, emulsification time, stability, in-vitro release, and ex-vivo intestinal permeation study. The optimized PE-SNEDDS (OF3) showed the globule size of 70.34 ± 3.27 nm, percentage transmittance of 99.02 ± 2.02%, and emulsification time of 53 ± 2 s Finally, the formulation OF3 was transformed into solid PE-SNEDDS (S-PE-SNEDDS) using avicel PH-101 as adsorbent. The reconstituted SOF3 showed a globule size of 73.56 ± 3.54 nm, PDI of 0.35 ± 0.03, and zeta potential of −28.12 ± 2.54 mV. SEM image exhibited the PE-SNEDDS completely adsorbed on avicel. Thermal analysis showed the drug was solubilized in oil, surfactant, and co-surfactant. S-PE-SNEDDS formulation showed a more significant (p < 0.05) release (97.87 ± 4.89% in 1 h) than pure PE (27.87 ± 2.65% in 1 h). It also exhibited better antimicrobial activity against S. aureus and P. aeruginosa and antioxidant activity as compared to PE dispersion. The in vivo activity in rats exhibited better (p < 0.05) antihypertensive activity as well as 4.92-fold higher relative bioavailability than pure PE dispersion. Finally, from the results it can be concluded that S-PE-SNEDDS might be a better approach for the oral delivery to improve the absorption and therapeutic activity.

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Self-microemulsifying drug delivery system (SMEDDS) for improved oral delivery and photostability of methotrexate

International Journal of Nanomedicine ◽

10.2147/ijn.s211014 ◽

2019 ◽

Vol Volume 14 ◽

pp. 4949-4960 ◽

Cited By ~ 8

Author(s):

Dong Shik Kim ◽

Jung Hyun Cho ◽

Jong Hyuck Park ◽

Jung Suk Kim ◽

Eon Soo Song ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Oral Delivery

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Pharmacodynamics and Pharmacokinetics Evaluation of Ranitidine Microemulsion on Experimental Animals

Advances in Pharmaceutics ◽

10.1155/2014/304392 ◽

2014 ◽

Vol 2014 ◽

pp. 1-6

Author(s):

Sajal Kumar Jha ◽

Roopa Karki ◽

Venkatesh Dinnekere Puttegowda ◽

Amitava Ghosh

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Intestinal Permeability ◽

Delivery System ◽

Oral Delivery ◽

Tween 80 ◽

Standard Drug ◽

Alternative Drug ◽

And Control ◽

Antiulcer Therapy

Ranitidine microemulsion was investigated for its pharmacodynamic and pharmacokinetic evaluation to find out the suitability of microemulsion as a potential drug delivery system in the treatment of ulcer. The bioavailability of ranitidine after oral administration is about 50% and is absorbed via the small intestine; this may be due to low intestinal permeability. Hence the aim of present investigation was to maximize the therapeutic efficacy of ranitidine by developing microemulsion to increase the intestinal permeability as well as bioavailability. A ground nut oil based microemulsion formulation with Tween-80 as surfactant and PEG-400 as cosurfactant was developed for oral delivery of ranitidine and characterized for physicochemical parameters. In pharmacodynamic studies, significant (P<0.05) variation in parameters estimated was found between the treated and control groups. Ranitidine microemulsion exhibited higher absorption and Cmax (863.20 ng·h/mL) than the standard (442.20 ng/mL). It was found that AUC0–24 hr obtained from the optimized ranitidine test formulation (5426.5 ng·h/mL) was significantly higher than the standard ranitidine (3920.4 ng·h/mL). The bioavailability of optimized formulation was about 1.4-fold higher than that of standard drug. This enhanced bioavailability of ranitidine microemulsion may be used as an effective and alternative drug delivery system for the antiulcer therapy.

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Bilayer Floating Tablets for Gastroretentive Drug Delivery System

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2013.6.3.1 ◽

2013 ◽

Vol 6 (3) ◽

pp. 2097-2112

Author(s):

Sai Sowjanya Palla ◽

Rajkumar Kotha ◽

Anusha Paladugu ◽

E. Rajesh Kumar Reddy ◽

Suryasri Lavanya Adavi ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Oral Delivery ◽

Immediate Release ◽

Gastric Fluid ◽

New Era ◽

Floating Tablets ◽

Colloidal Gel ◽

Floating Tablet

Oral delivery of the drug is by far the most preferable route of drug delivery due to the ease of administration, patient compliance and flexibility in the formulations but has a drawback of non-site specificity and short gastric resident time. In recent years, scientific and technological advancements have been made in the development of novel drug delivery systems by overcoming physiological troubles such as short gastric residence times and unpredictable gastric emptying times. Among Several approaches of floating systems, Bilayer floating technology is considered as promising approach. It combines the principle of bilayer technology and floating mechanism. The combined principle of bilayer floating tablet helps to release initial dose from the immediate release layer to reach the plasma concentration and then the floating layer absorbs gastric fluid forming an impermeable colloidal gel barrier on its surface, maintains a bulk density less than unity and thereby remains buoyant in stomach providing steady state concentration of drug in system. This review focuses on bilayer floating tablet technology a new era of gastro retentive drug delivery system, its advantages over conventional tablets and it also summarizes the bilayer tablet presses used in the industry, formulation design and evaluation parameters of bilayer floating tablets.

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Chronomodulated Drug Delivery System of Salmeterol Fluticasone Nlcs Loaded Tablets: Preparation, Characterization, Stability and Drug Release Studies for Management of Asthma

Asian Journal of Research in Pharmaceutical Science ◽

10.52711/2231-5659.2021-11-2-1 ◽

2021 ◽

Vol 11 (2) ◽

pp. 95-102

Author(s):

Mohammed Waseem A ◽

Ajin P Kurian ◽

Dhanapal Y

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Oral Delivery ◽

Ex Vivo ◽

Drug Loading ◽

Water Soluble ◽

Size Analysis ◽

Differential Scanning Calorimetric ◽

Time Interval

Objective: The purpose of this study was to develop salmeterol, fluticasone nano-lipid carriers to estimate as potentials of oral delivery system for poorly water soluble drugs. Nano-lipid carriers applied to chronomodulated pulsatile drug delivery system maintain the concentration level by releasing the drug at predetermined time interval throughout the management of asthma. Method: The particle size analysis revealed that all the formulations were within the nanometer range of 150.0±2.4nm. Percentage of entrapment efficiency and drug loading were found to be 69.5±4.4 - 85.3±1.3 and 9.358±2.2-10.45±8.1, respectively. The SLM-FCN nano-lipid carrier’s optimized formulation showed spherical morphology with smooth surface under the transmission electron microscope (TEM), the crystalline characterization of drug in NLC was investigated by X-ray diffraction and differential scanning calorimetric (DSC). The ex-vivo permeation study showed many folds increment in the SLM-FCN NLCs compared to powder SLM-FCN 96.0±2.55 and pulsing plugs in-vivo drug released effectively in pre-determine time intervals. Conclusion: The progression concludes that chronomodulated programming pulsatile release was achieved with modified pulsing bilayerd plugged of salmeterol, fluticasone propionate NLCs, formulation remarkably improved oral bioavailability. we promise that finding in this investigations suggest practicability of the dosage form system can be taken after at bedtime then it will be delivered in the early morning which maintains the drug concentration throughout to control asthma.

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