scholarly journals Preparation and Evaluation of Zafirlukast Compression Coated Tablets for Chronotherapeutic Drug Delivery

2021 ◽  
pp. 154-166
Author(s):  
M. S. Neeharika ◽  
B. Jeevana Jyothi
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Solid Dispersion ◽  
Chemical Interaction ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Natural Polymers ◽  
Compression Coating

The objective of the present study was to formulate and evaluate an oral, time-controlled drug delivery system of Zafirlukast. Zafirlukast belongs to BCS class II drugs as it has poor aqueous solubility and good permeability. Hence an attempt has been made to improve its aqueous solubility by solid dispersion technique so that its dissolution, bioavailability, and therapeutic effect can be optimized. The optimized solid dispersion was then formulated into a chronotherapeutic drug delivery system by compression coating technology. FT-IR study revealed that there was no chemical interaction between the drug and polymers used. Tablets were prepared by direct compression method using different super disintegrants and then followed by compression coating using natural polymers. Pre-compression and post-compression parameters complied with the Pharmacopoeia limit for the tablets. In vitro release studies were performed and the results indicated the formulation Z9F9 to be the optimized formulation.

scholarly journals Formulation and Development of Gastroretentive Drug Delivery System of Efavirenz

2019 ◽  
Vol 11 (05) ◽  
Author(s):  
Monica RP Rao ◽  
Pooja B. Karanjkar
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Solid Dispersion ◽  
In Vitro Release ◽  
Lag Time ◽  
Intrinsic Dissolution ◽  
Drug Content

Efavirenz, a non-nucleotide reverse transcriptase inhibitor is an important drug for treating patients with Human Immunodeficiency Virus infections. It belongs to BCS class II have low solubility and poor intrinsic dissolution rate. It is highly basic (pKa 10.2) which makes it suitable candidate for floating dosage form for continuous delivery in stomach.The study was aimed to improve the solubility by solid dispersion technique.Saturation solubility study and drug content were evaluated for solid dispersion preparation. Saturation solubility shows 8 fold increases in 0.1 N HCL compared to plain drug and drug content was found to be between 95%-102%. Further effervescent floating gastroretentive drug delivery system was prepared by 32 full factorial design with independent variables i.e., concentration of HPMC K100 as matrix forming agent and citric acid as gas generating agent. Lag time, floating time, percent drug release were studied as responses. The optimized batch exhibited floating lag time of 40 sec and the in vitro release studies showed 89.5% drug release in 9 h and tablet remained floating for greater than 8 h. The study thus demonstrated that solubility is increased by solid dispersion technique and floating delivery systems may increase solubility and bioavailability of Efavirenz.

Montmorillonite-Alginate Nanocomposites as a Drug Delivery System: Intercalation and In Vitro Release of Vitamin B1 and Vitamin B6

2009 ◽  
Vol 25 (2) ◽  
pp. 161-177 ◽  
Author(s):  
Bhavesh D. Kevadiya ◽  
Ghanshyam V. Joshi ◽  
Hasmukh A. Patel ◽  
Pravin G. Ingole ◽  
Haresh M. Mody ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Vitamin B6 ◽  
In Vitro Release ◽  
Vitamin B1 ◽  
Vitro Release

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

Nanomaterials ◽  
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.

Enhanced Oral Bioavailability and Improved Biological Activities of a Quercetin/Resveratrol Combination Using a Liquid Self-Microemulsifying Drug Delivery System

Planta Medica ◽  
2020 ◽  
Author(s):  
Patcharawalai Jaisamut ◽  
Subhaphorn Wanna ◽  
Surasak Limsuwan ◽  
Sasitorn Chusri ◽  
Kamonthip Wiwattanawongsa ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Biological Activities ◽  
Area Under The Curve ◽  
Aqueous Solubility ◽  
The Self

AbstractBoth quercetin and resveratrol are promising plant-derived compounds with various well-described biological activities; however, they are categorized as having low aqueous solubility and labile natural compounds. The purpose of the present study was to propose a drug delivery system to enhance the oral bioavailability of combined quercetin and resveratrol. The suitable self-microemulsifying formulation containing quercetin together with resveratrol comprised 100 mg Capryol 90, 700 mg Cremophor EL, 200 mg Labrasol, 20 mg quercetin, and 20 mg resveratrol, which gave a particle size of 16.91 ± 0.08 nm and was stable under both intermediate and accelerated storage conditions for 12 months. The percentages of release for quercetin and resveratrol in the self-microemulsifying formulation were 75.88 ± 1.44 and 86.32 ± 2.32%, respectively, at 30 min. In rats, an in vivo pharmacokinetics study revealed that the area under the curve of the self-microemulsifying formulation containing quercetin and resveratrol increased approximately ninefold for quercetin and threefold for resveratrol compared with the unformulated compounds. Moreover, the self-microemulsifying formulation containing quercetin and resveratrol slightly enhanced the in vitro antioxidant and cytotoxic effects on AGS, Caco-2, and HT-29 cells. These findings demonstrate that the self-microemulsifying formulation containing quercetin and resveratrol could successfully enhance the oral bioavailability of the combination of quercetin and resveratrol without interfering with their biological activities. These results provide valuable information for more in-depth research into the utilization of combined quercetin and resveratrol.

scholarly journals SELF-NANO EMULSIFYING DRUG DELIVERY SYSTEM OF EFAVIRENZ: FORMULATION, IN VITRO EVALUATION AND CHARACTERIZATION

2019 ◽  
pp. 217-226
Author(s):  
PAMU SANDHYA
Keyword(s):  
Drug Delivery ◽  
Dissolution Rate ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Vitro Release ◽  
Visual Observation ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Tween 20

Objective: The main objective of this study was to preparation and evaluation of efavirenz (EFV) to enhance its solubility and dissolution rate by self-emulsifying drug delivery system. Methods: EFV self-emulsifying drug delivery systems (SNEDDS) were formulated using different oils, surfactant, and co-surfactant. Peceol, Tween 20, and Capmul MCM were used as oil, surfactant, and co-surfactant, respectively, followed by the evaluation by the performance of different tests such as visual observation, solubility studies, thermodynamic stability study, transmittance studies, drug content, and in-vitro release study. Results: Fourier-transform infrared studies revealed negligible drug and polymer interaction. From the phase diagram, it was observed that self-emulsifying region was enhanced with increasing surfactant and co-surfactant concentrations with oil. F13 was selected as optimized formulation on the basis of physicochemical parameters, particle size, and in-vitro dissolution studies with the release of 98.39±5.10% drug in 1 hour. The optimized formulation size was found to be 156.7 nm as mean droplet size and Z-Average of 808.6 nm with -18.3 mV as zeta potential. Conclusion: The study demonstrated that SNEDDS was a promising strategy to enhance the dissolution rate of EFV by improving solubility.

scholarly journals In Vitro Release Mechanisms of Doxorubicin From a Clinical Bead Drug-Delivery System

2016 ◽  
Vol 105 (11) ◽  
pp. 3387-3398 ◽  
Author(s):  
Emelie Ahnfelt ◽  
Erik Sjögren ◽  
Per Hansson ◽  
Hans Lennernäs
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Vitro Release ◽  
Release Mechanisms ◽  
Vitro Release

An Investigation of the Release Properties of a Cationic Drug From a Hydrophobic Polyanhydride Matrix as a Function of Dissolution Medium

1998 ◽  
Vol 550 ◽  
Author(s):  
E. J. Ginsburg ◽  
T. D. Stultz ◽  
D. A. Stephens ◽  
D. Robinson ◽  
Y. Tian ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Anion Exchange ◽  
Polymer Chain ◽  
Delivery System ◽  
In Vitro Release ◽  
Dissolution Medium ◽  
Poorly Soluble ◽  
Vitro Release

AbstractThe dissolution of a drug delivery system consisting of gentamicin sulfate in a hydrophobic polyanhydride matrix has been examined. The in vitro release of gentamicin is a function of the composition of the dissolution medium, with slower release in pH 7.4 buffer than in unbuffered water. This is consistent with an anion exchange taking place under conditions in which carboxylate polymer chain-ends form a poorly soluble salt with gentamicin, and sulfate is released into solution. Results of additional experiments probing this model are digeussed.

scholarly journals Drug delivery system and in vitro release of luteolin based on magnetic nanocomposite (Fe 3 O 4 @ZIF‐67)

2020 ◽  
Vol 15 (7) ◽  
pp. 425-429 ◽  
Author(s):  
Yuqiong Shi ◽  
Beibei Qiu ◽  
Xiangrong Wu ◽  
Yuxuan Wang ◽  
Jinhua Zhu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Vitro Release ◽  
Magnetic Nanocomposite ◽  
Vitro Release

Preparation and Characterization of Mucoadhesive Nanoemulsion containing Piperine for Nasal Drug Delivery System

2021 ◽  
pp. 2381-2386
Author(s):  
Deepika Yadav ◽  
Avijit Mazumder ◽  
Roop K Khar
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Vitro Release ◽  
Nasal Administration ◽  
Piper Nigrum ◽  
Therapeutic Effects ◽  
Globule Size

Piperine a bio active constituent isolated from pepper (Piper nigrum and Piper longum L.) is a naturally occurring alkaloid have validated for several health effects and valuable therapeutic effects. However, its biological applications are limited due to its poor aqueous solubility. This emphasizes on the development of new drug delivery system for piperine to improve its in-vivo bioavailability. The present study reports the development and characterization of mucoadhesive nanoemulsion (MNE) containing piperine. MNE formulations were prepared using titration method and characterized in relation to appearance, globule size, zeta potential, thermodynamic stability testing, Ex-vivo evaluation and in-vitro drug permeation study. The MNE of piperine have small globule size (˂ 150nm) and positive zata potential. The spherical surface was confirmed from TEM. pH of MNE was compatible with nasal administration. In vitro release of MNE system in nasal mucosal membrane demonstrated prompt and effective release with more than 75 % of drug release in 4 h.

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