scholarly journals Solubility Enhancement of Aripiprazole by Solid-Self Emulsifying Drug Delivery Systems

2018 ◽  
Vol 10 (4) ◽  
Author(s):  
Amoolya Chennuri ◽  
D. Prasanthi
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery Systems ◽  
Ternary Phase Diagram ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
Delivery Systems ◽  
In Vitro Drug Release ◽  
Pure Drug

Self-emulsifying drug delivery systems are a promising aptemsproach for the formulation of drug compounds with poor aqueous solubility. The main objective of this work was to formulate liquid and solid-self emulsifying drug delivery systems for poorly soluble aripiprazole. Aripiprazole is an atypical anti-psychotic drug used in the management of schizophrenia. The maximum solubility of aripiprazole was found in oleic acid (oil), Tween 80 (surfactant) and Transcutol P (co-surfactant). The L-SMEDDS were formulated in different ratios of oil: s-mix (surfactant: co-surfactant) from 1:9 to 9:1. For the formulation of stable SMEDDS, micro-emulsion region was identified by constructing pseudo-ternary phase diagram by phase titration method. The optimized F4 formulation was at the ratio of 4 (oil): 6 (s-mix). In-vitro drug release of F4 was significantly higher (99.89%) when compared to the pure drug (43.63%) in 1 hour. The F4 formulation had a droplet size of 115.9 nm and zeta potential of -24.9 mV. The pre-compression and post-compression parameters of the optimized S-SMEDDS formulation (SS1) containing Neusilin US2 as solid adsorbent were within the limits as per the official requirements of the Pharmacopoeia. SS1 formulation showed a better drug release (97% in 20 minutes) when compared to the marketed drug (59.75%) and pure drug (19.77%). In conclusion, this study illustrated that adsorption to solid carrier technique could be a useful method to prepare the solid SMEDDS tablets from liquid SMEDDS, which can enhance the solubility and improve the in-vitro drug release of aripiprazole.

scholarly journals A hydrogel based quasi-stationary test system for in vitro dexamethasone release studies for middle ear drug delivery systems

2021 ◽  
Vol 7 (2) ◽  
pp. 692-695
Author(s):  
Thomas Eickner ◽  
Michael Teske ◽  
Natalia Rekowska ◽  
Volkmar Senz ◽  
Klaus-Peter Schmitz ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Drug Concentration ◽  
Drug Delivery Systems ◽  
Test System ◽  
Delivery Systems ◽  
In Vitro Drug Release

Abstract For the investigation of in vitro drug release, methods have been used in which samples of drug delivery systems are immersed in release medium. The medium is used to measure drug concentration via chromatography or photometry. These systems are suitable to investigate the drug release of different systems or to simulate tissue environments. When considering predominantly humid regions, e.g. for drug release into the cochlea through the round window membrane by a drug delivery system placed at that membrane, reproducible in vitro determination of drug release becomes particularly challenging. In this study the development of a system is reported that allows the investigation of the in vitro drug release simulating such conditions. The presented test system consists of an alginate hydrogel in glass vials simulating the biological membrane, which separates the drug delivery system from the medium filled compartment. Saline is used as release medium and injected under the hydrogel. The samples are placed on top of the hydrogel, which slightly contacts the medium surface. The drug concentration in the release medium was determined by HPLC measurements. This system allows for testing the release of dexamethasone without the samples being completely surrounded by medium. The hydrogel mediates the diffusion of the drug by ensuring the contact with the medium. Release was monitored for more than 23 days. The presented concept was successfully designed and manufactured. The system is inexpensive and can be duplicated easily. In this study, it was used to monitor the drug release of dexamethasone from PEGDA700 derived polymer. One challenge that remains to be considered is the low mechanical stability of the hydrogel, which results in a need for repeated manufacturing during the handling of the system.

scholarly journals Preparation of self micro emulsifying drug delivery system(smedds) of poorly soluble drug eprosartan mesylate and its in vitro evaluation

2019 ◽  
Vol 10 (4) ◽  
pp. 3304-3314
Author(s):  
Sabitri Bindhani ◽  
Snehamayee Mohapatra ◽  
Rajat Ku. Kar ◽  
Utkalika Mahapatra
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ternary Phase Diagram ◽  
Tween 80 ◽  
Angiotensin Ii Receptor Blocker ◽  
Angiotensin Ii Receptor ◽  
Pure Drug

Eprosartan Mesylate (EM), an angiotensin II receptor blocker used in the treatment of high blood pressure. But poor solubility and bioavailability (13%) of eprosartan mesylate is a major challenging factor for improving its drug release rate. The main objective of the present work to develop and characterize self micro emulsifying drug delivery system of eprosartan mesylate by using compatible oil, surfactant and co-surfactant. For the selection of oil, surfactant and cosurfactant, solubility screening studies has been carried out. The nine formulations are prepared using peppermint oil, tween 80 and PEG 400. A pseudo ternary phase diagram was prepared to determine the self emulsion region. Four optimized formulations were prepared at 1:1 ratio(a mixture of surfactant and cosurfactant). These four formulations were evaluated for self-emulsification time, droplet size measurement, drug content analysis robustness to dilution test, viscosity analysis, f.t.i.r. The study and in-vitro diffusion studies. The ratio of scosmix (a mixture of surfactant and cosurfactant) of optimized formulation (pf5) was varied to pfa1 (2:1), pf2 (3:1), pfa3 (1:2) and compared with pure drug. The formulation having pfa1 (2:1) shown drug release of 93.13 % in 330 minutes where as pure drug showed a drug release of 54.51% in 330 minutes. So the prepared SMEDDS formulations were efficient and better than the pure drug, and it followed Korsmeyer pappes due to highest r2 value followed by Hixon crowel. It was concluded that incorporation of eprosartan mesylate in selfmicroemulsifying system is a great potential for improving the solubility and dissolution rate of eprosartan mesylate.

scholarly journals Development and Evaluation of Novel Self-Nanoemulsifying Drug Delivery Systems Based on a Homolipid from Capra hircus and Its Admixtures with Melon Oil for the Delivery of Indomethacin

2014 ◽  
Vol 2014 ◽  
pp. 1-9
Author(s):  
Nicholas C. Obitte ◽  
Kenneth C. Ofokansi ◽  
Franklin C. Kenechukwu
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery Systems ◽  
Tween 80 ◽  
Delivery Systems ◽  
Inflammatory Activity ◽  
Capra Hircus ◽  
Anti Inflammatory

In this study, goat fat (Capra hircus) and melon oil were extracted and used to formulate self-nanoemulsifying drug delivery systems (SNEDDS) based on either goat fat alone or its admixture with melon oil by employing escalating ratios of oil(s), surfactant blend (1 : 1 Tween 60 and Tween 80), and cosurfactant (Span 85), with or without carbosil, a glidant, for the delivery of indomethacin. The formulations were encapsulated in hard gelatin capsules and then assessed using isotropicity test, aqueous dilution stability and precipitation propensity, absolute drug content, emulsification time, in vitro drug release, and anti-inflammatory activity. The SNEDDS exhibited low precipitation propensity and excellent stability on copious dilution, as well as high drug release in vitro and in vivo. The inhibition produced by the SNEDDS was comparable to that of indomethacin injection (positive control) for much of the 5 h test period, indicating a high degree of bioavailability of the administered SNEDDS. The absolute drug contents and emulsification times fell within narrow limits. This study has shown that a 1 : 1 ratio of melon oil and goat fat could confer favourable properties with respect to drug release and anti-inflammatory activity on SNEDDS for the delivery of indomethacin, thus encouraging further development of the formulations.

scholarly journals Metronidazole- and Amoxicillin-Loaded PLGA and PCL Nanofibers as Potential Drug Delivery Systems for the Treatment of Periodontitis: In Vitro and In Vivo Evaluations

Biomedicines ◽  
2021 ◽  
Vol 9 (8) ◽  
pp. 975
Author(s):  
Shahla Mirzaeei ◽  
Mahla Mansurian ◽  
Kofi Asare-Addo ◽  
Ali Nokhodchi
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
High Performance ◽  
Drug Delivery Systems ◽  
Periodontal Diseases ◽  
Delivery Systems ◽  
Electrospinning Process ◽  
In Vitro Drug Release

The purpose of this study was to prepare poly (D-L) lactide-co-glycolide (PLGA) and poly ε-caprolactone (PCL) nanofibers containing metronidazole and amoxicillin using an electrospinning process as intrapocket sustained-release drug delivery systems for the treatment of periodontal diseases. Scanning electron microscopy showed that the drug containing PLGA and PCL nanofibers produced from the electrospinning process was uniform and bead-free in morphology. The obtained nanofibers had a strong structure and resisted external tension according to the tensiometry results. The cytotoxicity results indicated acceptable cell viability (>80%). Quantification by high-performance liquid chromatography showed almost complete in vitro drug release between 7 and 9 days, whereas 14 days were required for complete drug release in vivo. No significant signs of irritation or inflammatory reaction were detected after three weeks of subcutaneous implantation of nanofibers in the animal models, thus indicating suitable compatibility. The results therefore suggest that the designed nanofibers can be used as potential commercial formulations in the treatment of periodontitis as controlled-release intrapocket drug delivery systems that can increase patient compliance. This is due to their ability to reduce the frequency of administration from three times daily in a systemic manner to once weekly as local delivery.

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