Permeation enhancement effects of leaf materials from different aloe species on in vitro and ex vivo nasal epithelial models

Introduction: The nasal route of drug administration offers an alternative way for oral drug delivery and has the benefit of avoiding first-pass metabolism through drug delivery directly into the systemic circulation. The drug absorption enhancing effects of selected aloe leaf materials have been shown across various delivery routes, but their efficacies in this regard across nasal epithelia have not yet been investigated. The aim of this study was to determine the effects of gel and whole leaf extract materials from three selected aloe species (Aloe vera, Aloe ferox and Aloe muth-muth) on FITC-dextran 4400 permeation across two nasal epithelial models. Methods: Permeation of FITC-dextran 4400 and histological studies were conducted on both RPMI 2650 cell layers and excised sheep nasal mucosa, while toxicity studies were conducted using a neutral red assay on the RPMI 2650 cell model. Results: Significantly increased (P ≤ 0.05) apparent permeability coefficient (Papp) values of FITC-dextran 4400 in the presence of the aloe materials as compared to the control were found with all three aloe species at the highest concentrations (1.5% and 3% w/v) in the RPMI 2650 cell line, while only Aloe muth-muth at the highest concentration exhibited significantly (P ≤ 0.05) higher Papp values across the excised tissue model. Histological and neutral red analysis showed that Aloe vera materials exhibited detrimental effects, Aloe muth-muth only showed slight effects on cell viability and Aloe ferox exhibited no effect on the nasal epithelium. Conclusion: This in vitro study showed for the first time the potential of Aloe ferox and Aloe muth-muth leaf materials to enhance nasal drug delivery without causing damaging effects on the epithelium, while Aloe vera enhanced nasal drug delivery with detrimental effects as determined by means of cytotoxicity assays and histological analysis.

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Investigation of Mucoadhesion and Degradation of PCL and PLGA Microcontainers for Oral Drug Delivery

Polymers ◽

10.3390/polym11111828 ◽

2019 ◽

Vol 11 (11) ◽

pp. 1828 ◽

Cited By ~ 8

Author(s):

Zarmeena Abid ◽

Mette Dalskov Mosgaard ◽

Giorgio Manfroni ◽

Ritika Singh Petersen ◽

Line Hagner Nielsen ◽

...

Keyword(s):

Drug Delivery ◽

Glycolic Acid ◽

Oral Drug Delivery ◽

Ex Vivo ◽

The Other ◽

Oral Drug ◽

Intestinal Tissue ◽

Retention Model ◽

In Vitro Degradation

Microfabricated devices have been introduced as a promising approach to overcome some of the challenges related to oral administration of drugs and, thereby, improve their oral bioavailability. In this study, we fabricate biodegradable microcontainers with different polymers, namely poly-ɛ-caprolactone (PCL), poly(lactic-co-glycolic acid) (PLGA) 50:50 and PLGA 75:25 by hot punching. The mucoadhesion of the microcontainers is assessed with an ex vivo retention model on porcine intestinal tissue. Finally, in vitro degradation studies of the biodegradable microcontainers are completed for six weeks in simulated intestinal medium with the addition of pancreatic enzymes. Through SEM inspection, the PLGA 50:50 microcontainers show the first signs of degradation already after two weeks and complete degradation within four weeks, while the other polymers slowly degrade in the medium over several weeks.

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Preparation and optimization of polymeric micelles as an oral drug delivery system for deferoxamine mesylate: in vitro and ex vivo studies

Research in Pharmaceutical Sciences ◽

10.4103/1735-5362.263554 ◽

2019 ◽

Vol 14 (4) ◽

pp. 293 ◽

Cited By ~ 4

Author(s):

BehzadSharif Makhmal Zadeh ◽

Anayatollah Salimi ◽

Moloud Kazemi

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Polymeric Micelles ◽

Oral Drug Delivery ◽

Ex Vivo ◽

Oral Drug ◽

Deferoxamine Mesylate ◽

Oral Drug Delivery System

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In vitro evaluation of the genotoxicity of poly(anhydride) nanoparticles designed for oral drug delivery

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2017.03.016 ◽

2017 ◽

Vol 523 (1) ◽

pp. 418-426 ◽

Cited By ~ 9

Author(s):

T. Iglesias ◽

M. Dusinska ◽

N. El Yamani ◽

J.M. Irache ◽

A. Azqueta ◽

...

Keyword(s):

Drug Delivery ◽

Oral Drug Delivery ◽

Oral Drug ◽

In Vitro Evaluation

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Preparation, characterization and in-vitro evaluation of bacterial cellulose matrices for oral drug delivery

Cellulose ◽

10.1007/s10570-017-1474-8 ◽

2017 ◽

Vol 24 (11) ◽

pp. 5041-5052 ◽

Cited By ~ 14

Author(s):

Munair Badshah ◽

Hanif Ullah ◽

Shujaat Ali Khan ◽

Joong Kon Park ◽

Taous Khan

Keyword(s):

Drug Delivery ◽

Bacterial Cellulose ◽

Oral Drug Delivery ◽

Oral Drug ◽

In Vitro Evaluation

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FORMULATION AND EVALUATION OF PERINDOPRIL MICROENCAPSULES BY USING DIFFERENT POLYMER

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i2.14899 ◽

2017 ◽

Vol 10 (2) ◽

pp. 153

Author(s):

Leena Jacob ◽

Abhilash Tv ◽

Shajan Abraham

Keyword(s):

Drug Delivery ◽

Particle Size ◽

Release Rate ◽

Oral Drug Delivery ◽

Entrapment Efficiency ◽

Water Soluble ◽

Oral Drug ◽

Percentage Yield ◽

Drug Entrapment Efficiency

Objective: The study was carried out with an objective to achieve a potential sustained release oral drug delivery system of an antihypertensive drug, Perindopril which is a ACE inhibitor having half life of 2 hours. Perindopril is water soluble drug, so we can control or delay the release rate of drug by using release retarding polymers. This may also decrease the toxic side effects by preventing the high initial concentration in the blood.Method: Microcapsules were prepared by solvent evaporation technique using Eudragit L100 and Ethyl cellulose as a retarding agent to control the release rate and magnesium stearate as an inert dispersing carrier to decrease the interfacial tension between lipophilic and hydrophilic phase. Results: Prepared microcapsules were evaluated for the particle size, percentage yield, drug entrapment efficiency, flow property and in vitro drug release for 12 h. Results indicated that the percentage yield, mean particle size, drug entrapment efficiency and the micrometric properties of the microcapsules was influenced by various drug: polymer ratio. The release rate of microcapsules could be controlled as desired by adjusting the combination ratio of dispersing agents to retarding agents.Conclusion:Perindopril microcapsules can be successfully designed to develop sustained drug delivery, that reduces the dosing frequency and their by one can increase the patient compliance.

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EFFECT OF NATURAL AND SYNTHETIC POLYMERS ON THE PROPERTIES OF CANDESARTAN CILEXETIL MATRIX TABLET PREPARED BY DRY GRANULATION

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2016.v9s3.14719 ◽

2016 ◽

Vol 9 (9) ◽

pp. 161

Author(s):

Omar Saeb Salih ◽

Roaa Abdalhameed Nief

Keyword(s):

Drug Delivery ◽

Candesartan Cilexetil ◽

Oral Drug Delivery ◽

In Vitro Release ◽

Oral Drug ◽

Matrix Tablet ◽

Sustained Release Formulation ◽

Weight Variation ◽

Vitro Release

ABSTRACTObjective: The objective of this study is to develop a controlled release matrix tablet of candesartan cilexetil to reduce the frequency of administration,enhance bioavailability and improve patient compliance; a once daily sustained release formulation of candesartan cilexetil is desirable.Methods: The prepared tablets from F1 to F24 were evaluated with different evaluation parameters like weight variation, drug content, friability,hardness, thickness and swelling ability. In vitro release for all formulas were studied depends on the type and amount of each polymer, i.e. (16 mg,32 mg and 48 mg) respectively beside to the combination effect of polymers on the release of the drug from the tablet.Results: In vitro release showed that formula 13 had the faster release (100% after 4 h) which contained acacia (1:1) and the lowest sustain releasewas showed for F7 (73% after 8 h) which contained HPMC K100M (1:1). Formula 1 was an 89 % release after 8 h which contain eudragit RS100; F4was a 100 % release after 5 h which contain Na CMC, F10 was a 100% after 8 h which contain xanthan gum and F16 was a 100 % release after 5 hwhich contain tragacanth polymer. Formula 9 had a lower release than F7 and F8 respectively. Formula 7 can be used for sustain oral drug delivery ofcandesartan cilexetil while Formula 13 can be used in contrary as fast release tablets for faster response.Conclusion: Controlled drug delivery system is promising for less dosing and higher patient compliance.Keywords: Angiotensin II receptor antagonist, Hypertension, Matrix system, Control release.

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Formulation and characterization of a paediatric nanoemulsion dosage form with modified oral drug delivery system for improved dissolution rate of nevirapine

MRS Advances ◽

10.1557/adv.2018.320 ◽

2018 ◽

Vol 3 (37) ◽

pp. 2203-2219 ◽

Cited By ~ 3

Author(s):

Tapiwa E. Manyarara ◽

Star Khoza ◽

Admire Dube ◽

Chiedza C. Maponga

Keyword(s):

Drug Release ◽

Dissolution Rate ◽

Oral Drug Delivery ◽

Cell Model ◽

Oral Drug ◽

Drug Efflux ◽

Inversion Point ◽

Improve Rate

ABSTRACTBackground: The development of appropriate dosage forms for paediatric antiretroviral therapy is key for improved therapeutic outcomes in children. The focus of this study was to improve solubility, dissolution rate, drug release and maintain high drug permeability.Methodology: A nanoemulsion was prepared using emulsion inversion point and evaluated. The nanoemulsion had nevirapine (3% w/w). In vitro drug release studies were performed using dialysis membrane. Permeability studies using the Caco-2 cell model were performed for the formulation.Results: The optimized nevirapine nanoemulsion had a mean droplet size of 36.09±12.27nm, low pdI of 0.598 and zeta potential of -7.87±4.35mV. At pH 2, the nanoemulsion released 76 ± 2 % of nevirapine within 2 h, while at pH 6.4 value representing the small intestine, amount of nevirapine released was 41.6± 4 %. The permeability rate of the nevirapine nanoemulsion was 30.02 x 10-6cm/s and higher than that of propranolol. Efflux ratio was 0.02 indicating low chance of drug efflux occurring.Conclusion: The results showed that a modified liquid drug release formulations of nevirapine could improve rate of dissolution and maintain high permeability and low drug efflux improving bioavailability of nevirapine in vivo.

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Alginate-Coated Thiolated Chitosan Microspheres for an Oral Drug Delivery System In Vitro

Advanced Biomaterials VII - Key Engineering Materials ◽

10.4028/0-87849-436-7.433 ◽

2007 ◽

pp. 433-436

Author(s):

Hu Lin Jiang ◽

Rohidas B. Arote ◽

Ji Shan Quan ◽

Mi Kyong Yoo ◽

You Kyoung Kim ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Oral Drug Delivery ◽

Oral Drug ◽

Thiolated Chitosan ◽

Chitosan Microspheres ◽

Oral Drug Delivery System

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In Vitro and In Vivo Test Methods for the Evaluation of Gastroretentive Dosage Forms

Pharmaceutics ◽

10.3390/pharmaceutics11080416 ◽

2019 ◽

Vol 11 (8) ◽

pp. 416 ◽

Cited By ~ 3

Author(s):

Schneider ◽

Koziolek ◽

Weitschies

Keyword(s):

Drug Delivery ◽

Drug Delivery Systems ◽

Oral Drug Delivery ◽

Test Methods ◽

Delivery Systems ◽

Oral Drug ◽

Gastrointestinal Physiology ◽

In Vivo Test

More than 50 years ago, the first concepts for gastroretentive drug delivery systems were developed. Despite extensive research in this field, there is no single formulation concept for which reliable gastroretention has been demonstrated under different prandial conditions. Thus, gastroretention remains the holy grail of oral drug delivery. One of the major reasons for the various setbacks in this field is the lack of predictive in vitro and in vivo test methods used during preclinical development. In most cases, human gastrointestinal physiology is not properly considered, which leads to the application of inappropriate in vitro and animal models. Moreover, conditions in the stomach are often not fully understood. Important aspects such as the kinetics of fluid volumes, gastric pH or mechanical stresses have to be considered in a realistic manner, otherwise, the gastroretentive potential as well as drug release of novel formulations cannot be assessed correctly in preclinical studies. This review, therefore, highlights the most important aspects of human gastrointestinal physiology and discusses their potential implications for the evaluation of gastroretentive drug delivery systems.

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