Synthesis and Characterization of Thiolated Gum Ghatti as a Novel Excipient: Development of Compression Coated Mu-Coadhesive Tablets of Domperidone

Background: Mucoadhesive polymers represent a major part of site-specific and localized retention strategies in oral drug delivery. Present research was designed to synthesize and characterize a novel mucoadhesive carbohydrate polymer (thiolated gum ghatti; TGG) which was further employed to fabricate mucoadhesive tablets of domperidone using an industrially viable compression coating technique. Methods: Thiolation of gum ghatti was achieved by the ester formation (esterification) between hydroxyl group and carboxyl group of gum ghatti and thioglycolic acid. Results: TGG was characterized by various physico-chemical techniques such as FTIR, XRD, SEM and DSC techniques. In rheological studies, the observed viscosities of pure gum-mucin were 45.45 and 71.75 mPas and that of thiolated gum were 78.7 and 112.58 mPas respectively in water and simulated gastric fluid. Signifi-cant increase in viscosity for thiolated gum may be attributed to increased macromolecular interactions responsible for enhanced mucoadhesive potential of thiolated gum. In-silico studies corroborate the role of mucin gum interaction and energetic stabilization for en-hanced mucoadhesion properties of thiolated gum. Ex-vivo mucoadhesion strength of gum ghatti and thiolated gum ghatti coated tablets was found to be ranging between 4.67± 0.79 to 8.99± 0.75 g and 11.76± 1.34 to 18.83± 2.07 g respectively. Conclusion: Thiolated gum ghatti may be regarded as a promising polymer for developing different mucoadhesive drug delivery systems.

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Evaluation of Ibuprofen/Montmorillonite Nano-Clay Composites as an Oral Drug Delivery System and In-Vitro Drug Release Performance

Journal of Nanoscience and Nanotechnology ◽

10.1166/jnn.2021.19167 ◽

2021 ◽

Vol 21 (7) ◽

pp. 3651-3655

Author(s):

Woo Chang Kwon ◽

Moonhee Choi ◽

Kyung Chan Kang ◽

Dong Hyun Kim

Keyword(s):

Oral Drug Delivery ◽

Gastric Fluid ◽

Controlled Delivery ◽

Simulated Gastric Fluid ◽

Oral Drug ◽

Simulated Intestinal Fluid ◽

Oral Drug Delivery System ◽

Nano Clay ◽

Best Fitting

A formulation for controlled delivery of ibuprofen (IBU) involving montmorillonite (MMT) nanoclays has been proposed. The present work has investigated the beneficial effect of MMT in improving controlled delivery of IBU. The intercalation of IBU into the interlayer of MMT was studied under different processing conditions such as reaction time and initial concentration of IBU. To characterize the IBU/MMT composites, X-ray diffraction (XRD) and Fourier transform infrared spectra (FTIR) were performed. The release behavior of IBU from IBU/MMT composites have been investigated under vitro conditions using buffer media of simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 7.4) at 37 °C. Controlled release of IBU from IBU/MMT composite has been observed during in vitro release experiments. Different mathematical models were used for fitting our experimental results, among them the best fitting was found for Higuchi equation based on the parabolic diffusion process.

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

Journal of Herbmed Pharmacology ◽

10.34172/jhp.2020.45 ◽

2020 ◽

Vol 9 (4) ◽

pp. 355-365

Author(s):

Werner Gerber ◽

Dewald Steyn ◽

Awie Kotzé ◽

Hanna Svitina ◽

Ché Weldon ◽

...

Keyword(s):

Drug Delivery ◽

Oral Drug Delivery ◽

Cell Model ◽

Ex Vivo ◽

Aloe Vera ◽

Neutral Red ◽

Oral Drug ◽

Nasal Drug Delivery ◽

Aloe Ferox

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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Enhancement of bioavailability through transdermal drug delivery of paliperidone palmitate-loaded nanostructured lipid carriers

Therapeutic Delivery ◽

10.4155/tde-2021-0036 ◽

2021 ◽

Author(s):

Shilpa Raval ◽

Parva Jani ◽

Pravin Patil ◽

Parth Thakkar ◽

Krutika Sawant

Keyword(s):

Drug Delivery ◽

Oral Drug Delivery ◽

Ex Vivo ◽

Drug Loading ◽

Physicochemical Characterization ◽

Nanostructured Lipid Carriers ◽

Paliperidone Palmitate ◽

Oral Drug ◽

Pharmacokinetic Studies ◽

Transdermal Patch

Aim: The work describes enhanced bioavailability of paliperidone palmitate through transdermal delivery using nanostructured lipid carriers (NLC). Materials & methods: NLCs were formulated by nanoprecipitation method followed by incorporation in transdermal patch and physicochemical characterization. Results: NLCs showed high percentage entrapment efficiency of 83.44 ± 0.8%, drug loading of 24.75 ± 1.10% (w/w), particle size of 173.8 ± 3.25 nm, polydispersity index of 0.143 ± 0.05 and zeta potential of -15.9 ± 0.75 mV. In vitro and ex vivo studies indicated zero-order controlled drug release from NLCs and transdermal patch up to 48 h. Pharmacokinetic studies indicated 1.76-fold enhanced bioavailability by transdermal route as compared with oral drug delivery. Conclusion: From the results, it was concluded that drug-loaded NLCs-transdermal patch is promising drug delivery system for poorly bioavailable drugs.

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Bolalipid-Doped Liposomes: Can Bolalipids Increase the Integrity of Liposomes Exposed to Gastrointestinal Fluids?

Pharmaceutics ◽

10.3390/pharmaceutics11120646 ◽

2019 ◽

Vol 11 (12) ◽

pp. 646 ◽

Cited By ~ 1

Author(s):

Sindy Müller ◽

Kai Gruhle ◽

Annette Meister ◽

Gerd Hause ◽

Simon Drescher

Keyword(s):

Oral Drug Delivery ◽

Lipid Vesicles ◽

Gastric Fluid ◽

Simulated Gastric Fluid ◽

Oral Drug ◽

Single Chain ◽

Drug Delivery Vehicles ◽

The Stability ◽

Archaeal Lipids ◽

Calcein Release

The use of archaeal lipids and their artificial analogues, also known as bolalipids, represents a promising approach for the stabilization of classical lipid vesicles for oral application. In a previous study, we investigated the mixing behavior of three single-chain alkyl-branched bolalipids PC-C32(1,32Cn)-PC (n = 3, 6, 9) with either saturated or unsaturated phosphatidyl-cholines. We proved, that the bolalipids PC-C32(1,32C6)-PC and PC-C32(1,32C9)-PC show miscibility with 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) and 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC). In the present work, we extended our vesicle system to natural lipid mixtures using phosphatidylcholine from soy beans, and we investigated the effect of incorporated bolalipids on the integrity of these mixed liposomes (bolasomes) in different gastrointestinal fluids using a dithionite assay and a calcein release assay in combination with particle size measurements. Finally, we also studied the retention of calcein within the bolasomes during freeze-drying. As a main result, we could show that in particular PC-C32(1,32C6)-PC is able to increase the stability of bolasomes in simulated gastric fluid—a prerequisite for the further use of liposomes as oral drug delivery vehicles.

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Preparation and Charaterization of DAM-1 type Materials

MRS Proceedings ◽

10.1557/proc-662-nn6.5 ◽

2000 ◽

Vol 662 ◽

Author(s):

Decio Coutinho ◽

Ying Ma ◽

Kenneth J. Balkus

Keyword(s):

Vitamin E ◽

Oral Delivery ◽

Oral Drug Delivery ◽

Gastric Fluid ◽

Simulated Gastric Fluid ◽

Oral Drug ◽

Preliminary Evaluation ◽

Structure Directing Agent ◽

Vitamin E Tpgs ◽

Gel Composition

AbstractVitamin E TPGS was found to be an effective structure-directing agent for the preparation of both hexagonal all silica DAM-1 and the alumina analog, Al-DAM-1. These free flowing powders offer many advantages in the handling and oral delivery of the sticky vitamin E TPGS. Upon exposure to simulated gastric fluid, the Al-DAM-1 host molecular sieve is dissolved releasing the vitamin E TPGS. As much as 0.6 grams of vitamin E TPGS can be immobilized into 1 gram of Al-DAM-1. Vitamin E TPGS also templates highly ordered mesoporous DAM-1 with tunable morphologies such as hexagons (various lengths), gyroids, rods, spheres and discoids depending upon the temperature and gel composition. Characterization of these composites as well as a preliminary evaluation of Al-DAM-1 as an oral drug delivery system under physiological conditions is presented.

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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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Applications of Ion Exchange Resin in Oral Drug Delivery Systems

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v7i03.9556 ◽

2017 ◽

Vol 7 (03) ◽

Author(s):

Kathpalia Harsha ◽

Das Sukanya

Keyword(s):

Drug Delivery ◽

Ion Exchange ◽

Drug Delivery Systems ◽

Oral Drug Delivery ◽

Physical Stability ◽

Delivery Systems ◽

Oral Drug ◽

Ion Exchange Resins ◽

Exchange Resins ◽

Oral Drug Delivery Systems

Ion Exchange Resins (IER) are insoluble polymers having styrene divinylbenzene copolymer backbone that contain acidic or basic functional groups and have the ability to exchange counter ions with the surrounding aqueous solutions. From the past many years they have been widely used for purification and softening of water and in chromatographic columns, however recently their use in pharmaceutical industry has gained considerable importance. Due to the physical stability and inert nature of the resins, they can be used as a versatile vehicle to design several modified release dosage forms The ionizable drug is complexed with the resin owing to the property of ion exchange. This resin complex dissociatesin vivo to release the drug. Based on the dissociation strength of the drug from the drug resin complex, various release patterns can be achieved. Many formulation glitches can be circumvented using ion exchange resins such as bitter taste and deliquescence. These resins also aid in enhancing disintegrationand stability of formulation. This review focuses on different types of ion exchange resins, their preparation methods, chemistry, properties, incompatibilities and their application in various oral drug delivery systems as well as highlighting their use as therapeutic agents.

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