Challenges in oral drug delivery: a nano-based strategy to overcome

Viswanathan, Pragasam; Muralidaran, Yuvashree; Ragavan, Gokulakannan

doi:10.1016/b978-0-323-47720-8.00008-0

Cited by 71 publications

(44 citation statements)

References 63 publications

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“…Active pharmaceutical ingredients are especially challenging adsorbate because their bioavailability depends on many aspects that the drug carrier is supposed to maintain. Pharmaceutics usually exhibit low solubility, chemical lability, or poor permeability through biological membranes [ 22 ]. Therefore, the carriers applied have to be stable in aqueous media, harmless in biological systems, and should have a good affinity towards API.…”

Section: Introductionmentioning

confidence: 99%

Design of Paracetamol Delivery Systems Based on Functionalized Ordered Mesoporous Carbons

et al. 2020

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The oxidized ordered mesoporous carbons of cubic and hexagonal structure obtained by two templating methods (soft and hard) were applied for the first time as delivery systems for paracetamol—the most common antipyretic and analgesic drug in the world. The process of carbon oxidation was performed using an acidic ammonium persulfate solution at 60 °C for 6 h. The functionalization was found to reduce the specific surface area and pore volume of carbon materials, but it also led to an increasing number of acidic oxygen-containing functional groups. The most important element and the novelty of the presented study was the evaluation of adsorption and release ability of carbon carriers towards paracetamol. It was revealed that the sorption capacity and the drug release rate were mainly affected by the materials’ textural parameters and the total amount of surface functional groups, notably different in pristine and oxidized samples. The adsorption of paracetamol on the surface of ordered mesoporous carbons occurred according to different mechanisms: donor–acceptor complexes and hydrogen bond formation. The adsorption kinetics was assessed using pseudo-first- and pseudo-second-order models. The regression results indicated that the adsorption kinetics was more accurately represented by the pseudo-second-order model. Paracetamol was adsorbed onto the carbon materials studied following the Langmuir type isotherm. The presence of oxygen-containing functional groups on the surface of ordered mesoporous carbons enhanced the amount of paracetamol adsorbed and its release rate. The optimal drug loading capacity and expected release pattern exhibited oxidized ordered mesoporous carbon with a hexagonal structure obtained by the hard template method.

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Section: Introductionmentioning

confidence: 99%

Design of Paracetamol Delivery Systems Based on Functionalized Ordered Mesoporous Carbons

et al. 2020

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“…Microspheres have an advantage of the reduction of dosing frequency, solubility enhancement of poorly soluble drugs and provide a constant and prolonged therapeutic effect. 3 Fabrication of polymeric microspheres involve three fundamental methods: (1) Interfacial polymerization methods like suspension polymerization, emulsion polymerization, dispersion polymerization and other methods like compressed anti-solvent precipitation and photo-polymerization; (2) emulsion-solvent extraction/ evaporation and (3) extrusion. Prajapati et al (2015) developed highly spherical, smooth, crosslinked chitosan microspheres loaded with progesterone.…”

Section: Microspheresmentioning

confidence: 99%

“…Liquid and solid dosage forms are generally administered orally. 1 With respect to the physical as well as chemical stability of liquids and semi-solids, they can be converted into solid particles (powders or granules) which can be packed into capsules or compacted into tablets by selecting the appropriate particles. Steroids include the drugs used to relieve swelling and inflammation such as prednisolone and cortisone, sex hormones such as testosterone and estradiol, etc.…”

Section: Introductionmentioning

confidence: 99%

Novel Oral Drug Delivery Systems for Steroids: Overview and Recent Updates

Ganapa¹,

Mhatre²,

Raut³

et al. 2020

IJPER

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This review summarises the oral route of drug delivery of steroids. Oral drug delivery is widespread owing to its non-invasive nature which complements high patient compliance. This article summarises the problems associated with oral delivery of steroids including bioavailability. In this review, a brief description of the novel types of drug delivery systems of steroids such as microspheres, nanoparticles, solid lipid nanoparticles, multimatrix tablets, pellet technology, liposomes are presented. The review also presents the latest innovations and advances that have been achieved in recent years.

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“…Complexation is the association between two or more molecules to form a non-bonded entity with a well-defined stoichiometry 2 . Complexation depends on comparatively weak forces like van der waals forces, gas bonding and hydrophobic interactions.…”

Section: Complexationmentioning

confidence: 99%

FORMULATION AND CHARACTERISATION OF AZITHROMYCIN DIHYDRATE INCLUSION COMPLEXES USING DERIVATIVES OF b-CYCLODEXTRINS AS COMPLEXING AGENTS

Maddukuri¹,

Gv²

2019

Int. Res. J. Pharm.

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In the present research, an attempt was made to study enhancement of solubility and bioavailability of azithromycin, a sparingly water soluble macrolide antibiotic, by use of inclusion complexation technique, using 1:1 and 1:2 w/w ratios of three complexing agents-β-cyclodextrin, epichlorohydrin-βcyclodextrin and sulfobutylether cyclodextrin. Two methods were used-solvent evaporation and freeze drying/lyophilisation. Drug-excipients incompatibilities were studied using Fourier transform Infra-red spectroscopy and Differential scanning calorimetry. IR spectra did not show any significant changes in characteristic peaks of pure drug and excipients. DSC thermograms showed characteristic endothermic peaks at respective melting points of pure drug and excipients, thus ruling out of any undesirable interactions. Drug content of all prepared 12 inclusion complexes ranged from 97.4-99.5 %. Prepared inclusion complexes were characterised using In-Vitro dissolution studies, kinetic modelling patterns, Scanning electron microscopy images and X Ray Diffractograms. In Vitro drug profiles showed 96 % drug release for inclusion complexes using Sulfobutyl ether βcyclodextrin, prepared using freeze drying method. From the kinetics, it could be possibly stated that the release from the matrix was through diffusion. The XRD pattern depicted by optimised complexes reveals a decrease in the number of 2θ peaks which probably represents decrease in crystallinity. SEM images also showed the nature of particles to be highly porous. Thus, it can be concluded that, Inclusion complexation technique using freeze drying method, and newer derivatives of β-cyclodextrin as complexing agents has proven to be highly effective in improving bioavailability of poorly water-soluble drugs than β-Cyclodextrin alone.

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Challenges in oral drug delivery: a nano-based strategy to overcome

Cited by 71 publications

References 63 publications

Design of Paracetamol Delivery Systems Based on Functionalized Ordered Mesoporous Carbons

Design of Paracetamol Delivery Systems Based on Functionalized Ordered Mesoporous Carbons

Novel Oral Drug Delivery Systems for Steroids: Overview and Recent Updates

FORMULATION AND CHARACTERISATION OF AZITHROMYCIN DIHYDRATE INCLUSION COMPLEXES USING DERIVATIVES OF b-CYCLODEXTRINS AS COMPLEXING AGENTS

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