Bioadhesive polymers for the peroral delivery of peptide drugs

Lueßen, H.L.; Lehr, Claus‐Michael; Rentel, Claus; Noach, A.B.J.; Boer, Albertus G. de; Verhoef, J.; Junginger, Hans E.

doi:10.1016/0168-3659(94)90078-7

Cited by 138 publications

(50 citation statements)

References 33 publications

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“…The importance of the mucoadhesive properties of chitosan has been reported in works by (Lehr et al, 1992, Fiebrig et al, 1995, Illum et al, 1994, Lueben et al, 1994, Aspden et al, 1996. Chitosan microspheres with small particle sizes less than 5 µm, containing anticancer agents such as 5-fluorouracil (5-FU) (Ohya et al, 1993), and magnetic microspheres (Hassan et al, 1992), have been described for sitespecific delivery.…”

Section: Chitosanmentioning

confidence: 99%

Gastroretentive microparticles for drug delivery applications

Adebisi

Conway

2011

Journal of Microencapsulation

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Many strategies have been proposed to explore the possibility of exploiting gastroretention for drug delivery. Such systems would be useful for local delivery, for drugs that are poorly soluble at higher pH or primarily absorbed from the proximal small intestine. Generally, the requirements of such strategies are that the vehicle maintains controlled drug release and exhibits prolonged residence time in the stomach. Despite widespread reporting of technologies, many have an inherent drawback of variability in transit times. Microparticulate systems, capable of distributing widely through the GI tract, can potentially minimize this variation. While being retained in the stomach, the drug content is released slowly at a desired rate,

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Section: Chitosanmentioning

confidence: 99%

Gastroretentive microparticles for drug delivery applications

Adebisi

Conway

2011

Journal of Microencapsulation

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“…This polymer presents a swelling ability when it is placed within an aqueous media, 5) and mucoadhesivity in the oral cavity [6][7][8] and in the gastrointestinal tract. 9) CS is a well-known polycation that reacts with negatively charged components, either ions or molecules, leading to the formation of polyelectrolyte complex through ionic bridges between polymer chains.…”

Section: )mentioning

confidence: 99%

Mucoadhesive Tablets for Controlled Release of Acyclovir

Ruíz-Caro

Gago-Guillan²,

Otero-Espinar³

et al. 2012

Chem. Pharm. Bull.

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Mucoadhesive chitosan (CS) and/or hydroxypropyl-methylcellulose (HPMC) tablets for gastric drug delivery of acyclovir (ACV) have been developed in order to improve the ACV oral bioavailability. Swelling, bioadhesive and dissolution studies were carried out in two acidic media (pH 1.5 and 4) in order to determine the tablets behaviour in both fed and fasted states. All the designed tablets showed good mucoadhesive properties on gastric mucosa due to the presence of CS and/or HPMC. In vitro dissolution of ACV from tablets was influenced by the swelling behaviour of each polymer. All data release of the studied tablets fitted to Hopfenberg model, which describes drug release from tablets displaying heterogeneous erosion. HPMC and CS/HPMC tablets revealed a sustained release for 24 h, but a complete dissolution of the tablets was not produced at this time. On the contrary, tablets which contained only CS as polymer were able to release the total amount of ACV for 4 h, due to the CS imbibition and erosion processes in pH 1.5 medium. These results allowed us to conclude that CS is the excipient to be chosen to obtain gastroretentive formulations, due to its demonstrated gastric compatibility.Key words acyclovir; chitosan; hydroxypropyl-methylcellulose; mucoadhesivity; drug controlled release; swelling behaviourIn recent years, the excipients choice for drug formulation has focused on natural and biocompatible products. Chitosan (CS) is a biocompatible material obtained from an abundant natural polysaccharide like chitin by deacetylation processes. 1)Several excellent reviews have compiled different methods for obtaining a wide range of chitosans with different deacetylation degrees and molecular weights which affect some of their physico-chemical parameters.2-4) In pharmaceutical technology field CS has found applicability as a potential formulation excipient acting as a disintegrant, binder or tablet coating agent. This polymer presents a swelling ability when it is placed within an aqueous media, 5) and mucoadhesivity in the oral cavity [6][7][8] and in the gastrointestinal tract. 9) CS is a well-known polycation that reacts with negatively charged components, either ions or molecules, leading to the formation of polyelectrolyte complex through ionic bridges between polymer chains. Their mucoadhesive property is mainly based on the ionic interaction with anionic substructures of mucous layer. 10)Hydroxypropyl-methylcellulose (HPMC) is a non-ionic cellulose ether which has methoxylic and hydroxypropoxylic moieties substituted onto the glucose units. Types of HPMC differ by various degrees of substitution of hydroxypropyl (hydrophilic) and methoxy (hydrophobic) groups and hence its versatility to retard drug release of various solubilities due to the ratio of hydroxypropyl to methoxyl content affects the extent of polymer interaction with water.11) This cellulose ether is the hydrophilic and swellable polymer most commonly used for the preparation of oral controlled drug delivery systems. [12][13][14] Upon contact wit...

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“…Chitosan is linear, hydrophilic, positively charged and has mucoadhesive property [108][109][110]. It is an excellent biopolymer for preparation of microparticles [8] and nanoparticles [111] owing to its excellent biocompatibility and biodegradability [112,113]. In vivo, it is degraded by lysozyme [114].…”

Section: Chitosanmentioning

confidence: 99%

“…It was employed as a vehicle for drug delivery for sustained release systems [152][153][154][155] and mucoadhesive formulations [112,113,156]. Chitosan was also used for the improvement of the dissolution rate of poorly soluble drugs [157], drug targeting [158] and enhancement of peptide drug absorption [111,156].…”

Section: Application Of Nanoparticles In Drug Deliverymentioning

confidence: 99%

Biopolymeric nanoparticles

Sundar

Kundu

2010

Science and Technology of Advanced Materials

277

159

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This review on nanoparticles highlights the various biopolymers (proteins and polysaccharides) which have recently revolutionized the world of biocompatible and degradable natural biological materials. The methods of their fabrication, including emulsification, desolvation, coacervation and electrospray drying are described. The characterization of different parameters for a given nanoparticle, such as particle size, surface charge, morphology, stability, structure, cellular uptake, cytotoxicity, drug loading and drug release, is outlined together with the relevant measurement techniques. Applications in the fields of medicine and biotechnology are discussed along with a promising future scope.

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Bioadhesive polymers for the peroral delivery of peptide drugs

Cited by 138 publications

References 33 publications

Gastroretentive microparticles for drug delivery applications

Gastroretentive microparticles for drug delivery applications

Mucoadhesive Tablets for Controlled Release of Acyclovir

Biopolymeric nanoparticles

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