Evaluation of mucoadhesion for two polyelectrolyte gels in simulated physiological conditions using a rheological method

Hägerström, Helene; Paulsson, Mattias; Edsman, Katarina

doi:10.1016/s0928-0987(99)00070-6

Cited by 109 publications

(50 citation statements)

References 28 publications

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“…Beads obtained from alkaline crosslinking medium showed improved mucoadhesivity; this might be due to (1) the decreased intramolecular cohesivity in gellan chains in the presence of drug and increase in adhesivity with stomach mucosa and (2) induced capillary forces due to channels formed by dissolution of drug (9,27). Chitosan-coated beads showed higher mucoadhesivity with increasing gellan amount, suggesting increased gellan-chitosan cross-linking and, in turn, availability of polymer chains for mucous membrane interactions (29,30). Batch AM8 having higher in vitro mucoadhesivity was further tested for in vivo mucoadhesion where more than 85% beads retained on stomach mucosa after 7 h.…”

Section: Characterization Of Beadsmentioning

confidence: 99%

Stomach-Specific Controlled Release Gellan Beads of Acid-Soluble Drug Prepared by Ionotropic Gelation Method

2010

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Abstract. The purpose of the present work was the development and evaluation of stomach-specific controlled release mucoadhesive drug delivery system prepared by ionotropic gelation of gellan beads, containing acid-soluble drug amoxicillin trihydrate, using 3 2 factorial design with concentration of gellan gum and quantity of drug as variables. The study showed that beads prepared in alkaline cross-linking medium have higher entrapment efficiency than the acidic cross-linking medium. The entrapment efficiency was in the range of 32% to 46% w/w in acidic medium, which increased up to 60% to 90% w/w in alkaline medium. Batches with lowest, medium, and highest drug entrapment were subjected to chitosan coating to form a polyelectrolyte complex film. As polymer concentration increases, entrapment efficiency and particle size increases. Scanning electron microscopy revealed spherical but rough surface due to leaching of drug in acidic cross-linking solution, dense spherical structure in alkaline cross-linking solution, and rough surface of chitosan-coated beads with minor wrinkles. The in vitro drug release up to 7 h in a controlled manner following the Peppas model (r=0.9998). In vitro and in vivo mucoadhesivity study showed that beads have good mucoadhesivity and more than 85% beads remained adhered to stomach mucosa of albino rat even after 7 h. In vitro growth inhibition study showed complete eradication of Helicobacter pylori. These results indicate that stomach-specific controlled release mucoadhesive system of amoxicillin gellan beads may be useful in H. pylori treatment.

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Section: Characterization Of Beadsmentioning

confidence: 99%

Stomach-Specific Controlled Release Gellan Beads of Acid-Soluble Drug Prepared by Ionotropic Gelation Method

2010

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“…If the hydration value exceeds 83％, it indicates that the cornea has suŠered some damage. 18) As shown in Table 2, the hydration value from fresh corneas was measured as 78.31± 1.24％. The values of all the test groups increased slightly from those of fresh corneas, but there was no It is the rate of the w/v concentrations of Carbopol980NF and HPMC E4M.…”

Section: Phase-solubility Studiesmentioning

confidence: 90%

“…The composition of STF was sodium chloride 0.670 g, sodium bicarbonate 0.200 g, calcium chloride･2H 2 O 0.008 g, and bi-distilled water q.s. 100.0 g. 18) Physiological pH (7.4 ±0.1) was adjusted by adding the required amount of 0.1 N HCl.…”

Section: Sample Preparationmentioning

confidence: 99%

Preparation and Evaluation of a Carbopol®/HPMC-based In Situ Gelling Ophthalmic System for Puerarin

Chen

et al. 2007

YAKUGAKU ZASSHI

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The purpose of this study was to develop a pH-triggered in situ gelling vehicle for ophthalmic delivery of puerarin. The eŠect of hydroxypropyl-b-cyclodextrin (HP-b-CD) on the aqueous solubility and in vitro corneal permeation of puerarin was also investigated. The puerarin solubility increased linearly and proportionally to the HP-b-CD concentrations and 5％ (w/v) HP-b-CD enhanced its ocular permeability signiˆcantly. Carbopol980NF was used as the gelling agent in combination with HPMC (Methocel E4M) which acted as a viscosity-enhancing agent. The optimum concentrations of Carbopol980NF and HPMC E4M for the in situ gel-forming delivery systems were 0.1％ (w/v) and 0.4％ (w/v), respectively. When these two vehicles were combined, an in situ gel that had the appropriate gel strength and gelling capacity under physiological condition could be obtained. This combined solution could ‰ow freely under nonphysiological condition and showed the character of pseudoplastic ‰uid under both conditions. Both in vitro release studies and in vivo pharmacokinetics studies indicated that the combined polymer systems performed better in retaining puerarin than puerarin eye drops did. These results demonstrate that the Carbopol980NF/HPMC E4M can be a viable alternative to conventional puerarin eye drops to enhance ocular bioavailability and patient compliance.

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“…28,29 In vitro release profiles of dirithromycin were investigated in freshly prepared simulated tear fluid (STF) at pH 7.4. [30][31][32] Briefly, spray-dried nanoparticles containing 5.0 mg dirithromycin were put in dialysis bags. Bags were closed tightly from both ends and were immersed in the dissolution medium containing 30 mL STF at 34°C±1°C on a water bath using continuous magnetic stirrer with a stirring rate of 150 rpm.…”

Section: Drug Loading and Encapsulation Efficiency (Ee) Were Calculatmentioning

confidence: 99%

Ocular Application of Dirithromycin Incorporated Polymeric Nanoparticles: an In Vitro Evaluation

Başaran¹

2017

tjps

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ÖZAmaç: Özellikle gözyaşı üretimi ve kırpma refleksleri gibi gözün koruyucu mekanizmalarına bağlı olarak göze topik olarak uygulanan formülasyonların göz yüzeyinden hızla uzaklaştırılması ve korneal yüzeyden verimsiz absorbsiyonu söz konusu olmaktadır. Prekorneal tutunma süresinin ve korneal permeabilitenin arttırılması ile oküler biyoyararlanımın arttırılmasında kolloidal ilaç taşıyıcı sistemler büyük önem taşımaktadır. Bu çalışmada antibakteriyel etkili bir madde olan diritromisin yüklü Kollidon ® SR yapılı polimerik nanopartiküller şiddetli oküler bakteriyel enfeksiyonların etkin tedavisi amacı ile hazırlanmıştır. Gereç ve Yöntemler: Bu çalışmada diritromisin Kollidon ® SR yapılı polimerik nanopartiküllere püskürterek kurutma yöntemi ile yüklenmiştir. Nanopartiküllerin in vitro karakteristik özellikleri üç farklı ortamda üç ay süresince detaylı olarak incelenmiştir. Bulgular: İn vitro analiz sonuçları parçacıkların üç aylık saklama süresince karakteristik özelliklerini koruduklarını göstermiştir. Sonuç: Kollidon ® SR yapılı polimerik nanopartiküllerin şiddetli oküler bakteriyel enfeksiyonların diritromisin ile tedavisinde oldukça etkili ilaç taşıyıcı sistem adayları olduklarını göstermiştir. Anahtar kelimeler: Diritromisin, Kollidon ® SR, polimerik nanopartiküller, oküler ilaç taşıyıcı sistemler Objectives: Ocular drug delivery is a difficult challenge especially with topical intillation which results in rapid drainage and non-productive drug absorption. For the improvement of the pre-corneal retention time and enhancing the corneal permeability, colloidal drug delivery systems play an important role in enhancement of the ocular bioavailability. In this study, dirithromycin incorporated Kollidon ® SR-based polymeric nanoparticles, an antibacterial agent, were formulated for the efficient treatment of severe ocular bacterial infections. Materials and Methods: In this study, dirithromycin was incorporated into the Kollidon ® SR-based nanoparticles by spray drying method. In vitro characteristic properties were evaluated in detail during the storage period of three months at three different conditions. Results: The results of in vitro analyses revealed that characteristic properties of the particles were remained unchanged during the storage period of three months. Conclusion: Kollidon ® SR-based polymeric nanoparticles are good candidates for drug delivery systems in the treatment of severe ocular bacterial infections with dirithromycin.

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Evaluation of mucoadhesion for two polyelectrolyte gels in simulated physiological conditions using a rheological method

Cited by 109 publications

References 28 publications

Stomach-Specific Controlled Release Gellan Beads of Acid-Soluble Drug Prepared by Ionotropic Gelation Method

Stomach-Specific Controlled Release Gellan Beads of Acid-Soluble Drug Prepared by Ionotropic Gelation Method

Preparation and Evaluation of a Carbopol<sup>®</sup>/HPMC-based <i>In Situ</i> Gelling Ophthalmic System for Puerarin

Ocular Application of Dirithromycin Incorporated Polymeric Nanoparticles: an <i>In Vitro</i> Evaluation

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