S-protected gellan gum: Decisive approach towards mucoadhesive antimicrobial vaginal films

Jalil, Aamir; Asim, Mulazim Hussain; Le, Nguyet‐Minh Nguyen; Laffleur, Flavia; Matuszczak, Barbara; Tribus, Martina; Bernkop‐Schnürch, Andreas

doi:10.1016/j.ijbiomac.2019.02.092

Cited by 57 publications

(32 citation statements)

References 36 publications

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“…Mucoadhesive properties were further evaluated by the flow-through method. The basic principle of this mucoadhesion test is the quantification of PAA conjugates detaching from the mucosa as a function of time [ 31 ]. The results of the mucoadhesive studies on porcine intestinal mucosa, as illustrated in Figure 11 , showed higher mucoadhesion of s -protected thiolated PAA than unmodified PAA.…”

Section: Resultsmentioning

confidence: 99%

Less Reactive Thiol Ligands: Key towards Highly Mucoadhesive Drug Delivery Systems

et al. 2020

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As less reactive s-protected thiomers can likely interpenetrate the mucus gel layer to a higher extent before getting immobilized via disulfide bond formation with mucins, it was the aim of this study to develop a novel type of s-protected thiomer based on the less reactive substructure cysteine-N-acetyl cysteine (Cys-NAC) in order to obtain improved mucoadhesive properties. For this purpose, two types of s-protected thiomers, polyacrylic acid-cysteine-mercaptonicotinic acid (PAA-Cys-MNA) and polyacrylic acid-cysteine-N-acetyl cysteine (PAA-Cys-NAC), were synthesized and characterized by Fourier-transform infrared spectroscopy (FT-IR) and the quantification of attached disulfide ligands. The viscosity of both products was measured in the presence of NAC and mucus. Both thiomers were also evaluated regarding swelling behavior, tensile studies and retention time on the porcine intestinal mucosa. The FT-IR spectra confirmed the successful attachment of Cys-MNA and Cys-NAC ligands to PAA. The number of attached sulfhydryl groups was in the range of 660–683 µmol/g. The viscosity of both s-protected thiomers increased due to the addition of increasing amounts of NAC. The viscosity of the mucus increased in the presence of 1% PAA-Cys-MNA and PAA-Cys-NAC 5.6- and 10.9-fold, respectively, in comparison to only 1% PAA. Both s-protected thiomers showed higher water uptake than unmodified PAA. The maximum detachment force (MDF) and the total work of adhesion (TWA) increased in the case of PAA-Cys-MNA up to 1.4- and 1.6-fold and up to 2.4- and 2.8-fold in the case of PAA-Cys-NAC. The retention of PAA, PAA-Cys-MNA, and PAA-Cys-NAC on porcine intestinal mucosa was 25%, 49%, and 76% within 3 h, respectively. The results of this study provide evidence that less reactive s-protected thiomers exhibit higher mucoadhesive properties than highly reactive s-protected thiomers.

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Section: Resultsmentioning

confidence: 99%

Less Reactive Thiol Ligands: Key towards Highly Mucoadhesive Drug Delivery Systems

et al. 2020

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“…Mucoadhesive properties of films usually determine their residence on mucosal tissues. Films with good mucoadhesiveness are expected to retain on vaginal mucosa for a longer time and to maintain high drug levels at the site of administration [41]. The tensile method is one of the approaches widely used to evaluate mucoadhesive properties of various formulations, including films [42].…”

Section: Ex Vivo Mucoadhesion Studiesmentioning

confidence: 99%

Chitosan/Poly(2-ethyl-2-oxazoline) Films with Ciprofloxacin for Application in Vaginal Drug Delivery

et al. 2020

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Chitosan (CHI) and chitosan/poly(2-ethyl-2-oxazoline) (CHI/POZ)-based films were prepared by casting from aqueous solutions of polymer blends with different compositions. Ciprofloxacin was used as a model drug in these formulations. The weight, thickness, folding endurance and transparency of blend films were measured and characterised. All films had a uniform thickness (0.06 ± 0.01 mm) and exhibited sufficient flexibility. The surface pHs of films ranged from 3.76 ± 0.49 to 4.14 ± 0.32, which is within the pH range suitable for vaginal applications. The cumulative release of the drug from the films in experiments in vitro was found to be 42 ± 2% and 56 ± 1% for pure CHI and CHI/POZ (40:60) films, respectively. Drug-free chitosan/poly(2-ethyl-2-oxazoline) films showed weak antimicrobial activity against Escherichia coli. Drug-loaded CHI and CHI/POZ films showed good antimicrobial properties against both Gram-positive Staphylococcus aureus and Gram-negative bacteria Escherichia coli. Mucoadhesive properties of these films with respect to freshly excised sheep vaginal mucosa were evaluated using a tensile method. It was established that all films were mucoadhesive, but an increase in POZ content in the blend resulted in a gradual reduction of their ability to stick to vaginal mucosa. These films could potentially find applications in vaginal drug delivery.

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“…42 The film of which has earlier been used for the treatment of oral cancer as a bioadhesive patch and as a film for vaginal delivery of metronidazole. 33,5 A recent study concluded that the povidone-iodine is the most effective antiseptic agent for prevention of postcesarean endometriosis and treatment of vaginal infections. 43 It is commercially available in various formulations, such as solutions, pessaries, and creams.…”

Section: Evaluation Of Gellan Film and Iodine-loaded Poly(silicic Amentioning

confidence: 99%

“…3,4 It is also used as a substitute for agar for culturing microorganisms and for cell immobilization. In pharmaceutical applications it has been evaluated as release retardant matrix, in situ gelling agent, mucoadhesive drug delivery system, 5 and for its bone regeneration property. 6 Gellan gum has excellent mucoadhesive property that is, ability to adhere to the mucosal surface lining the epithelia.…”

Section: Introductionmentioning

confidence: 99%

Iodine‐loaded poly(silicic acid) gellan nanocomposite mucoadhesive film for antibacterial application

Pahwa

Ahuja

2020

J of Applied Polymer Sci

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Iodine‐loaded poly(silicic acid) gellan nanocomposite film was fabricated and evaluated for antibacterial properties. Poly(silicic acid) nanoparticles were synthesized by condensation of silicic acid under alkaline conditions in the presence of polyvinyl pyrrolidone, phosphate ions, and molecular iodine. The nanoparticles were incorporated into gellan dispersion to prepare gellan nanocomposite film using the solvent casting method. The nanocomposite films were characterized by Fourier transformed infrared spectroscopy, thermogravimetric analysis, and X‐ray diffraction studies. The results of characterization studies indicated improved thermal stability and an increase in the degree of crystallinity. The scanning electron micrographs and energy dispersive X‐ray spectrum confirmed the uniform dispersion of silica and iodine in the nanocomposite films. The analysis of physical and mechanical properties revealed the enhanced tensile strength, moisture resistance, and higher folding endurance of poly(silicic acid) gellan nanocomposite films as compared to gellan film. Further, the iodine‐loaded poly(silicic acid) gellan nanocomposite films showed good antibacterial activity against Staphylococcus aureus and Escherichia coli and effective mucoadhesive strength. The results indicate that iodine‐loaded poly(silicic acid) gellan nanocomposite mucoadhesive film can be used for potential antibacterial applications in pharmaceuticals.

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S-protected gellan gum: Decisive approach towards mucoadhesive antimicrobial vaginal films

Cited by 57 publications

References 36 publications

Less Reactive Thiol Ligands: Key towards Highly Mucoadhesive Drug Delivery Systems

Less Reactive Thiol Ligands: Key towards Highly Mucoadhesive Drug Delivery Systems

Chitosan/Poly(2-ethyl-2-oxazoline) Films with Ciprofloxacin for Application in Vaginal Drug Delivery

Iodine‐loaded poly(silicic acid) gellan nanocomposite mucoadhesive film for antibacterial application

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