Bioadhesive analysis of controlled-release systems. I. Fracture and interpenetration analysis in poly(acrylic acid)-containing systems

Ponchel, Gilles; Touchard, Frédéric; Duchêne, Dominique; Peppas, Nikolaos A.

doi:10.1016/0168-3659(87)90004-6

Cited by 212 publications

(72 citation statements)

References 14 publications

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“…Bioadhesion of Carbopol 974P-NF®, an anionic polymer to the intestinal membrane seemed to be because of its partially ionizable carboxylic acid groups. The bioadhesion phenomena of Carbopol 974P-NF® and the membrane tissue composed of two mechanisms, a chemical interaction between functional groups and an interpenetration of the polyacrylic acid chains into the mucus, which was favored by high swelling (12).…”

Section: In Vitro Bioadhesion Studiesmentioning

confidence: 99%

“…The small intestine segment of the rat was rinsed with 0.9% icecold saline and transferred into a beaker filled with oxygenated Tyrode buffer, pH 7.4. Tablets formulations (F1-F3) were incubated in 10 ml Tyrode buffer, in a 16 X 100 mm test tube for 20 minutes, which is the optimal time for the tablet to equilibrate at the swollen state (12). The small intestine was cut into 6 cm segments, everted on a glass rod and tied at one end with a suture thread.…”

Section: In Vitro Tissue Permeability Studiesmentioning

confidence: 99%

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Characterization of a novel lyophilized chitosan hydrogel complex for the controlled release of a highly water soluble drug, niacinamide.

Ma¹,

Prabhu²

2011

Int J Drug Del

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The purpose of this research was to prepare and characterize a novel lyophilized chitosan-based hydrogel complex (termed CS-M) for controlled drug delivery applications using a highly water soluble model drug, niacinamide. Characterization studies were undertaken to evaluate the physical-chemical properties, polymer swelling, in vitro controlled release kinetics, tissue bioadhesion, intestinal permeability and stability of the novel chitosan complex. Additionally, a comparative analysis was conducted with commercial polymers namely, Carbopol 974P-NF® and hydroxypropyl methylcellulose (HPMC K4M). FT-IR and 1 H NMR studies confirmed that despite alteration in physical structure and morphology of the chitosan complex the chemical properties remained unchanged, when compared to the parent chitosan compound. Polymer swelling studies showed consistency in the structural integrity and water uptake of CS-M compared to other polymers which showed inconsistent swelling and disintegration behavior over a 5 h period. In vitro controlled release profiles of CS-M showed a slower, more controlled release rate of niacinamide than other polymers indicating the influence of polymer swelling capacity on water uptake and subsequent drug release. CS-M demonstrated an overall increase in bioadhesion to intestinal tissue when compared to commercial polymers at same concentrations. Similarly, drug transport through everted sac intestinal tissue showed enhanced absorption properties of CS-M when compared to other polymers. Finally, a 3 month accelerated stability study showed all polymers including CS-M to be stable when formulated with niacinamide. Overall, the modified chitosan-based hydrogel polymer, CS-M, demonstrated enhanced characteristics indicating its potential to be used as a controlled release excipient in oral drug formulations.

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Section: In Vitro Bioadhesion Studiesmentioning

confidence: 99%

Section: In Vitro Tissue Permeability Studiesmentioning

confidence: 99%

Characterization of a novel lyophilized chitosan hydrogel complex for the controlled release of a highly water soluble drug, niacinamide.

Ma¹,

Prabhu²

2011

Int J Drug Del

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“…Moderate levels of polymers should, therefore, be employed to yield an apt value of t 50 and ext 18 . (3,14,25). Hydrogels are known to swell readily on contact with the hydrated mucous membrane (14).…”

Section: In Vitro Drug Release Studiesmentioning

confidence: 99%

Formulation development of oral controlled release tablets of hydralazine: Optimization of drug release and bioadhesive characteristics

Singh¹,

Pahuja²,

Kapil³

et al. 2009

Acta Pharmaceutica

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Oral controlled release (CR) systems constitute the most »sought after« route of drug administration since they obviate the need of frequent dosage administration and fluctuating blood levels characterized by saw-tooth kinetics, and hence improve the patient compliance (1). The success of CR devices is invariably hindered by their inability to localize in the selected region(s) of the gastrointestinal (GI) tract (2). Mucoadhesive drug delivery systems (DDS) offer a promising approach for controlled and site-specific delivery to the GI tract by attaching the devices to the mucus and mucosa of the tract via the process of bioadhesion. These mucoadhesive systems are also known to provide intimate contact between the dosage form and the absorptive mucosa, resulting in high drug flux through the absorbing tissue with improved bioavailability (3).Hydralazine (HZ), a directly acting vasodilator, is widely prescribed in the treatment of hypertension and congestive heart failure. Albeit the drug is readily absorbed following oral administration, it is subjected to significant first-pass metabolism (4). Oral bio- The current study involves development of oral bioadhesive hydrophilic matrices of hydralazine hydrochloride, and optimization of their in vitro drug release profile and ex vivo bioadhesion against porcine gastric mucosa. A 3 2 central composite design was employed to systematically optimize the drug delivery formulations containing two polymers, viz., carbomer and hydroxypropyl methyl cellulose. Response surface plots were drawn and optimum formulations were selected by brute force searches. Validation of the formulation optimization study indicated a very high degree of prognostic ability. The study successfully undertook the development of an optimized once-a--day formulation of hydralazine with excellent bioadhesive and controlled release characteristics.

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“…During the experiment, the force was recorded as a function of displacement until the break point. 16 Data collection and calculation were performed by dedicated software (Instron series IX, version 8.32.00). The peak detachment force was used to evaluate the bioadhesive force of the films.…”

Section: In Vitro Bioadhesionmentioning

confidence: 99%

Micromatricial metronidazole benzoate film as a local mucoadhesive delivery system for treatment of periodontal diseases

2007

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The main objective of this study was to develop a local, oral mucoadhesive metronidazole benzoate (MET) delivery system that can be applied and removed by the patient for the treatment of periodontal diseases. Mucoadhesive micromatricial chitosan/poly(ε-caprolactone) (CH/PCL) films and chitosan films were prepared. Thermal behavior, morphology, and particle size measurements were used to evaluate the prepared films. The effect of different molar masses of CH and different ratios of medium Mwt molar mass chitosan (MCH):PCL on water absorption, in vitro bioadhesion, mechanical properties, and in vitro drug release was examined. In vivo performance of the selected formulation was also evaluated. Differential scanning calorimetry examination revealed that MET existed mainly in amorphous form. Under microscopic examination, PCL microparticles were homogeneously dispersed in the films. The use of different molar masses of CH and different ratios of (MCH):PCL affected the size of the entrapped particles. Addition of PCL significantly decreased percentage water uptake and bioadhesion force compared with pure CH film. With regard to mechanical properties, the 2-layered film containing 1:0.625 MCH:PCL had the best tensile properties. At fixed CH:PCL ratio (1:1.25), the slowest drug release was obtained from films containing high molar mass CH. On the other hand, the 2-layered film that consisted of 1:0.625 MCH:PCL had the slowest MET release. In vivo evaluation of the selected film revealed that metronidazole concentration in saliva over 6 hours ranged from 5 to 15 μg/mL, which was within and higher than the reported range of minimum inhibitory concentration for metronidazole. A significant in vitro/in vivo correlation under the adopted experimental conditions was obtained.

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Bioadhesive analysis of controlled-release systems. I. Fracture and interpenetration analysis in poly(acrylic acid)-containing systems

Cited by 212 publications

References 14 publications

Characterization of a novel lyophilized chitosan hydrogel complex for the controlled release of a highly water soluble drug, niacinamide.

Characterization of a novel lyophilized chitosan hydrogel complex for the controlled release of a highly water soluble drug, niacinamide.

Formulation development of oral controlled release tablets of hydralazine: Optimization of drug release and bioadhesive characteristics

Micromatricial metronidazole benzoate film as a local mucoadhesive delivery system for treatment of periodontal diseases

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