Comparative permeability of various chemical markers through human vaginal and buccal mucosa as well as porcine buccal and mouth floor mucosa

Eyk, A D van; Bijl, Pieter van der

doi:10.1016/j.archoralbio.2003.12.002

Cited by 66 publications

(31 citation statements)

References 31 publications

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“…The oral mucosa of pigs resembles that of humans more closely than any other animal in terms of structure and composition (19,20) and therefore porcine buccal mucosa was selected for drug permeation studies. The results of drug permeation from buccal tablets through the porcine buccal mucosa reveal that carvedilol was released from the formulation and permeated through the porcine buccal membrane and could possibly permeate through the human buccal membrane.…”

Section: In Vitro Drug Permeationmentioning

confidence: 99%

Development and in vitro evaluation of buccoadhesive carvedilol tablets

Yamsani¹,

Gannu²,

Kolli³

et al. 2007

Acta Pharmaceutica

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Buccal delivery of drugs provides an attractive alternative to the oral route of drug administration, particularly in overcoming deficiencies associated with the latter mode of administration. Problems such as high first-pass metabolism and drug degradation in the harsh gastrointestinal environment can be circumvented by administering the drug via the buccal route (1-3). Moreover, buccal drug absorption can be promptly terminated in case of toxicity by removing the dosage form from the buccal cavity. It is also possible to administer drugs to patients who cannot be dosed orally to prevent accidental swallowing. Therefore adhesive mucosal dosage forms were suggested for oral delivery, which included adhesive tablets (4-6), adhesive gels (7, 8) and adhesive patches (9, 10). Buccoadhesive tablets of carvedilol were prepared using HPMC K4M, HPMC K15M and Carbopol 934 as mucoadhesive polymers. Fifteen formulations were developed with varying concentrations of polymers. Formulations of the BC or BD series were composed of HPMC K4M or HPMC K15M in ratios of 1:1 to 1:5 whereas in the BE series Carbopol 934 was used (1:0.25 to 1:1.50). The formulations were tested for in vitro drug release, in vitro bioadhesion, moisture absorption and in vitro drug permeation through porcine buccal mucosa. Formulation BC3 showed maximum release of the drug (88.7 ± 0.4%) with the Higuchi model release profile and permeated 21.5 ± 2.9% of the drug (flux 8.35 ± 0.291 µg h -1 cm -2 ) permeation coefficient 1.34 ± 0.05 cm h -1 ) through porcine buccal membrane. BC3 formulation showed 1.62 ± 0.15 N of peak detachment force and 0.24 ± 0.11 mJ of work of adhesion. FTIR results showed no evidence of interaction between the drug and polymers. XRD study revealed that the drug is in crystalline form in the polymer matrix. The results indicate that suitable bioadhesive buccal tablets with desired permeability could be prepared.

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Section: In Vitro Drug Permeationmentioning

confidence: 99%

Development and in vitro evaluation of buccoadhesive carvedilol tablets

Yamsani¹,

Gannu²,

Kolli³

et al. 2007

Acta Pharmaceutica

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“…Prior to use the frozen samples were. thawed and hydrated in PBS (phosphate buffered saline) for 24 hours at 4°C (5,(11)(12).…”

Section: Human Skinmentioning

confidence: 99%

In vitro Skin Permeability of Different Terbinafine Hydrochloride Formulations

et al. 2008

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The objectives of the study are to determine the in vitro permeability of different terbinafine hydrochloride formulations through human skin and to measure the respective concentrations of each formulation within the exposed skin tissue. The permeation of three commercially available 1% terbinafine hydrochloride formulations and two terbinafine hydrochloride solutions of 10 and 20 mg/ml through human skin was investigated using an in vitro continuous flow-through perfusion system. The terbinafine hydrochloride retained in the skin was extracted and analysed. The terbinafine hydrochloride from the different formulations readily diffused into the skin tissue. However, no flux values for any of the terbinafine hydrochloride formulations through the skin into the receptor fluid were found. The mean terbinafine hydrochloride concentrations in the skin after 24 h exposure to the three commercial formulations were 3.589, 1.590 and 4.219 ug/ml respectively. The mean terbinafine hydrochloride concentrations in the skin after 24 h of exposure to the terbinafine hydrochloride solutions (PBS/Methanol 1:1) of 10 and 20 mg/ml were 85.280 and 154.680 ug/m] respectively. The mean terbinafine hydrochloride concentration in the skin exposed to the 10 mg/ml PBS/Methanol solution was higher than those from the three commercial formulations. Terbinafine seems to accumulate in skin/bind to the skin, rather than to diffuse through the skin into the receptor compartment. This unique pharmacokinetic property of terbinafine hydrochloride may enhance its efficacy as topical antifungal and reduce systemic side effects.Dermal and transdermal drug delivery serve as an attractive alternative to conventional drug delivery methods. Topical administration of drugs can be used to achieve systemic or local effects. The barrier properties and the subsequent impermeability of the skin are a considerable problem in the delivery of active compounds both to and through skin. The pharmaceutical industry is therefore investing everincreasing amounts of resources on the development of new products that are able to overcome the barrier properties of the skin (l). Even though the skin is very accessible for drug administration and research, some aspects of transdermal drug penetrations remain unknown.Due to modem high-throughput technologies large numbers of potential drugs are produced by parallel synthesis and combinatorial chemistry. The pharmaceutical industry therefore requires rapid and accurate methods to screen drug leads for tissue permeability potential in the early stages of drug discovery. In vivo human dermal studies are not always feasible due to the invasiveness of biopsies

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“…A better understanding of how the physicochemical properties of different molecules affect their diffusion across the mucosal epithelial barrier layer may be helpful in designing more effective drug products that will have higher absorption rates as well as greater bioavailability (11). Conditions affecting the epithelial integrity of the vaginal mucosa were simulated by heat de-epithelialisation (18)(19)(20). Vaginal mucosa, of which the epithelial layer has become damaged due to various conditions (e.g.…”

Section: Discussionmentioning

confidence: 99%

“…Oe-epithelialised mucosal specimens were prepared by dipping intact mucosa for a period of 30 seconds in 80°C distilled water and the epithelial layer gently removed with tweezers (18)(19). Either intact or de-epithelialised mucosal sections were then mounted in flow-through diffusion cells (exposed areas 0.039 em") as previously described, and six permeation experiments were performed for each permeant molecule tested (20). Tissue disks were equilibrated for 10 min in PBS (pH 7.4) at 20°C in both the donor and acceptor compartments of the diffusion cells prior to each permeability experiment.…”

Section: Permeability Experimentsmentioning

confidence: 99%

Physicochemical Characteristics of Molecules and Their Diffusion across Human Vaginal Mucosa

2008

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The diffusion rate of permeant molecules through mucosal tissue depends on the physicochemical characteristics of the molecules themselves as well as the properties of the tissue. In this study the diffusion kinetics of various molecules was examined through intact as well as de-epithelialised human vaginal mucosa. The molecules studied included tritium-labelled water, 17β-estradiol, reduced-arecoline, vasopressin, oxytocin, bradykinin, tacrolimus, cyclosporin A, dihydro-alprenolol, cimetidine and benzylpenicillin. Freshly harvested human vaginal tissue was frozen in liquid nitrogen and stored at −85°C. A flow-through diffusion apparatus was used for the in vitro permeability studies (24 h, 20°C, 1.5 ml/h). The mean estimated – or mean steady-state flux values for all the molecules studied across intact human vaginal mucosa, were generally found to be lower than those of the corresponding de-epithelialised tissue. Using an F-test and comparing whole curves, statistically significant differences in the diffusion rates of tacrolimus, reduced-arecoline, vasopressin, bradykinin, benzylpenicillin, water and cimetidine were found when comparing intact and de-epithelialised vaginal mucosa. Generally, smaller permeant molecules diffused at a higher rate than larger molecules. The epithelial layer retarded the diffusion rate of molecules carrying charges at physiological pH. Damage to the epithelial layer did not necessarily increase the diffusion rate of all molecules tested and small lipophilic molecules did not necessarily diffuse at higher rates than hydrophilic molecules.

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Comparative permeability of various chemical markers through human vaginal and buccal mucosa as well as porcine buccal and mouth floor mucosa

Cited by 66 publications

References 31 publications

Development and in vitro evaluation of buccoadhesive carvedilol tablets

Development and in vitro evaluation of buccoadhesive carvedilol tablets

In vitro Skin Permeability of Different Terbinafine Hydrochloride Formulations

Physicochemical Characteristics of Molecules and Their Diffusion across Human Vaginal Mucosa

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