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Ilan, Ehud; Amselem, Shimon; Weisspapir, Michael; Schwarz, Joseph S.; Yogev, Ayala; Zawoznik, Eduardo; Friedman, Doron

doi:10.1023/a:1016023111248

Cited by 26 publications

(5 citation statements)

References 9 publications

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“…The results observed were an extensive and persistent fall in plasma calcium level after oral administration of the mucoadhesive emulsion, indicating the absorption of EC from the emulsions adhered to the mucosa, as suggested by many researchers. 4,5,9,26) In the experiment using the emulsions containing FD-4, in fact, a strong mucoadhesion of mucoadhesive emulsion to the mucosa was demonstrated (Table 3). Thus, the usefulness of mucoadhesive emulsions for the oral administration of EC was demonstrated.…”

Section: Discussionmentioning

confidence: 95%

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Oral Delivery of Synthetic Eel Calcitonin, Elcatonin, in Rats.

Ogiso

Funahashi

Tsukioka

et al. 2001

Biological & Pharmaceutical Bulletin

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Recent advances in biotechnology have made available large numbers of bioactive peptides, which may have therapeutic potential. Many polypeptides are susceptible to degradation by proteolytic enzymes and are poorly absorbed in the gastrointestinal tract. With very few exceptions of small and cyclic peptides such as cyclosporin, most peptide drugs have low oral bioavailabilities with typical values of less than 1%. 1)There are many examples of the use of particulate systems which attempt to achieve systemic delivery of peptide drugs via the intestinal tract. These include nanoparticles, 2-5) microspheres, 2,6) liposomes 7,8) and multiple emulsions 9,10) that shield peptide drugs from enzymatic attack.Elcatonin (EC), synthetic [Asu 1,7 ]-eel calcitonin and a hypocalcemic peptide, has been used for the treatment of Paget's disease as well as certain types of osteoporosis. 11)The usual routes of its administration are subcutaneous and intramuscular. On the other hand, intranasal administration of human calcitonin (hCT) and salmon calcitonin (sCT) has proved effective in the management of Paget's disease 12,13) and postmenopausal osteoporosis.14-16) The colonic absorption of 125 I-hCT in humans 17) and the rectal absorption of EC in rabbits 18) have been recently evaluated, estimating the hypocalcemic effect. However, among all alternative routes for administration of EC and calcitonin, the oral route is a suitable alternative, because it offers improved convenience and patient compliance. It is of particular interest that EC has considerable resistance to enzymatic degradation conformationally, 19) a property which is beneficial to the oral administration. In order to meet these challenges we aimed to develop an oral dosage form whose EC bioavailability would be sufficient to promote the hypocalcemic response at the same level as obtained with parental dosage forms.This paper describes an approach to oral administration of EC in rats. We have estimated the intestinal absorption of EC coadministered with some protease inhibitors and absorption enhancers. In addition, to realize the oral delivery of EC, mucoadhesive W/O/W multiple emulsions and a capsule of the peptide were prepared and the hypocalcemic effects were evaluated in rats after their oral administration. We discuss the possibility of oral delivery of EC for the treatment of disease based on the results obtained. Treatment of Animals Male Wistar rats (Japan SLC, Shizuoka, Japan), weighing 200-240 g, were used throughout this experiment. The animals were maintained on MF diet (Oriental Yeast Co., Tokyo) for 3-4 d prior to the experiment. A group of 3-7 rats was randomly selected from the population. On the day before the experiment, the rat jugular vein was cannulated with silicon tubing, 20) and the rat was fasted overnight (for 16 h). MATERIALS AND METHODS Materials Preparation of W/O/W Multiple Emulsions and Mucoadhesive EmulsionsThe multiple emulsions were prepared by a two-step process.21) The primary emulsion con- * To whom correspondence should be add...

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Section: Discussionmentioning

confidence: 95%

“…Considerable attempts have been made to develop an efficient drug delivery system for the oral administration of these peptides. Trials for the oral route have used mucoadhesive nanoparticles, 4,5) W/O/W multiple emulsions, 10,21,25) mucoadhesive submicron emulsions 9,26) and surface-coated liposomes.…”

Section: Discussionmentioning

confidence: 99%

Oral Delivery of Synthetic Eel Calcitonin, Elcatonin, in Rats.

Ogiso

Funahashi

Tsukioka

et al. 2001

Biological & Pharmaceutical Bulletin

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“…Studies have shown that the oral absorption of vitamin A, vitamin D 3 and insulin was improved by administering them as milk fat globule membrane emulsions [7]. Improved oral delivery of cefpodoxime proxetil [8] and desmopressin [9] from submicron emulsions has been reported. Relatively higher oral availability of drugs contained in cationic emulsions was also reported [10].…”

Section: Myers and Stellamentioning

confidence: 99%

Improved Oral Absorption of Carbamazepine from 1-O-Alkylglycerol Stabilized o/w Nanoemulsions

Madhusudhan¹,

Rambhau²,

Apte³

et al. 2007

CNANO

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Absorption of carbamazepine (CBZ) from gastrointestinal tract is slow and erratic. In order to improve oral absorption of CBZ, 1-O-alkylglycerol/lecithin stabilized o/w nanoemulsions incorporating CBZ in oil phase were prepared and characterized. Nanoemulsions had a size around 200 nm. Their oral bioavailability in rabbits and in situ intestinal absorption in rats were evaluated. In in situ studies, the test and control systems were charged into intestine and instead of lumenal samples, blood samples from tail vein were analyzed for CBZ content. These results indicated faster rate and higher extent of absorption for nanoemulsions than control (a micron sized aqueous CBZ suspension). The high rate of release from and adherence of nano-oil particles to mucosa seems to have enhanced absorption of CBZ in this model. Among nanoemulsions 1-O-decylglycerol/lecithin stabilized system showed faster rate of absorption, higher Cmax and area under the curve (AUC). Improvement in oral absorption of CBZ from nanoemulsions was also evident from the bioavailability study conducted on rabbits. Peak serum concentration (Cmax) and AUC were higher for nanoemulsions than control. This study indicated increase in absorption and decrease in disposition of CBZ when administered as nanoemulsions. Broadly the globule size and permeabilization effect due to 1-O-alkylglycerols seem to be the factors responsible for enhanced absorption due to nanoemulsions in in situ and in vivo experiments. However the permeability effect of 1-O-alkylglycerol was prominent only in in situ experiments.

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“…Based on the promising potential and good acceptance of orally administered drug delivery systems, some recent research has examined alternative application methods for desmopressin to enhance BA. By using a mucoadhesive submicron emulsion, a 12-fold increase in the BA of DDAVP was observed compared with a pure saline solution ( Ilan et al, 1996 ). The incorporation of DDAVP into mucoadhesive, multi-layer film preparations has also been investigated ( Lindert, 2016 ).…”

Section: Introductionmentioning

confidence: 99%

Development and evaluation of a composite dosage form containing desmopressin acetate for buccal administration

Kottke

Burckhardt

Knaab

et al. 2021

International Journal of Pharmaceutics: X

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Desmopressin acetate (DDAVP) is an oligopeptide indicated for the treatment of primary nocturnal enuresis, for example. The poor oral bioavailability of DDAVP accelerated a shift to alternative routes of administration like nasal and oromucosal, whereby nasal administration results in high fluctuations increasing the risk of undesirable side effects. Aim of the study was to use a new composite dosage form (solid matrix attached to a bilayer mucoadhesive film) to make DDAVP available via oromucosal route, reducing the risk of undesirable side effects through precise dosing. DDAVP was incorporated into a solid matrix in the form of a minitablet, and both direct tableting (AV > 30) and granulation followed by tableting (AV = 17.86) were compared. Minitablets with content uniformity could only be obtained by granulation and loss supplementation (AV = 11.27) with immediate drug release (>80% after 7–8 min) and rapid disintegration (<49 s). Permeation studies were performed with a clinically relevant dose (200 μg) in a time interval of up to one hour, resulting in apparent permeation coefficients of 4.90 × 10 −6 cm/s (minitablet) and 2.04 × 10 −6 cm/s (composite). Comparable fluctuations showed no inferiority of composite and minitablet regarding dosing accuracy. Thus, a step towards controlled and dose-accurate transmucosal delivery of systemically active DDAVP could be achieved.

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Cited by 26 publications

References 9 publications

Oral Delivery of Synthetic Eel Calcitonin, Elcatonin, in Rats.

Oral Delivery of Synthetic Eel Calcitonin, Elcatonin, in Rats.

Improved Oral Absorption of Carbamazepine from 1-O-Alkylglycerol Stabilized o/w Nanoemulsions

Development and evaluation of a composite dosage form containing desmopressin acetate for buccal administration

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