Nasal Absorption of Natural Contraceptive Steroids in Rats—Progesterone Absorption

Hussainx, Anwar A.; Hirai, Shinichiro; Bawarshi, Rima

doi:10.1002/jps.2600700435

Cited by 71 publications

(11 citation statements)

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“…Attractive features of nasal drug delivery include the large surface area of the nasal cavity, avoidance of the hepatic first-pass effect, and the relatively high blood flow, which promotes rapid absorption (Hussain, Hirai, and Bawarshi 1981;Faraj et al 1990;Merkkus, Schipper, and Verhoef 1996). Various in vivo and in vitro models on nasal drug delivery have been described in literature (Krishnamoorthy and Mitra 1998;Cornaz and Burri 1994), where in vivo animal models or in vitro excised animal tissue models have been used due to the methodological and ethical limitations associated with use of human specimens.…”

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confidence: 98%

Air-Liquid Interface Culture of Serially Passaged Human Nasal Epithelial Cell Monolayer forIn VitroDrug Transport Studies

et al. 2005

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The objective of this study was to establish a drug transport study using human nasal epithelial (HNE) cell monolayers cultured by the air-liquid interface (ALI) method using serum-free medium (BEGM:DME/F12, 50:50). The cells were developed and characterized in comparison to those that have been previously cultured by the liquid-covered culture (LCC) method. The epithelial cell monolayer cultured by the ALI method resulted in a significantly higher transepithelial electrical resistance value (3,453 +/- 302 ohm x cm(2)) that was maintained (>1,000 ohm x cm(2)) for up to 20 days compared with that cultured by the LCC method. Observation by scanning electron microscopy revealed mature cilia after 2 weeks in the ALI culture, while flatten unhealthy ciliated cells were observed in the LCC method. After 21 days, higher level of MUC5AC and 8 mRNA were expressed in ALI culture which confirmed the secretory differentiation of HNE monolayers in vitro. No significant difference in the permeability coefficients of a model hydrophilic marker ((14)C-mannitol) and a lipophilic drug (budesonide) was observed between the two conditions on day 7. The passage 2-3 of the HNE monolayer using ALI condition retained the morphology and differentiated features of normal epithelium. Thus it would be a suitable model for in vitro nasal drug delivery studies.

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confidence: 98%

Air-Liquid Interface Culture of Serially Passaged Human Nasal Epithelial Cell Monolayer forIn VitroDrug Transport Studies

et al. 2005

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“…The serum levels obtained after intramuscular injec tion of 10 mg P are similar to the 3.3 ng/ml which is widely accepted as evidence of ovulation [8], However, this type of administration is both uncomfortable and impractical for daily use [3], In rats and rhesus monkeys, it has been shown that the systemic bioavailability of P after nasal absorption is sim ilar to that obtained after intravenous administration [9][10][11]. Nasal mucosa may represent an effective route of systemic administration because of its high degree of vas cularization and the fact that the presence of microvillous structures in the epithelium extend the absorption surface [ 12], The effectiveness of this route for the administration of P to menopausal women has already been demon strated [5,6].…”

Section: Discussionmentioning

confidence: 85%

Comparative Study of Progesterone Plasma Levels after Nasal Spray and Intramuscular Administration of Natural Progesterone in Menopausal Women

Cicinelli¹,

Savino²,

Cagnazzo³

et al. 1993

Gynecol Obstet Invest

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11 mg natural progesterone (P) was administered to 20 healthy menopausal women by means of a nasal spray or intramuscular injection. Circulating P levels were calculated at various times after administration. The spray formulation yielded a CMax of 3.75 ng/ml at T_Max = 60 min, the area under the curve (AUC)_0–720 being 1,481.6 ± 343. Intramuscular administration yielded a mean Cm3x of 4.137 ng/ml at T_Max = 240 min, the AUC_0–720 being 2,491.2 ± 540. P absorption was faster through the nasal than through the intramuscular route, but intramuscular administration led to high serum levels for a much longer period.

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“…75 The animal models using sheep 76 , rat 77,78 , rabbit 79,80 , dog 81 and monkey 82 are reported for estimation of nasal absorption. Various studies have reported the usage of ex vivo nasal perfusion models (using sheep and rat).…”

Section: Fig 3: Various Models For Intra Nasal Drug Transport and Abmentioning

confidence: 99%

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2017

IJPSR

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Intra nasal drug delivery system (INDDS) has emerged as a noninvasive alternative for delivering peptides, proteins and other therapeutic agents, specifically to CNS (Central nervous system). This route is well suitable for systemic delivery because of high vasculature, permeability, elimination of hepatic first pass metabolism and low enzymatic environment of the nasal cavity. This route of delivery is especially suited to treat CNS disorders like -neurodegenerative diseases, mood disorders, cognitive dysfunctioning etc., due to drugs ability to directly reach the brain by passing blood brain barrier (BBB). It is also a well suited delivery route for the biotechnological products like DNA plasmids, hormone, proteins, peptides, DNA vaccines to give enhanced bioavailability. A wide variety of therapeutic compounds may be administered intra-nasally for topical, systemic and CNS disorders. In this review, we have focussed on the nasal passage anatomical pathway leading to CNS drug delivery, different factors affecting nasal absorption, bioavailability barriers, vaccines and other therapeutic, biologically active molecules delivered via intra nasal route and strategies to improve nasal absorption. We have also outlined various in vitro and in vivo cellular models for nasal drug absorption and permeability studies.

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Nasal Absorption of Natural Contraceptive Steroids in Rats—Progesterone Absorption

Cited by 71 publications

References 2 publications

Air-Liquid Interface Culture of Serially Passaged Human Nasal Epithelial Cell Monolayer forIn VitroDrug Transport Studies

Air-Liquid Interface Culture of Serially Passaged Human Nasal Epithelial Cell Monolayer forIn VitroDrug Transport Studies

Comparative Study of Progesterone Plasma Levels after Nasal Spray and Intramuscular Administration of Natural Progesterone in Menopausal Women

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