Optimization of systemic nasal drug delivery with pharmaceutical excipients

Behl, Christian; Pimplaskar, H.K; Sileno, Anthony; Xia, Wenquan; Gries, W.J; deMeireles, J.C; Romeo, V. D.

doi:10.1016/s0169-409x(97)00064-1

Cited by 83 publications

(27 citation statements)

References 99 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…The drug, therefore, must absorb and/or act quickly. Formulation changes, such as using absorption enhancers (Behl et al 1998b ;Costantino et al 2007 ;Na et al 2010 ) and using mucoadhesives to increase residence time (Ugwoke et al 2005 ), are actively being researched in order to take advantage of benefi ts of nasal drug delivery.…”

Section: Challenges Of Nasal Drug Deliverymentioning

confidence: 99%

Considerations for the Development of Nasal Dosage Forms

Ehrick¹,

Shah²,

Shaw³

et al. 2013

AAPS Advances in the Pharmaceutical Sciences Series

View full text Add to dashboard Cite

The anatomy and physiology of the nasal cavity provide unique advantages for accessing targets for local, systemic, and potentially central nervous system drug delivery. This chapter discusses these advantages and the challenges that must be overcome to reach these targets. The chapter then comprehensively reviews nasal dosage forms, analytical testing, and regulatory requirements in the context of existing nasal spray products. Since nasal sprays are moving towards being preservativefree, the chapter covers specialized methods of achieving a sterile product, namely, formulation strategies, manufacturing strategies, and the device landscape that support this upcoming platform. Finally, the chapter reviews various pathways for regulatory approval around the world, for brand and generic, with particular emphasis on the growing acceptance of in vitro data for locally acting nasal spray products.

show abstract

Section: Challenges Of Nasal Drug Deliverymentioning

confidence: 99%

Considerations for the Development of Nasal Dosage Forms

Ehrick¹,

Shah²,

Shaw³

et al. 2013

AAPS Advances in the Pharmaceutical Sciences Series

View full text Add to dashboard Cite

show abstract

“…Co., St Louis, MO, USA) was used as an optimizer of nasal leptin absorption. 15,16 The 0.1 or 0.5% LPC was dissolved in 10% ethanol containing distilled water. Recombinant mouse leptin (0.5 mg/20 ml) (R&D Systems, Inc., Minneapolis, MN, USA) was dissolved in 10% ethanol containing distilled water with or without LPC for i.n.…”

Section: Animalsmentioning

confidence: 99%

“…leptin administration may be more effective than peripheral leptin administration in activation of the satiety center in the hypothalamus and inhibition of appetite in rodents. In addition, we investigated the effects of an optimizer, lysophosphatidylcholine (LPC), 15,16 on the transport of leptin to the systemic circulation and intracerebrospinal space.Materials and methods…”

Section: Introductionmentioning

confidence: 99%

Inhibition of appetite by nasal leptin administration in rats

et al. 2005

View full text Add to dashboard Cite

OBJECTIVE: Leptin inhibits appetite and reduces body weight. However, subcutaneous leptin administration is not very effective on weight reduction. The present studies were undertaken to test the hypotheses that nasally administered leptin effectively accesses to the brain and inhibits appetite. METHODS: Recombinant leptin (0.5 mg/rat) was administered into the bilateral nasal spaces of rats (i.n.). Changes in serum immunoreactive leptin (IRL) and cerebrospinal fluid (CSF)-IRL concentrations after i.n. leptin administration were compared after intraperitoneal (i.p.) administration. The influence of 0.1 or 0.5% lysophosphatidylcholine (LPC) as an optimizer of leptin absorption was examined. The anorexic effects of i.n. leptin were compared with i.p. leptin in ad libitum fed rats. RESULTS: The i.n. leptin increased CSF-IRL concentrations, although serum IRL concentrations of rats administered leptin i.n. were lower than those administered i.p. The addition of 0.1 and 0.5% LPC dose-dependently increased serum IRL concentrations, but did not modify CSF-IRL concentrations in i.n. leptin-treated rats. The i.n. leptin inhibited dark-time food consumption at 0-1 h and 3-6 h in ad libitum fed rats. In contrast, i.p. leptin reduced food consumption only for an hour. Phosphorylated signal transducer and activator of transcription (STAT) 3 immunoreactive cells increased in the arcuate nucleus (ARC) of the hypothalamus at 3 h only following i.n. leptin. CONCLUSION: The present study demonstrated that i.n. leptin caused longer inhibition of appetite and phosphorylation of STAT3 in ARC. It is concluded that the trans-nasal route may be useful for the selective access of leptin to the brain in obese people.

show abstract

“…But nasal mucosa irritancy and metered dose delivery are some of the challenges for formulation scientists and device manufacturers ( (A) In vitro nasal permeation studies: Various approaches used to determine the drug diffusion through nasal mucosa from the formulation. The two important methodologies to study the diffusion profile of the drug are discussed here,  In vitro diffusion studies 16,17 : The nasal diffusion cell is fabricated in glass. The waterjacketed recipient chamber has total capacity of 60 ml and a flanged top of about 3mm; the lid has 3 opening, each for sampling, thermometer, and a donor tube chamber.…”

Section: Nasal Powdermentioning

confidence: 99%

Untitled

2011

IJPSR

View full text Add to dashboard Cite

The convenience of administration and improved patient compliance are important in the design of nasal drug delivery system which remains the preferred route of drug delivery in spite of various disadvantages. Therapy through intranasal administration has been an accepted form of treatment in the Ayurvedic system of Indian Medicine. Advances in biotechnology have made available a large number of protein and peptide drug for the treatment of a variety of diseases. These drugs are unsuitable for oral administration because they are significantly degraded in the gastrointestinal tract or considerably metabolized by first pass effect in the liver. Even the parenteral route is inconvenient for long term therapy. Of many alternate routes tried, intranasal drug delivery is found much promising for administration of these drugs. In this article, an overview on the design and development of intranasal drug delivery system is presented. Advantages of NDDS are Drug degradation that is observed in the gastrointestinal tract is absent, hepatic first pass metabolism is absent, Rapid drug absorption and quick onset of action can be achieved, bioavailability of larger drug molecules can be improved by means of absorption enhancer or other approach, the nasal bioavailability for smaller drug molecules is good, Drugs that are orally not absorbed can be delivered to the systemic circulation by nasal drug delivery, Studies so far carried out indicate that the nasal route is an alternate to parenteral route, especially, for protein and peptide drugs, convenient for the patients, especially for those on long term therapy, when compared with parenteral medication, Large nasal mucosal surface area for dose absorption, rapid drug absorption via highly-vascularized mucosa, ease of administration, non-invasive, lower dose/reduced side effects.

show abstract

Optimization of systemic nasal drug delivery with pharmaceutical excipients

Cited by 83 publications

References 99 publications

Considerations for the Development of Nasal Dosage Forms

Considerations for the Development of Nasal Dosage Forms

Inhibition of appetite by nasal leptin administration in rats

Untitled

Contact Info

Product

Resources

About