Investigation of Absorption Routes of Meloxicam and Its Salt Form from Intranasal Delivery Systems.

نویسندگان

  • Csilla Bartos
  • Rita Ambrus
  • Anita Kovács
  • Róbert Gáspár
  • Anita Sztojkov-Ivanov
  • Árpád Márki
  • Tamás Janáky
  • Ferenc Tömösi
  • Gábor Kecskeméti
  • Piroska Szabó-Révész
چکیده

The aim of this article was to study the trans-epithelial absorption to reach the blood and to target the brain by axonal transport using nasal formulations with nanonized meloxicam (nano MEL spray) and its salt form known as meloxicam potassium monohydrate (MELP spray). The physicochemical properties and the mucoadhesivity of nasal formulations were controlled. In vitro and in vivo studies were carried out. These forms were first investigated in "nose-to-brain" relation. It was found that the in vitro study and in vivo study did not show any significant correlation. In vitro experiments demonstrated faster dissolution rate and higher diffusion of MELP from the spray compared with the nano MEL spray. The administration of the nano MEL spray resulted in faster absorption and constant plasma concentration of the drug after five minutes of administration as compared to MELP. The axonal transport of the drug was justified. MEL appeared in the brain tissues after the first five minutes of administration in the case of both spray forms, but its amount was too small in comparison with the total plasma concentration. The application of the nano MEL spray resulted in the same AUC in the brain as the intravenous injection. The "nose-to-blood" results predicted the nasal applicability of MEL and MELP in pain management. The "nose-to-brain" pathway requires further study.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Meloxicam transdermal delivery: effect of eutectic point on the rate and extent of skin permeation

Objective(s):Drug delivery through the skin can transfer therapeutic levels of drugs for pharmacological effects. Analgesics such as NSAIDs have gastrointestinal side effects and topical dosage forms of these drugs are mainly preferred, especially for local pains. Meloxicam is one of NSAIDs with no topical form in the market. In this research, we attempted to quantify the skin permeation of a m...

متن کامل

A Review of Vesicular and Polymeric Nano-systems in Olanzapine Drug Delivery

 Olanzapine (2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno [2, 3-b][1, 5]benzodiazepine) is an antipsychotic drug with poor water-solubility that has a suitable affinity to some receptors. This benzodiazepine derivative is a new (atypical) antipsychotic drug and has a wide range of efficacy, especially in treatment of patients with negative psychiatric symptoms of schizophrenia. Olanzapine is ...

متن کامل

Transdermal Delivery of Desmopressin Acetate from Water-in- Oil Nano/submicron Emulsion Systems

Desmopressin acetate is a potent synthetic peptide hormone. A more acceptable route of Desmopressin acetate is a potent synthetic peptide hormone. That is administered via parenteral, intranasal, and oral routes. A more acceptable route of administration with potentially good bioavailability could be offered by transdermal delivery. The present work reports on the development of water-in-oil (w...

متن کامل

Bioavailability and pharmacokinetics of lorazepam after intranasal, intravenous, and intramuscular administration.

The purpose of this study was to evaluate the pharmacokinetic profile of intranasal lorazepam in comparison to currently established administration routes. Eleven healthy volunteers completed this randomized crossover study. On three occasions, each separated by a 1-week washout, subjects received a 2 mg dose of lorazepam via the intranasal, intravenous, or intramuscular route. Blood samples we...

متن کامل

Gamma scintigraphy in the evaluation of drug delivery systems [Persian]

Gamma-scintigraphy is applied extensively in the development and evaluation of pharmaceutical delivery systems, particularly for monitoring formulations in the gastrointestinal and respiratory tracts. The radiolabelling is generally achieved by the incorporation of an appropriate radionuclide such as technetium-99m or indium-111 into the formulation or by addition of a non-radioactive iso...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • Molecules

دوره 23 4  شماره 

صفحات  -

تاریخ انتشار 2018