Proniosomal Oral Tablets for Controlled Delivery and Enhanced Pharmacokinetic Properties of Acemetacin
Journal Title: AAPS PharmSciTech - Year 2015, Vol 16, Issue 2
Abstract
Free-flowing proniosomal powders of acemetacin (AC) were prepared using the slurry method and maltodextrin as carrier. Positively charged proniosomes composed of 70:20:10 of Span 60/cholesterol (Chol)/stearylamine (SA), respectively, were successively compressed into tablets using direct compression method. The tablets were characterized for weight variability, friability, hardness, drug content uniformity, and dissolution properties. The in vivo evaluation of the prepared proniosomes (powder or tablet forms) after oral administration was investigated by the determination of AC and its active metabolite indomethacin (IND) in the blood of albino rabbits. Results indicated that the increase of Chol from 10% to 20% markedly reduced the efflux of the drug. Further Chol addition from 30% to 50% led to increased AC release rates. The proniosome tablets of AC showed greater hardness and disintegration time and less friability than AC plain tablets. The dissolution of proniosomal tablets indicated a lower drug release percentage compared to powdered proniosomes and AC plain tablets. The mean pharmacokinetic parameters of AC and IND from different formulations indicated increased t1/2 and area under the curve (AUC) of both AC and IND for proniosomal tablets compared with both proniosomal powders and AC plain tablets. This study suggested the formulation of AC proniosomal powder into tablets to control and extend its pharmacologic effects.
Authors and Affiliations
Tamer M. Shehata, Marwa H. Abdallah, Mahmoud Mokhtar Ibrahim
Keywords
Related Articles
- EP ID EP682210
- DOI 10.1208/s12249-014-0233-5
- Views 82
- Downloads 0
A New Extrudable Form of Hypromellose: AFFINISOL™ HPMC HME
The online version of this article (doi:10.1208/s12249-015-0395-9) contains supplementary material, which is available to authorized users.
Preparation of Polyamide Nanocapsules of Aloe vera L. Delivery with In Vivo Studies
Aloe vera is the oldest medicinal plant ever known and the most applied medicinal plant worldwide. The purpose of this study was to prepare polyamide nanocapsules containing A. vera L. by an emulsion diffusion technique...
Model Drug as Pore Former for Controlled Release of Water-Soluble Metoprolol Succinate from Ethylcellulose-Coated Pellets Without Lag Phase: Opportunities and Challenges
The objective of the present study was to evaluate the feasibility of using model drug metoprolol succinate (MS) as a pore former to modify the initial lag phase (i.e., a slow or non-release phase in the first 1–...
Topical Lyogel Containing Corticosteroid Decreases IgE Expression and Enhances the Therapeutic Efficacy Against Atopic Eczema
Hydrocortisone cream intended for atopic eczema often produces unwanted side effects after long-term use. These side effects are essentially due to repeated percutaneous administration of the medication for skin dermatit...
Use of Polyvinyl Alcohol as a Solubility Enhancing Polymer for Poorly Water-Soluble Drug Delivery (Part 2)
The KinetiSol® Dispersing (KSD) technology has enabled the investigation into the use of polyvinyl alcohol (PVAL) as a concentration enhancing polymer for amorphous solid dispersions. Our previous study revealed...