Influence of heat treatment on spray-dried mixtures of Amioca starch and Carbopol 974P used as carriers for nasal drug delivery (original) (raw)

Effect on the nasal bioavailability of co-processing drug and bioadhesive carrier via spray-drying

International journal of pharmaceutics, 2009

A mucoadhesive combination of a maize starch (Amioca, mainly consisting of amylopectine) and a cross-linked acrylic acid-based polymer (Carbopol 974P) was spray-dried with metoprolol tartrate (used as model molecule) in order to develop a powder suitable for nasal drug delivery via a one-step manufacturing process. The bioavailability of metoprolol tartrate after nasal administration of this powder to rabbits was compared with powders manufactured via other procedures: (a) freeze-drying of a dispersion prepared using the co-spray-dried powder, (b) freeze-drying of a dispersion prepared using a physical mixture of drug and mucoadhesive polymers. After co-processing via spray-drying a low bioavailability (BA 10.8+/-2.3%) was obtained, whereas manufacturing procedures based on freeze-drying yielded a higher BA: 37.9+/-12.8% using the co-processed powder and 73.6+/-24.9% using the physical mixture. The higher bioavailability was due to the deprotonation of poly(acrylic acid) during neut...

Spray-dried mucoadhesive microspheres: preparation and transport through nasal cell monolayer

AAPS PharmSciTech, 2006

The purpose of this research was to prepare spray-dried mucoadhesive microspheres for nasal delivery. Microspheres composed of hydroxypropyl methylcellulose (H), chitosan (CS), carbopol 934P (CP) and various combinations of these mucoadhesive polymers, and maltodextrin (M), colloidal silicon dioxide (A), and propylene glycol (P) as filler and shaper, were prepared by spray-drying technique. Using propranolol HCl as a model drug, microspheres were prepared at loadings exceeding 80% and yields between 24% and 74%. Bulky, free flowing microspheres that had median particle size between 15 and 23 mum were obtained. Their zeta potential was according to the charge of polymer. Adhesion time of mucoadhesive microspheres on isolated pig intestine was ranked, CS > CP:H > CP > H, while the rank order of swelling was CP > CS > H. Increasing the amount of CP in CP:H formulations increased the percentage of swelling. Infrared (IR) spectra showed no interaction between excipients us...

Feasibility Investigation of Cellulose Polymers for Mucoadhesive Nasal Drug Delivery Applications

Molecular pharmaceutics, 2015

The feasibility of various cellulose polymer derivatives, including methylcellulose (MC), hydroxypropyl methylcellulose (HPMC), sodium-carboxymethylcellulose (sodium-CMC), and cationic hydroxyethylcellulose (cationic HEC), for use as an excipient to enhance drug delivery in nasal spray formulations was investigated. Three main parameters for evaluating the polymers in nasal drug delivery applications include rheology, ciliary beat frequency (CBF), and permeation across nasal tissue. Reversible thermally induced viscosity enhancement was observed at near nasal physiological temperature when cellulose derivatives were combined with an additional excipient, polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PVCL-PVA-PEG). Cationic-HEC was shown to enhance acyclovir permeation across the nasal mucosa. All tested cellulosic polymers did not cause any adverse effects on porcine nasal tissues and cells, as assessed by alterations in CBF. Upon an increase in polyme...

Formulation and Evaluation of Thermosensitive Intranasal in situ Gel of Sumatriptan Succinate by using A Blend of Polymers

Journal of Pharmacy and Chemistry, 2014

The prolonged residence of drug formulation in the nasal cavity is of utmost importance for intranasal drug delivery. To improve the nasal retention time of Sumatriptan Succinate, it has been formulated as in situ mucoadhesive gel by using blend of sodium CMC, Poloxamer 188 and carbopol 934P. The objective of this work was to improve the nasal bioavailability of antimigraine drug, Sumatriptan Succinate by increasing its nasal retention time as well as by means of nasal permeation. The in vitro tests performed for mucoadhesive strength and drug diffusion showed that nasal in situ gelling formulations prepared were having good mucoadhesive strength with nearly 100% drug diffusion. The formulations were evaluated for physiochemical parameter, gelation temperature, viscosity, gel strength, content uniformity, FTIR and DSC. So, this study points to the potential of mucoadhesive in situ nasal gel in terms of ease of administration, accuracy of dosing, prolonged nasal residence and improved nasal bioavailability.

Formulation and Evaluation of thermal Induced intranasal In- Situ Gel of Sumatriptan Succinate

IOSR Journal Of Pharmacy , 2020

Sumatriptan is having high first pass metabolism leading to low bioavailability (absolute Bioavailability 14% in humans).So there is a need to improve the nasal bioavailability by improving nasal penetration because of long duration of retention. The prolonged residence of drug formulation in the nasal cavity is of utmost importance for intranasal drug delivery.The objective of this work was to improve the nasal bioavailability of antimigraine drug, Sumatriptan Succinate by increasing its nasal retention time as well as by means of nasal permeation.To improve the nasal retention time of Sumatriptan Succinate, it has been formulated as In-situ mucoadhesive gel by using blend of Poloxamer 407 and HPMC K4 M. The In-vitro tests performed for mucoadhesive strength and drug diffusion showed that nasal In-situ gelling formulations prepared were having good mucoadhesive strength with very good drug diffusion. The drug release mechanism gel matrices was found to be anomalous and following the Higuchi equation and the diffusion follows Fickian diffusion mechanism. The formulations were evaluated for physiochemical parameter like gelation temperature,viscosity, gel strength, drug content , FTIR and DSC. FTIR and DSC studies were carried out on pure drug as well as for all excipients used in the final formulation and exhibited no interaction.So, this study points to the potential of mucoadhesive In-situ nasal gel of Sumatriptan Succinate in terms of ease of administration, accuracy of dosing, prolonged nasal residence and improved nasal bioavailability.