Rheological, adhesive and release characterisation of semisolid Carbopol/tetraglycol systems.
Gels dosage forms are successfully used as drug delivery systems considering their ability to control drug release and to protect medicaments from an hostile environment. This study deals with the gelation properties of Carbopol 971 e 974 polymeric systems in tetraglycol, a water-miscible cosolvent. In this paper, the attention was noted of the thickening properties of the different Carbopol in tetraglycol solvent at increasing temperatures, in order to obtain gels avoiding neutralisation and, at the same time, to make possible the dissolution in these gels of insoluble or poorly soluble water drugs. Samples were prepared by simply dispersing different Carbopols amount (0.5-4%) were added to tetraglycol and different systems were prepared at room temperature and by heating at 70 degrees C. All these systems were then characterised rheologically. Frequency sweep, creep-recovery, temperature sweep and time sweep analyses outlined that Carbopol 971 and 974 in tetraglycol gave rise after heating to gels with satisfactory rheological behaviour: the elastic modulus was greater than the viscous one and a remarkable elastic character was found to be present. Systems obtained by heating procedure were examined also from a mechanical point of view using a texture profile analysis. Besides, being Carbopols well known mucoadhesive polymers, gels adhesive properties were also studied using the ex vivo method. Texture and adhesion characterisation confirmed rheological results pointing out a certain greater elasticity and adhesiveness of Carbopol 974 systems. Then, the possible cutaneous irritation was also tested using the in vivo method (Draize test). No signs of cutaneous irritation were obtained for all the samples that were analysed. After rheological and mucoadhesive properties were set, paracetamol as a model drug was inserted in the composition of the gels and the release characteristics were defined. Dissolution tests pointed out the greater release control properties of tetraglycol/Carbopol 971 samples. These studies showed tetraglycol/Carbopol systems as a first-rate alternative to traditional water gels when low water-soluble drugs have to be added.
Bonacucina
Giulia
G
University of Camerino, Department of Chemical Sciences, via S. Agostino 1, 62032 Camerino, Italy.
Cespi
Marco
M
Misici-Falzi
Monica
M
Palmieri
Giovanni F
GF
D000082:Acetaminophen / Q000737:chemistry; D000179:Acrylates / Q000737:chemistry / Q000378:metabolism; D000180:Acrylic Resins; D000268:Adhesiveness; D000818:Animals; D002417:Cattle; D004337:Drug Carriers; D004548:Elasticity; D004947:Esophagus; D005782:Gels; D006168:Guinea Pigs; D066298:In Vitro Techniques; D009092:Mucous Membrane / Q000737:chemistry / Q000378:metabolism; D011092:Polyethylene Glycols / Q000737:chemistry* / Q000378:metabolism; D011145:Polyvinyls / Q000737:chemistry* / Q000378:metabolism; D012212:Rheology; D023422:Skin Irritancy Tests; D012995:Solubility; D012997:Solvents; D013696:Temperature; D013997:Time Factors
D000179:Acrylates; D000180:Acrylic Resins; D004337:Drug Carriers; D005782:Gels; D011145:Polyvinyls; D012997:Solvents; C492577:carbopol 971P; C117167:carbopol 974P NF; C006912:carboxypolymethylene; D000082:Acetaminophen; D011092:Polyethylene Glycols