Table 4.
Comments on advantages and limitations of cinnarizine delivery systems as included in the text.
| Delivery system | Advantages | Limitations |
|---|---|---|
| Fast dissolving tablets | Rapid absorption and quick onset of action. | Have insufficient mechanical strength. |
| Rapid drug therapy intervention. | Require handling precautions. | |
| Ease of administration especially to pediatric and geriatric population. | Generally hygroscopic in nature, so require specialized product packaging. | |
| Disintegrate within seconds without the need of water. | May lead to unpleasant gritty mouth feeling. | |
| Improve dissolution of poorly soluble drug. | ||
| Allow high drug loading. | ||
| Pregastric absorption avoids hepatic metabolism and reduce side effects. | ||
|
| ||
| Lipid based systems | Enhance solubilization of poorly soluble drugs. | Lack of sound in vitro predictive models. |
| Overcome dissolution step. | Chemical instability of drugs. | |
| Submicron droplets size increases surface area for absorption resulted in increased rate and extent of absorption. | Need high surfactant concentration (30–60%). | |
| Selectively target to specific site in GIT. | May permit less drug loading. | |
| More consistent drug absorption. | Lack of appropriate in vitro-in vivo correlation. | |
| Resist precipitation of drug in upper part of GIT and on shifting the pH, compatible for cinnarizine. | May exhibit limited lymphatic uptake from emulsion based systems. | |
| Unsaturated fatty acids (an essential excipient) enhance solubility. | Oxidation of unsaturated fatty acids in the formulation. | |
| Prevent drug degradation in GIT. | ||
| Diminishes fasted and fed state variation in absorption and also food effect. | ||
| Liquid crystalline nanostructured particles provided better scope for sustained delivery. | ||
| Cubosomes improvise stability, bioadhesivity and biocompatibility. | ||
| Hexasomes accentuate stability of encapsulated drug | ||
|
| ||
| Gastroretentive systems | Residence in stomach for longer duration provides sustained effect. | Floating tablets and films undergo all or none effects. |
| Suitable system for drugs that have absorption window in upper GIT. | May be swept away due to Migrating Myoelectric Complex motility pattern | |
| Diminishes precipitation of basic drug at alkaline pH. | May cause gastric irritation. | |
| Appreciable therapeutic activity. | Bioadhesive systems have high turnover rate of mucus. | |
| Account for once a day therapy. | Require presence of food to delay gastric emptying. | |
| Advantageous for drugs with narrow therapeutic index. | Microspheres, microballoons have low drug loading capacity. | |
| Lesser risk of dose dumping for multiparticulate systems. | ||
| Less inter and intra subject variability. | ||
| Microspheres, microballoons provide high degree of dispersion in digestive tract. | ||
References to the above mentioned points are cited in the text.