Review Article

Recent Advances in Delivery Systems and Therapeutics of Cinnarizine: A Poorly Water Soluble Drug with Absorption Window in Stomach

Table 4

Comments on advantages and limitations of cinnarizine delivery systems as included in the text.

Delivery systemAdvantagesLimitations

Fast dissolving tabletsRapid 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 systemsEnhance 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 systemsResidence 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.