Ebastine (EBS) is a second-generation non-sedating antihistamine used for the prevention and treatment of allergic rhinitis and chronic idiopathic urticaria. It is BCS class II drug exhibiting low aqueous solubility and poor oral bioavailability. The present work was aimed at enhancing the dissolution rate of EBS by formulating it in the form of a liquisolid (LS) system using Tween 20 (non-volatile solvent), Avicel PH 102 (carrier material) and Aerosil 200 (coating material). Various batches of LS powder system were formulated by adopting a mathematical model for calculating required quantities of excipients. The absence of interaction between drug and excipients was checked by Fourier transform IR spectroscopy and differential scanning calorimetry studies. Formulated EBS tablets were evaluated for post compression parameters. X-ray powder diffraction studies and scanning electron microscopy showed the loss of EBS crystallinity in LS formulations. Formulation F9 was considered as optimum, showing a higher drug release of up to 99.06% in comparison to marketed tablet formulations. Stability of the optimized formulation was confirmed by results of the accelerated aging study. Thus, it is concluded that LS formulation is a favorable method of EBS solubility enhancement.

The aim of the present research work was to formulate and characterize gastroretentive mucoadhesive tablets of lacidipine (LCDP) intended for the treatment of gastroparesis. Polymers such as sodium alginate, HPMC K4M, carbopol 974P, and chitosan were utilized in LCDP formulation to ensure gastric retention up to 8 h. Direct compression method was adopted in preparation of mucoadhesive tablets. Prior to compression, powder blends were evaluated in order to check their flow and compression properties. Fourier transform infrared spectroscopy and differential scanning calorimetry measurements were performed to assess the compatibility of LCDP with polymers. Tablets were characterized with respect to the uniformity of weight, hardness, friability, drug content, swelling index, surface pH and in-vitro drug release. All formulations exhibited acceptable physicochemical properties. Formulation F4 exhibiting in-vitro drug release of 95.510% was selected as the optimized formulation and was further characterized by scanning electron microscopy. In vitro dissolution data was fitted to various kinetic models, and formulation F4 was found to display non-Fickian mechanism of drug release. No major change was observed in drug release and drug content upon storage of optimized formulation under accelerated aging conditions. The obtained results revealed that carbopol 974P and chitosan can be used in combination to formulate gastroretentive mucoadhesive LCDP tablets.

The aim of the current study was to formulate and characterise thermoreversible in situ nasal gels of flunarizine dihydrochloride (FDCL) for prophylaxis of migraine. FDCL was complexed with beta-cyclodextrin (1:1 ratio) to enhance its solubility. A mucoadhesive polymer, chitosan was used to increase nasal residence time of the drug. Gels were formulated by cold technique using poloxamer 188 and poloxamer 407. Drug content was determined before and after gelation. Optimised formulation exhibited 89.41% of in vitro drug release at the end of 6 h. In vitro release kinetics results demonstrated that all the prepared formulations released the drug by following first-order kinetics. Short term stability study revealed 5 +/- 3 degrees C as the appropriate storage condition for the formulations. Thus, the study proved that thermoreversible in situ nasal gel of FDCL with mucoadhesive agent could be a promising initiative for the treatment of migraine.

Lacidipine (LCDP), a BCS class II drug is used in the treatment of hypertension. Upon oral administration, LCDP shows poor absorption from gastrointestinal tract and undergoes extensive first pass hepatic metabolism. The oral bioavailability of LCDP is 10%. The present study involved the development and characterization of LCDP porous tablets to enhance its solubility and dissolution rate. Tablets were formulated by direct compression method followed by vacuum drying at 40 degrees C for 6 h. Optimized formulation contained croscarmellose sodium as superdisintegrants and camphor as sublimating agent. Tablets were characterized for post compression parameters. Dissolution was carried out in phosphate buffer pH 6.8 and in pH 1.2 buffer with 0.2% Tween 20. Scanning electron microscopy image revealed the presence of highly porous surface texture. Thus, collectively it can be concluded that porous tablets of LCDP can serve as an alternative for enhancement of drug solubility and release thereby enhancing its bioavailability.

Lacidipine (LCDP), a BCS class II calcium channel blocker, is used as antihypertensive agent. LCDP possesses low aqueous solubility and also undergoes extensive first pass metabolism resulting in oral bioavailability of 10%. The present study was aimed to enhance the solubility and hence dissolution rate of LCDP by formulating into liquisolid compacts. LCDP liquisolid compacts were formulated using avicel PH 102, tween 80, aerosil 200 and sodium starch glycolate. A mathematical model was adopted to determine the suitable quantity of carrier and coating materials. The formulated tablets were evaluated for post compression parameters. Liquisolid tablets showed high drug release as compared to the pure drug. The optimized formulation exhibited 99.89 +/- 0.162% of drug release within 45 min. Stability studies confirmed the stability of optimized formulation. Present study thus concluded that the liquisolid is a favourable technique to improve the solubility and drug release of LCDP.