Objectives: The objective of present study was to develop chitosan-based sustained release nicorandil microspheres to reduce the dosing frequency. Materials and Methods : The nicorandil-loaded chitosan microspheres were formulated by emulsion crosslinking method. A 3 ² factorial design was employed to study the influence of drug: Polymer ratio and volume of glutaraldehyde (GA) on percentage entrapment efficiency, particle size, and % drug release at 8 h. Results: The entrapment efficiency was found to be 41.67 ± 1.43-77.33 ± 1.97% and particle size range 65.67 ± 2.08-146.67 ± 2.18 μm. The batch CH5 showed 79.11 ± 2.23 and 96.21 ± 2.41% drug release at 8 and 12 h, respectively. Conclusions: Drug: Polymer ratio and volume of GA had significant effect on % entrapment efficiency, particle size, and % drug release. From the scanning electron microscopy (SEM) study observed that microspheres were spherical and fairly smooth surface. Fickian diffusion was the mode of drug release from nicorandil-loaded chitosan microspheres formulations.

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It seems to be a necessary need to develop an effective drug carrier system for targeted delivery of pharmaceuticals. Bacterial ghosts are emerging drug delivery platform that are capable of delivery of proteins, antigens, nucleic acids, and pharmaceuticals. Bacterial ghosts are generally produced by lysis of gram-negative bacteria. Pharmaceutically, these ghosts could be utilized to deliver proteins peptides, vaccines, drugs effectively. However, this technology is at initial stage and systematic studies are required to implement such system over humans.

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Aim: The preparation of novel PEGylated PAMAM (poly-amidoamine) dendrimers for delivery of anti-HIV drug Efavirenz is reported. Method and Materials: About 5.0 G PAMAM dendrimers are prepared by ethylene diamine core via Michael addition by divergent method. PEGylation is done by polyethylene glycol 600 using epichlorhydrin as linker. PEGylated 5.0 G PAMAM dendrimers loaded with Efavirenz (EFV) are evaluated for FTIR, DSC, SEM, drug release, and stability studies. Results and Conclusion: From the results it is proved that this method is less time consuming, inexpensive, and reproducible. Drug-release studies indicate, PEGylated 5.0 G PAMAM-EFV dendrimers have shown prolonged drug-release property.

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Aim: Zolmitriptan is a 5-HT receptor agonist (1B/1D). It is used in the acute treatment of migraine having low bioavailability about 40% orally due to hepatic first pass metabolism. The purpose of the present research was to formulate fast acting sublingual tablets of zolmitriptan. Materials and Methods: Sublingual tablets were prepared using ispaghula husk powder, gellan gum, sodium alginate as super disintegrating polymers and citric acid, tartaric acid and camphor as permeation enhancers by direct compressible technique and evaluated for weight variation, thickness, friability, content uniformity, hardness, disintegration time, wetting time, in-vitro drug release, in-vitro and ex-vivo permeation study. Stability study of optimized formulation was performed as per ICH (International Conference on Harmonisation) guideline. Results: The in-vitro disintegration time of the optimized formulation (D5) was 9 ± 2 s and all formulations showed 100% of dissolution within 6 ± 2 min. Formulation containing 4% of gellan gum (D5) showed highest disintegration and 2% of citric acid formulation (P3) showed highest permeation 88% within 30 min and ex-vivo permeation was 52% within 30 min. Optimized formulation was stable for 1 month during stability study as per ICH guideline. Conclusion: The sublingual tablet formulation gives better results using natural super disintegrant for fast onset of action.

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Objective: The objective of the present work was to formulate and to characterize a floating drug delivery system for clopidogrel bisulphate to improve bioavailability and to minimize the side effects of the drug such as gastric bleeding and drug resistance development. Materials and Methods: Clopidogrel floating tablets were prepared by direct compression technique by the use of three polymers xanthan gum, hydroxypropyl methylcellulose (HPMC) K15M and HPMC K4M in different concentrations (20%, 25% and 30% w/w). Sodium bicarbonate (15% w/w) and microcrystalline cellulose (30% w/w) were used as gas generating agent and diluent respectively. Studies were carried out on floating behavior and influence of type of polymer on drug release rate. All the formulations were subjected to various quality control and in-vitro dissolution studies in 0.1 N hydrochloric acid (1.2 pH) and corresponding dissolution data were fitted to popular release kinetic equations in order to evaluate release mechanisms and kinetics. Results and Discussion: All the clopidogrel floating formulations followed first order kinetics, Higuchi drug release kinetics with diffusion as the dominant mechanism of drug release. As per Korsmeyer-Peppas equation, the release exponent "n" ranged 0.452-0.654 indicating that drug release from all the formulations was by non-Fickian diffusion mechanism. The drug release rate of clopidogrel was found to be affected by the type and concentration of the polymer used in the formulation (P < 0.05). As the concentration of the polymer was increased, the drug release was found to be retarded. Conclusion: Based on the results, clopidogrel floating tablets prepared by employing xanthan gum at concentration 25% w/w (formulation F2) was the best formulation with desired in-vitro floating time and drug dissolution.

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Introduction: The polyelectrolyte Complexes (PECs) are based on ionic cross-linking. They have been employed to prepare a sustained release matrix tablets. These systems are based upon the fact that their structure can entrap the drug within them. Isosorbide Mononitrate (ISMN) is an anti-anginal organic nitrate vasodilator used in the treatment of various cardiovascular disorders and prophylaxis of angina Pectoris, which is poorly absorbed from the upper GIT, hence CR formulation is desirable. Materials and Methods: Chitosan (CH)/Sodium alginate (SA), Guar gum (GG), and Xanthan gum (XG) were used as PECs, and were prepared using different proportions i.e., in 1:1 and 1:2 ratio. The optimum ratio of CH: SA, CH: GG and CH: XG was in the ratio was 1:2; these are formed due to electrostatic interaction between oppositely charged poly ions. These normally employ a hydrophilic matrix system. Matrix tablet of ISMN was formulated by using PECs as matrix forming agent by wet granulation technique. Results: The tablets were evaluated for hardness, wt variation, drug content, and in-vitro dissolution studies and found to be within limits. Release kinetics data indicated that ISMN released from the PECs-based matrix tablets of CH-SA, CH-GG and CH-XG CP in 1:1 and 1:2 ratio, followed Fickian and non-Fickian diffusion mechanism respectively. Thus, the drug release rate was extended for over a period of more than 12 h stability studies. There is no significant difference in the mean % drug released from formulation CH-X ₂ after storing for 3 months at 40°C/75% RH. The FT-IR spectra revealed that there was no interaction between polymers and drug, Statistical analysis showed a significant differences (P < 0.05) for the amount of ISMN released from the formulations (MXG) and formulations (CH-X ₂ ). Conclusion : Formulation CH-XG ₂ (1:2) showed better sustained release of highly water-soluble ISMN with the desired release rate. Thus, the formulated PECs-based matrix tablets seems to be a potential candidate for sustained drug delivery of highly soluble drug ISMN in the symptomatic therapy of angina pectoris.

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Aim: The aim of the present work was to explore the development of a dual-controlled release periodontal system of a potent broad spectrum first-generation fluoroquinolone, ciprofloxacin, and the anti-inflammatory enzyme serratiopeptidase (STP). Materials and Methods: Based on 3 ² full factorial design, thermoreversible periodontal sols capable of controlled dual delivery of ciprofloxacin hydrochloride and STP were designed using pluronic F127 and carbopol 934P as thermosensitive gelling polymers. Sol gel transition characteristics, %cumulative drug release at 48 ^th h and exvivo mucoadhesive strength were designated as dependent responses. The sols were mucoadhesive, syringeable, and inverted into gels at simulated periodontal cavity temperature. Results: F9 with optimal drug release was identified as the best formulation. Extra design check point generated using Design Expert software 8.02 (Stat-Ease, USA) validated the experimental design. Textural analysis revealed that the developed sols were syringeable and spreadable enough for periodontal treatment so it can be expected that hardness and compressibility of sols would pose no problem during clinical application. The in vitro release behavior exhibited controlled release of both cipro HCl and STP (>90% release). Conclusion: A dual-controlled release thermoreversible periodontal sol of ciproflaxin and STP was successfully developed. Incorporation of STP as anti-inflammatory agent has the potential of developing a therapeutically efficacious system of cipro HCl for treatment of periodontal inflammatory anaerobic infections.

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