Development and Preclinical Testing of Nasal Aerosol for the Delivery of Novel Spray Dried Polyherbal Formulation to Treat Alzheimer’s Disease

Alzheimer’s disease (AD) is an irreversible, progressive brain disorder that slowly destroys memory and thinking skills and eventually the ability to carry out the simplest tasks. The present investigation was undertaken to evaluate anti-alzheimer’s activity of novel herbal aerosol spray formulation containing pure extracts of Curcuma longa, Commiphora wightii and Withania somnifera.Pressurized aerosol packs containing polyherbal spray dried dispersions in the concentration range of 0.5, 1 and 2% w/v dispersed in 10/90, 20/80, 30/70/ 40/60, 50/50) propellant blends of HFA-134a were developed in 3 in 1 aerosol filling machine and evaluated. Behavioural studies were performed in male wistar rats and histopathological studies were performed. The preparations were also assessed for AChE inhibitory activity. Results with P values < 0.05 were considered statistically significant. Chitosan exhibited compatibility with the polyherbal extracts in FT-IR studies. DSC thermogram revealed an endothermic peak of 65ᵒC with chitosan. Spray dried poly herbal extracts exhibited a spherical morphology particle size distribution of 5-50µm with a practical yield of 20-30%. Aerosol formulations exhibited a particle size range below 10µm. average weight per actuation of canister was 7-8mg with a total 210 deliveries per pack. Zeta potential of the formulations was ±0.997. HPTLC fingerprinting showed band ranges at 256 and 366nm. The optimized aerosol spray in behavioral tests exhibited 10mg/kg and 20mg/kg intranasally reversed the scopolamine induced amnesia. Histopathological findings showed decreased Ach activity in male albino wistar rats. Percentage inhibition of formulation and standaed on AChE activity shoed an IC50 of 62% for 10mg/kg aerosol spray and 72% with 20mg/kg aerosol spray dosing. Keywords: alzhiemer’s disease; herbal; spray dried chitosan; aerosol; nasal spray

Formulation, Characterization and Antihelminthic Activity Testing of Nitazoxanide Superporous Hydrogel Tablets

In the pharmaceutical field controlled release products have the ability to maintain desired medicament concentration or a longer period of time. Certain drugs are relatively insoluble in water and have high dose requirements that render unsuitable formulation difficulties in sustained release formulations. Nitazoxanide which is a high dose water insoluble antiprotozoal drug was formulated with the aim. To modulate gastro-retentive dosage form based on the superporous hydrogel composites. Foaming technique was used in the preparation of SPH composites. The superporous hydrogels were extremely sensitive to pH of swelling media and good porosity. Superporous hydrogels tablets of nitazoxanide showed good pre-compressional and post-compressional properties. Formulation X is the best formulation containing chitosan, polyvinyl alcohol, formaldehyde, exhibited good swelling ratio. The compatibility studies were performed by Fourier Transform Infrared (FT-IR) Spectroscopic Studies, Differential Scanning Calorimetry Studies (DSC). All formulations were evaluated for stability, drug content, and kinetic drug release & in-vitro drug release profile. It was concluded that the proposed gastro-retention drug delivery provides a different supply of nitazoxanide directly to the stomach. Keywords: Nitazoxanide, Anti protozoal, foaming technique, Chitosa

FORMULATION AND EVALUATION OF EXTENDED RELEASE PELLETS OF PIOGLITAZONE HYDROCHLORIDE USING NATURAL AND SYNTHETIC POLYMERS BY FLUIDIZED BED COATING TECHNIQUE

Objective: The objective of the current work was to develop Pioglitazone hydrochloride (HCl) pellets coated with natural polymer extracted from peas gum and also to compare the drug release profile with coatings containing semi-synthetic and synthetic polymers. Methods: Fluidized bed coating technique was used to develop pellets. A 22 factorial design was employed to study the effect of independent variables (inlet air temperature and spray rate), on dependent variables (percentage entrapment efficiency, percentage friability, and average particle size). Optimization was done by fitting experimental data to the software program. Obtained pellets were subjected to different evaluation parameters which are critical in the development of the dosage form. An in vitro lag phase study was carried out for all batches in simulated gastric fluid (0.1N HCl) for 5 h and in vitro drug release study was carried out for optimized batch (E-2 and P-3) in simulated intestinal fluid (pH 7.4 phosphate buffer). Results: The optimized batches E-2 and P-3 showed satisfactory percentage entrapment efficiency of 92.66±1.52, percentage friability of 0.57±0.03, and average particle size of 1424±16 μm. All batches maintained lag phase for 5 h in 0.1N HCl. An optimized batch of two different sizes exhibited a burst release within 30 min in a simulated intestinal fluid with no significant difference in release rate constant (*p>0.05) and followed first-order kinetics. Conclusion: Thus, Pioglitazone HCl pulsatile pellets were successfully developed for treating diabetes mellitus by fluidized bed coating technique employing factorial design

DESIGN AND DEVELOPMENT OF NOVEL DRUG DELIVERY SYSTEM USING HERBAL MEDICINE TO TREAT ALZHEIMER’S DISEASE

Objective: The present study was focused to design an herbal formulation for the treatment of Alzheimer’s disease (AD) to develop the formulation using various techniques such as spray drying, centrifugation, and lyophilization and to conduct behavioral studies to evaluate the activity of the herbal formulation. Methods: Formulation contains herbal extracts such as curcumin, guggul, and ashwagandha. To develop this formulation, various techniques such as spray drying, centrifugation, and lyophilization were employed along with a natural polymer chitosan in various combinations of excipient. Preformulation studies such as solubility of herbal extracts and Fourier transmission infrared spectroscopy (FT-IR) studies for compatibility of the natural polymer with herbal extracts were studied. The formulation was characterized by tests such as particle size determination using optical microscopy, surface morphological evaluation using scanning electron microscopy (SEM), and behavioral testing by Morris water maze test using diazepam-induced amnesia method. Results: The particle size varied from 12.27 μ for normal chitosan to 3.59 μ for spray-dried chitosan. In the same way, the particle of normal formulation (12.9 μ) was about 4–5 times larger than that of spray-dried formulation (2.7 μ). The SEM images showed no proper morphology for chitosan, round surface with wrinkles for spray-dried chitosan, improper structures for normal formulation, and rounded smooth surface for spray-dried formulation. Significant p value was shown when the spray-dried test formulation was tested using diazepam-induced amnesia method. The transfer latency was noted on the 8th day and after 24 h of intraperitoneal administration of diazepam for the test group. Conclusion: In the present research study, an attempt was made to design and develop a novel drug delivery system using herbal medicine to treat AD. FT-IR compatibility study was carried out using the selected polymer and the herbal extracts using novel spray-drying techniques; behavioral studies were also done

FABRICATION AND CHARACTERIZATION OF FAST DISSOLVING FILMS OF ECLIPTA PROSTRATE LEAVES EXTRACT TO TREAT MOUTH ULCERS

Objective: This research focused on the design of fast dissolving herbal film of Eclipta Prostrate leaves extract for mouth ulcers. Methods: The extract of Eclipta Prostrata leaves was formulated as films by solvent casting method using various polymers viz., HPMC E5, HPMC E15, sodium alginate and PVA. The films were designed by using propylene glycol as a plasticizer, SSG as super disintegrate and honey as a sweetener. Furthermore, the films were evaluated for thickness, folding endurance, weight variation, % elongation, surface pH, % moisture uptake, % moisture loss, disintegration and in vitro drug release study. Results: The revealed that all the films were good in appearance and had a smooth texture. Out of all ten formulations, F3 and F5 disintegrated rapidly with a disintegration time of 27 and 32 seconds. The drug release studies revealed that all the formulations had a good release profile, but the F3 formulation showed rapid release i.e. 83.57% in 4 min. The stability studies revealed that the formulations F3 and F5 were found good with non-tackiness, easily separable and disintegrated at 29 and 33 sec respectively with no appearance and drug release. Conclusion: The research revealed that Eclipta prostrate leaves extract can be formulated into oral films for the treatment of mouth ulcers with improved bioavailability and expected patient compliance

A COMPREHENSIVE REVIEW ON HYDROGELS

Polymers play a vital role in pharmaceutical development. Efforts have been continuously made to search a polymer that act in a controlled& desired way. Hydrogel development has solved many such issues. Hydrogels are hydrophilic, three-dimensional networks. Which are able to imbibe large amounts of water or biological fluids & thus resembles to a large extent, a biological tissue. They are insoluble due to the presence of physical or chemical crosslinks such as entanglements& crystallites. These materials can be synthesized to respond to a number of physiological stimuli present in the body, such as PH, ionic strength, temperature. The main aim of this article is to give a concise review on introduction, preparation methods, types, & various applications of hydrogels in the pharmaceutical field