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Oral administration of drugs having low water solubility is hampered by various enzymatic barriers present in gastrointestinal (GI) tract. Lipid nanoparticles based on solid matrix have emerged as a potential drug delivery system to improve the absorption and bioavailability of several drugs, especially lipophilic compounds. Solid lipid nanoparticles (SLN) are reported as the most promising technology for oral administration and offered several advantages over conventional dosages formulations including, enhancement in solubility, stability, permeability, and bioavailability with minimal side effects. In this review, we have highlighted recent advances in the development of SLN for the oral, parenteral, rectal, and topical administration of various drugs. We have also summarized the applications of SLN in the treatment of various diseases like tuberculosis, cancer, diabetes, and several nervous system related disorders. sustained release, timed release, extended release, and targeted release of a drug. The predominance of nanoparticles over the other drug delivery systems enables them to use for drug targeting. Nanoparticles are 10-100nm in size in which drug is either dispersed or entrapped in a matrix, encapsulated as the solid solution or may be adsorbed on the surface 2 .The nanoparticles are designed to provide intimate contact with GI epithelium, prolong residence time and allow permeation across the cell membrane. A pre-systemic metabolism of a drug can be avoided by using nanoparticles 3 . Lipid nanoparticles are safe to use as they contain lipids, which are included in the category of generally recognized as safe (GRAS). Solid Lipid NanoparticlesSolid lipid nanoparticles are an advanced and rapidly budding field of nanotechnology with several applications in pharmaceutical science. SLN were developed first in 1991. These are the colloidal carriers possesses an average diameter of 10 to 1000nm. They composed of single lipid core matrix dispersed in an aqueous surfactant solution. The carriers like liposomes, polymeric micelles, and porous solids can also be used to enhance the aqueous solubility of a drug. But SLN not only helps to increase the solubility of a drug but also offers target release of drugs. SLN can be used as a carrier for lipophilic as well as hydrophilic drugs 4 . SLN provides stability to the solid lipid matrix and overcomes the disadvantages of liposomes, which includes stability problems 5 . Instead of polymeric nanoparticles, SLN are found to be more compatible with the biological system. Exclusive properties of SLN such as smaller size, larger surface area and interaction of phases at the interface make them valuable candidate 2 . The release of encapsulated compounds is controlled by solid lipid matrix, which also improves the stability of incorporated lipophilic ingredients. The type of lipids, surfactants and their concentration in the formulation of SLN adjust the particle size, drug loading, and release behavior of drugs 5 . The physicochemical characteristics of the solid lipid...

Background: Development of polymeric micelles for the management of allergic conjunctivitis to overcome the limitations of topical installation, such as poor patient compliance, poor stromal permeability, and significant adverse effects, increase precorneal residence time and efficacy, and also control the release of drug at the target site. Objective: The investigation was aimed at developing a polymeric micellar system of Azelastine HCl for Ocular Delivery. Methods: Drug loaded micelles of tri-block copolymers Pf 127 were prepared by Thin Film hydration method. The polymeric micelles formulations (F1 to F9) were assessed for entrapment efficiency, micelle size, in vitro permeation, ex vivo transcorneal permeation, in vivo Ocular Irritation, and Histology. Results: Optimized micelles formulation (F3), with the lowest micelle size of 92 nm, least polydispersity value of 0.135, highest entrapment efficiency of 95.30 ± 0.17%, and a cumulative drug permeation of 84.12 ± 1.26% in 8h, was selected to develop pH-sensitive micelles loaded carbopol in situ gel. The optimized in situ gel (G4) proved to be superior in its ex vivo transcorneal permeation when compared with Market Preparation and pure drug suspension, exhibiting 43.35 ± 1.48% Permeation with zero-order kinetics (r2 = 0.9944) across goat cornea. Transmission Electron microscopy revealed spherical polymeric micelles trapped in the gel matrix. A series of experiments showed hydration capability, non-irritancy, and histologically safe gel formulation that had appropriate handling characteristics. Conclusion: A controlled release pH-sensitive ocular formulation capable of carrying the drug to the anterior section of the eye via topical delivery was successfully developed for the treatment of allergic conjunctivitis.

Purpose: A comparative study was carried out between surface solid dispersion (SSD) and solid dispersion (SD) of meloxicam (MLX) to assess the solubility and dissolution enhancement approach and thereafter develop as patient friendly orodispersible tablet.Methods: Crospovidone (CPV), a hydrophilic carrier was selected for SSD preparation on the basis of 89% in- vitro MLX adsorption, 19% hydration capacity and high swelling index. SD on the other hand was made with PEG4000. Both were prepared by co-grinding and solvent evaporation method using drug: carrier ratios of 1:1, 1:4, and 1:8. Formulation SSDS3 (MLX: CPV in 1:8 ratio) made by solvent evaporation method showed t50% of 28 min and 80.9% DE50min which was higher in comparison to the corresponding solid dispersion, SDS3 (t50% of 35min and 76.4% DE50min). Both SSDS3 and SDS3 were developed as orodispersible tablets and evaluated.Results: Tablet formulation F3 made with SSD3 with a disintegration time of 11 secs, by wetting time= 6 sec, high water absorption of 78%by wt and cumulative drug release of 97% proved to be superior than the tablet made with SD3.Conclusion: Conclusively, the SSD of meloxicam has the potential to be developed as fast acing formulation that can ensure almost complete release of drug.

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The main aim present work was to optimize fast dissolving tablet (FDT) formulation using response surface approach. The variables studied were sodium bicarbonate (X1), citric acid (X2), and superdisintegrant, Ac-Di-Sol (X3). The main aspect of present work was to develop FDT of Domperidone which possesses fast disintegration and high mechanical strength. It was found that the response was affected by all the three factors studied. The statistical models were successfully used to prepare FDT of Domperidone with fast disintegration (31.08 seconds) and adequate hardness (4.1 kg/cm(2)). Pharmacokinetic studies in rats showed statistically insignificant difference (p>0.05) between Domperidone fast dissolving tablet (DFDT) and market product. This concluded that optimized FDT is bioequivalent with the marketed formulation. The values of Tmax were found to be 0.5 h and 0.75 h for DFDT and reference product, respectively. Conditioned place aversion study was performed on Swiss Albino mice and the study showed the better anti emetic potency of optimized FDT in nauseated condition over market product (p<0.05). Thus, the present investigation conclusively demonstrates the potential role in terms of rapid disintegration and high mechanical strength.

: Introduction: Many nanoformulations have been designed and evaluated for ocular drug delivery system consistently. These nanoformulations are designed for prolonged retention and course time, stable, efficient and reversible drug loading. The ocular bioavailability is very less when the drug is given through topically. Various anatomical and physiological limitations, for example, tear turnover, nasal lachrymal waste, reflex squinting, and visual static and dynamic hindrances cause the challenges and delay the ocular drug permeation because of the limitation that less than 5% dose can reach into the ocular tissues. Different types of Polymeric micelles were prepared to overcome the above challenges. Polymeric nano micelles are prepared by different methods, such as direct dissolution, dialysis method, Oil-in-water emulsion, solvent evaporation, co-solvent evaporation, and freeze-drying method.

Due to poor bioavailability and chemical instability, the effectiveness of curcumin is negligible in the treatment of numerous diseases. Solid lipid nanoparticles (SLNs) increase the bioavailability of lipophilic compounds and protect the drug from gastrointestinal degradation. The objective of our study is the utilization of SLNs to improve the pharmacokinetics and pharmacodynamics of curcumin in the management of diabetes mellitus. Central composite design was used to prepare curcumin-loaded SLNs (Cur-SLN). The analysis of independent variables like drug concentration, lipid concentration, and surfactant concentration was carried out using analysis of variance (ANOVA) to obtain the optimized batch (optimized Cur-SLN) having the desired values of dependent variables particle size and entrapment efficiency. In vitro release, differential scanning calorimeter (DSC), transmission electron microscopy (TEM), and Fourier Transform Infra-Red (FTIR) studies of optimized Cur-SLN were carried out and then its pharmacokinetic and pharmacodynamic studies were performed. The model was found to be significant for particle size and entrapment efficiency based on F-value and p-value. The optimized batch's predicted values were in close agreement with the actual values of particle size and entrapment efficiency. TEM results confirm mono-dispersion and spherical shape of particles in the formulation. The DSC results confirmed the changing of drug from crystalline to amorphous form. Burst release followed by the sustained release was obtained in the in vitro release studies. The pharmacokinetic study shows enhanced bioavailability of optimized Cur-SLN compared with a plain drug suspension. The optimized Cur-SLN achieved higher antidiabetic activity in streptozotocin-induced diabetes mellitus rats than the plain drug suspension. SLNs can be used as a promising technique for delivering curcumin in the management of diabetes mellitus.