Nowadays exploration of novel lipid-based formulations is akin to a magnet for researchers worldwide for improving the in vivo performance of highly lipophilic drugs. Over the last few years, new compositions of lipids have been developed, and the probable bioavailability enhancement has been investigated. We reviewed the most recent data dealing with backlogs of conventional lipid-based formulations such as physical instability, limited drug loading capacities, drug expulsion during storage along with all the possible hindrances resulting in poor absorption of highly lipophilic drugs such as P-glycoprotein efflux, extensive metabolism by cytochrome P450 etc. In tandem with these aspects, an exclusive formulation approach has been discussed in detail in this paper. Therefore, this review focuses on resolving the concerned ambiguity with successful oral administration of highly lipophilic drugs through designing novel lipidic formulations (nanostructured lipid carriers [NLC]) that constitute a blend of solid and liquid lipids. The article highlights the potential role of such formulation in normalizing the in vivo fate of poorly soluble drugs. Finally, the present manuscript discusses the dominance of NLC over other lipid-based formulations and provides a perspective of how they defeat and overcome the barriers that lead to the poor bioavailability of hydrophobic drugs.

Needle free injection technology (NFIT)is an extremely broad concept which include a wide range of drug delivery systems that drive drugs through the skin using any of the forces as Lorentz, Shock waves, pressure by gas or electrophoresis which propels the drug through the skin, virtually nullifying the use of hypodermic needle. This technology is not only touted to be beneficial for the pharma industry but developing world too find it highly useful in mass immunization programmes, bypassing the chances of needle stick injuries and avoiding other complications including those arising due to multiple use of single needle. The NFIT devices can be classified based on their working, type of load, mechanism of drug delivery and site of delivery. To administer a stable, safe and an effective dose through NFIT, the sterility, shelf life and viscosity of drug are the main components which should be taken care of. Technically superior needle-free injection systems are able to administer highly viscous drug products which cannot be administered by traditional needle and syringe systems, further adding to the usefulness of the technology. NFIT devices can be manufactured in a variety of ways; however the widely employed procedure to manufacture it is by injection molding technique. There are many variants of this technology which are being marketed, such as Bioject® ZetaJetTM , Vitajet 3, Tev-Tropin® and so on. Larger investment has been made in developing this technology with several devices already being available in the market post FDA clearance and a great market worldwide.

Introduction: Development of novel biomaterials for drug delivery which forms a part of the so called novel drug delivery systems has always been exhilarating. Mechanical evaluation of polymer based topical gels, which would be subjected to load or stress during its application, is inevitable. Methods: Rheological characterization was done by studying viscosity and yielding. Rheological modeling was also carried out. Results: The viscosity and yield stress were inversely dependent on the eugenol concentration. The gels followed Herschel-Bulkley and Bingham rheological models. Conclusion: Nanodroplets are colloidal systems and the microstructural changes in the Carbopol based nanodroplet gels were unveiled using rheometry.

Background: The aim of the present study was to formulate and optimize the self-emulsifying drug delivery systems (SEDDS) of nevirapine (NVP) by use of 2 ² factorial designs to enhance the oral absorption of NVP by improving its solubility, dissolution rate, and diffusion profile. SEDDS are the isotropic mixtures of oil, surfactant, co-surfactant and drug that form oil in water microemulsion when introduced into the aqueous phase under gentle agitation. Materials and Methods: Solubility of NVP in different oils, surfactants, and co-surfactants was determined for the screening of excipients. Pseudo-ternary phase diagrams were constructed by the aqueous titration method, and formulations were developed based on the optimum excipient combinations with the help of data obtained through the maximum micro emulsion region containing combinations of oil, surfactant, and co-surfactant. The formulations of SEDDS were optimized by 2 ² factorial designs. Results: The optimum formulation of SEDDS contains 32.5% oleic acid, 44.16% tween 20, and 11.9% polyethylene glycol 600 as oil, surfactant, and co-surfactant respectively. The SEDDS was evaluated for the following drug content, self-emulsification time, rheological properties, zeta potential, in vitro diffusion studies, thermodynamic stability studies, and in vitro dissolution studies. An increase in dissolution was achieved by SEDDS compared to pure form of NVP. Conclusion: Overall, this study suggests that the dissolution and oral bioavailability of NVP could be improved by SEDDS technology.

Background: Hydrogel is a cross-linked network of polymers. Water penetrates these network causing swelling and giving the hydrogel a soft and rubbery consistency and there by maintaining the integrity of the membrane. Due to the drawback of conventional therapy for ocular delivery, hydrogel membranes containing the combination of gentamicin (GT) sulfate and dexamethasone (DX) were formulated for the treatment of conjunctivitis. The objective of this study was to formulate and evaluate the hydrogel membranes containing the combination of GT and DX for the treatment of conjunctivitis. Materials and Methods: In the present investigation, hydrogel membranes were prepared by using polymers such as gelatin, polyvinyl alcohol, and chitosan, which were cross-linked using physical/chemical methods. Results: The cross-linking of the membranes was confirmed by Fourier transform infra-red studies. The pH of the membranes ranged from 7.19 to 7.45 and drug content ranged from 69.82% to 89.19%. The hydrogels showed a considerably good swelling ratio ranging from 22.5% to 365.56%. The in vitro drug release study showed that there was a slow and sustained release of the drug from the membranes which were sufficiently cross-linked and followed zero order release. In vivo studies showed that the severity of conjunctivitis was remarkably lowered at day 3 with hydrogel membrane compared to marketed eye drops. Results of unpaired t-test of significance between two groups indicated that the hydrogel membrane showed a better response in the treatment of conjunctivitis compared to the marketed products. Stability studies proved that the formulations could be stable when stored at room temperature. Conclusion: Results of the study indicated that it is possible to develop a safe and physiologically effective hydrogels which are patient compliant.

Aim and Background: Pregabalin (PRG), an analog of gamma-aminobutyric acid, reduces the release of many neurotransmitters, including glutamate, and noradrenaline. It is used for the treatment of epilepsy; simple and complex partial convulsion. The present research work aims to ensure a high drug absorption by retarding the advancement of PRG formulation through the gastrointestinal tract. The work aims to design a controlled release PRG formulation which is administered as liquid and further gels in the stomach and floats in gastric juice. Materials and Methods: In situ gelling formulations were prepared using sodium alginate, calcium chloride, sodium citrate, hydroxypropyl methylcellulose (HPMC) K100M, and sodium bicarbonate. The prepared formulations were evaluated for solution viscosity, drug content, in vitro gelling studies, gel strength, and in vitro drug release. The final formulation was optimized using a 3 ² full factorial design. Results: The formulation containing 2.5% w/v sodium alginate and 0.2% w/v calcium chloride were considered optimum since it showed minimum floating lag time (18 s), optimum viscosity (287.3 cps), and gel strength (4087.17 dyne/cm ² ). The optimized formulation follows Korsmeyer-Peppas kinetic model with n value 0.3767 representing Fickian diffusion mechanism of drug release. Conclusion: Floating in situ gelling system of PRG can be formulated using sodium alginate as a gelling polymer and calcium chloride as a complexing agent to control the drug release for about 12 h for the treatment of epilepsy.

Introduction: The work was aimed to develop an enteric-coated hydroxypropyl methylcellulose (HPMC) capsules (ECHC) plugged with 5-fluorouracil (5-FU)-loaded microsponges in combination with calcium pectinate beads. Materials and Methods: The modified quasi-emulsion solvent diffusion method was used to prepare microsponges. A 3 ² factorial design was employed to study the formulation and the effects of independent variables (volume of organic solvent and Eudragit-RS100 content) on dependent variables (particle size, %entrapment efficiency, and %cumulative drug release). The optimized microsponge (F4) was characterized by scanning electron microscopy, powder X-ray diffraction, and thermogravimetric analysis. F4 was plugged along with the calcium pectinate beads in HPMC capsules coated with enteric polymer Eudragit-L100 (Ed-L100) and/or Eudragit-S100 (Ed-S100) in different proportions. An in vitro release study of ECHC was performed in simulated gastric fluid for 2 h, followed by simulated intestinal fluid for next 6 h and then in simulated colonic fluid (in the presence and absence of pectinase enzyme for further 16 h). The optimized formulation was subjected to in vivo roentgenographic and pharmacokinetic studies in New Zealand white rabbits to analyze the in vivo behavior of the developed colon-targeted capsules. Results: Drug release was retarded on coating with Ed-S100 in comparison to a blend of Ed-S100:Ed-L100 coating. The percentage of 5-FU released at the end of 24 h from ECHC3 was 97.83 ± 0.12% in the presence of pectinase whereas in the control study, it was 40.08 ± 0.02%. Conclusion: Thus, enteric-coated HPMC capsules plugged with 5-FU-loaded microsponges and calcium pectinate beads proved to be a promising dosage form for colon targeting.

Purpose: The aim of the present work was to improve rate of dissolution and processing parameters of BCS class II drug, chlorzoxazone using cogrinding technique in the presence of different excipients as a carrier. Materials and Methods: The drug was coground with various carriers like polyethylene glycol (PEG 4000), hydroxypropyl methylcellulose (HPMC) E50LV, polyvinylpyrrolidone (PVP)K30, Kaolin and Neusilin US2 using ball mill, where only PEG 4000 improved dissolution rate of drug by bringing amorphization in 1:3 ratio. The coground mixture after 3 and 6 h was evaluated for various analytical, physicochemical and mechanical parameters. Results: The analysis showed conversion of Chlorzoxazone from its crystalline to amorphization form upon grinding with PEG 4000. Coground mixture as well as its directly compressed tablet showed 2.5-fold increment in the dissolution rate compared with pure drug. Directly compressible tablets prepared from pure drug required a large quantity of microcrystalline cellulose (MCC) during compression. The coground mixture and formulation was found stable in nature even after storage (40°C/75% relative humidity). Conclusions: Cogrinding can be successfully utilized to improve the rate of dissolution of poorly water soluble drugs and hence bioavailability.

Introduction: The insect repellent compounds are used to protect humans, animals and plants against insect bites. Aromatic amides have insect repellent effects. N,N-diethyl-meta-toluamide (DEET) (C ₁₂ H ₁₇ NO) is one of the best insect repellents has been used for many years. DEET is a colorless, odorless liquid that is approximately insoluble in water and soluble in glycerin, ethanol, and isopropyl alcohol. Due to the solubility problem of DEET, its topical formulations usually have alcoholic bases, but these kind of formulations increase skin permeation and also systemic absorption of DEET, which leads to some toxic effects. The main goal of this study was to prepare the formulation of DEET niosomes in a topical dosage form with suitable stability properties. Materials and Methods: Three different methods were used to prepare niosome formulations: Dehydration rehydration vesicle method, direct mixing method, homogenizer method. Sorbitan surfactants, cholesterol, polyoxyethylenecetyl, phosphate buffer (pH 7.4), and charge inductive compounds like cetyltrimethylammonium bromide were used to provide a net negative charge to the final membrane structure. A high-performance liquid chromatography method was then used for the determination of the loaded DEET. Results: A large number of niosomes were multi-layered and have a spherical shape. In comparison, syringe method against direct mixing is more appropriate because of creation MLV and uniform niosomes but the best method is homogenizer method. Drug entrapment was between 14% and 21% in selected formulation. Conclusion: According to this study, homogenizing method can be used for formulation of DEET in niosome form in topical formulations.

Introduction: The objective of the present investigation was to develop a novel multifunctional directly compressible co-processed excipient consisting of dibasic calcium phosphate anhydrous, polyethylene glycol 4000 (PEG 4000) and crospovidone using Box-Behnken design. Materials and Methods: The technique of melt granulation was adopted for the preparation of the co-processed excipient. The percentage of crospovidone (5-10% w/w), percentage of PEG 4000 (5-15% w/w) and the heating time (4-12 min) were selected as independent variables. The co-processed granules were evaluated for bulk density, tapped density, Hausner's ratio and Carr's index. Placebo tablets of co-processed granules were prepared and evaluated for hardness, friability and disintegration time. Multiple linear regression was applied to develop mathematical models for hardness, Carr' index and disintegrating time. ANOVA was applied to study the fitting and significance of the model. The optimized batches (BB) were selected for further studies. The selected batches were characterized for particle size distribution, granular friability index, moisture uptake study, differential scanning calorimetry, Fourier transform infrared spectroscopy and scanning electron microscopy. Aceclofenac was selected as model drug for the preparation of tablets. Results: Aceclofenac tablets prepared using co-processed excipients showed better hardness, disintegration time and in vitro drug release as compared to aceclofenac tablets prepared using conventional wet granulation method. Conclusion: The developed co-processed excipient can serve as a novel co-processed excipient for improvement of tableting characteristics.

Introduction: Choline bitartrate (CBT) is a vital nutrient for fetal brain development and memory function. It is hygroscopic in nature which is associated with stability related problem during storage such as development of fishy odor and discoloration. Aim: Microencapsulation method was adopted to resolve the stability problem and for this hydrogenated soya bean oil (HSO) was used as encapsulating agent. Materials and Methods: Industrially feasible modified extrusion-spheronization technique was selected for microencapsulation. HSO was used as encapsulating agent, hydroxypropyl methyl cellulose E5/E15 as binder and microcrystalline cellulose as spheronization aid. Formulated pellets were evaluated for parameters such as flow property, morphological characteristics, hardness-friability index (HFI), drug content, encapsulation efficiency, and in vitro drug release. The optimized formulations were also characterized for particle size (by laser diffractometry), differential scanning calorimetry, powder X-ray diffractometry (PXRD), Fourier transform infrared spectroscopy, and scanning electron microscopy. Results and Discussions: The results from the study showed that coating of 90% and 60% CBT was successful with respect to all desired evaluation parameters. Optimized formulation was kept for 6 months stability study as per ICH guidelines, and there was no change in color, moisture content, drug content, and no fishy odor was observed. Conclusion: Microencapsulated pellets of CBT using HSO as encapsulating agent were developed using modified extrusion spheronization technique. Optimized formulations, CBT 90% (F5), and CBT 60% (F10), were found to be stable for 4M and 6M, respectively, at accelerated conditions.