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The existence of 3D printing (3DP) ways back to 1992, and its sound presence in the pharmaceutical industry was made in 2015 by the launch of 1st 3D printed drug, Spritam was manufactured by Aprecia Pharmaceuticals. Implementation of 3DP is escalating in the number of industries, including the pharmaceutical industry. The purpose of this review paper is to briefly discuss types of 3DP and their role in formulating novel dosage forms. Binder jet printing, VAT polymerization, powder bed fusion, and material extrusion are briefly explained along with an example of their implementation in the formulation of the dosage form. A few novel dosage forms which can bypass the first-pass metabolism and how 3D printing is useful in formulating them as been discussed. It also includes a comparison of the process of 3D printed tablets and conventional methods of manufacturing. The significance of 3D printing in novel dosage form and augmenting 3DP with hot-melt extrusion (HME) method is discussed. The regulatory concerns in adopting this technology on a large-scale are addressed. 3DP technology could rapidly print transdermal needles, buccal patches, and different shapes of vaginal rings and proved it can be a versatile tool in formulation technology. As the pharmaceutical industry involves stringent regulations, certain aspects need to be considered by regulatory authorities before implementing this tool into commercialscale manufacturing.

The objective of the study is to formulate Solid Self Emulsifying Drug Delivery System (SEDDS) for improvement of solubility and dissolution of poorly water-soluble drug Lercanidipine Hydrochloride which has very less water solubility (0.000165mg/mL) and absolute bioavailability of 10%. The Liquid Self Emulsifying Drug Delivery System concentrate was prepared using different oils, surfactants and cosurfactants which were screened based on saturation solubility studies. The SEDDS prepared using oil like peppermint oil, surfactant as propylene glycol, cosurfactant as PEG 400 showed very good self-emulsification property. The prepared SEDDS were subjected for evaluation of various parameters like self-emulsification property, FTIR studies, DSC studies, viscosity, globule size determination, zeta potential determination, robustness to dilution, thermodynamic stability studies. Liquid SEDDS showed good emulsification with globule size 357.2 nm and PDI 0.491. The optimized SEDDS formulation with 20% peppermint oil, 7% propylene glycol surfactant, 63% PEG 400 cosurfactant and 10% drug was used for the preparation of Solid SEDDS following physical adsorbent technique using Avicel PH 101 as an inert solid adsorbent in 1:4 ratio. The prepared solid SEDDS with free-flowing property were compressed as tablets and evaluated for hardness, friability, drug content, disintegration and dissolution studies. The results of our study conclude that the Avicel PH 101 can be used for the preparation of solid SEDDS to improve the solubility and dissolution of poorly water-soluble drug Lercanidipine Hydrochloride.

Diffusion of the drug from a formulation and across membranes simulating biological cell membranes is the major concern to be taken under consideration while formulating any dosage form. This brings on a major role in those which are to be applied along the skin, since drug needs to first release from the polymer matrix then enter systemic circulation via the skin. The purpose of the study was to compare the dispersion rate of diclofenac sodium from the gel formulation across five different synthetic membranes. In this work, we worked to measure the drug release profile using and using various kinetic models, found out the mechanism of diffusion through membranes on the drug release profile. The evaluation was done by an in vitro drug release system in the laboratory using Franz diffusion cell. Diclofenac sodium topical gel was formulated using carbopol 934 as the gel-forming agent(1). Diffusion studies showed that the highest release was given by mixed cellulose ester membrane (83.16%) in 71.5 hrs. Followed by cellulose acetate membrane (78.1%), cellulose acetate nitrate membrane (75.6), polyether sulphone membrane (70.8%) and sigma cellulose membrane (56.39%). Drug release followed first-order kinetics and Higuchi's model of diffusion from all the membranes with case II and super case II transport mechanisms

Solubility enhancement of poorly soluble drugs for improved oral absorption has become a challenging task for the scientists in the development of pharmaceuticals. The main goal of this study is to investigate the effect of the hydrophilic polymers on the poorly water soluble drug to enhance its solubility through the technique of hotmelt extrusion. The drug selected for this study is paracetamol and the hydrophilic polymers selected for this study are polyox, carbopol 980p, and PEG 6000. The drug and the polymer at a ratio of 1:2 was processed through STEERLife twin screw extruder. The obtained solid dispersion was subjected to the saturation solubility study. Among the selected polymers, paracetamol with polyox polymer has shown enhanced solubility followed by PEG 6000 and carbopol 980p.

Background In the present day scenario, where novel drug delivery system and controlled drug delivery systems have been developed over the conventional oral solid dosage forms, pellets emerged as a versatile delivery system. Pelletization is a technique to obtain pellets or spherical particles having a dimensions between 0.5 - 1.5 mm. These multiparticulate systems are either compressed into tablets or filled into capsules. Area covered The following review provides a brief outline on pelletization. In this review, we have discussed on various parameters affecting pelletization, different techniques of pelletization and assessment of pellets. Expert opinion It is expected that the pellatizaiton is an effective and efficient approach which can help in improvement of absorption, bioavailability, stability, etc. Pellets can offer therapeutic advantages with effordable cost. Several studies are performed to address the limitations of numerous drugs.

This work was aimed to improve solubility and dissolution rate of carbamazepine (CBZ), an antiepileptic, BCS class II drug by using different solubility enhancement techniques. Self-nanoemulsifying drug delivery system (SNEDDS) and solid dispersions of CBZ was attempted by spontaneous emulsification method and fusion method, respectively. The solubility studies of pure CBZ was performed in different oils, surfactants and co-surfactants. Very small amount of CBZ (20 mg) could be incorporated in SNEDDS, however the solid dispersion of CBZ using Soluplus® was successfully prepared with the required dose. The solid dispersion was characterized and evaluated for saturation solubility, in vitro dissolution studies, solid state characterization such as fourier transform infrared spectroscopy (FTIR) and powder X-ray diffraction studies (XRD). Based on the results, it can be concluded that the due to increased solubility and the dissolution, the bioavailability of CBZ could be improved by preparing solid dispersion

Lumefantrine is a BCS class -II drug having a poor aqueous solubility. There is a need for improvement in solubility, in order to enhance the therapeutic efficacy and reduce the dose. Hence in the present work, the solubility of lumefantrine is enhanced by formulating solid dispersions of lumefantrine using a hot melt extrusion process in a twin-screw processor using three different polymers such as Kollidon VA64, Soluplus and HPMC AS at a weight ratio of 1:2, 1:3 and 1:4, processed at different barrel temperatures and screw speeds. The obtained solid dispersions were characterized by differential scanning calorimetry and solubility studies. Solid dispersions prepared with KollidonVA64 and Soluplus showed a clear extrudate indicating a complete amorphous conversion of the lumefantrine at all the three ratios evaluated. Increase in polymer concentration, increased the solubility of the lumefantrine. With Kollidon VA 64 and Soluplus, lumefantrine to polymer ratio of 1:4 showed the highest increase in solubility, compared to that of the pure lumefantrine.

N-acetylcysteine (NAC), a precursor and a source of glutathione, which has been used for past four decades, with well-established safety, widely used for the treatment of acetaminophen poisoning and as a mucolytic. NAC also would be administered in combination with certain drugs, imparting beneficial effects and having a medical rationale. NAC is a molecule having a wider therapeutic index with a broad spectrum of prophylactic and therapeutic applications and has become an important social need. Research is ongoing to understand the various pharmacological and biochemical pathways by which NAC exhibits various therapeutic effects. Clinical uses of NAC is attributed, to the presence of thiol group, which acts as a direct antioxidant and also replenishes glutathione levels, which is decreased in various disease conditions. This review aims to understand the role of NAC in various clinical conditions. The article concludes that NAC may be beneficial in some conditions, especially in patients with depleted glutathione, or with oxidative stress, for which patients can be screened before prescribing NAC.

The aim of the work was to prepare co-crystals of irbesartan (IBS), a BCS Class II drug to enhance its aqueous solubility and bioavailability. The solvent evaporation method was used to prepare co-crystals by using different co-formers and varying the drug to co-former molar ratios. Succinic acid and benzoic acid co-crystals were formed with good physicochemical properties. The solid-state characterization of co-crystals was studied by FTIR, DSC, and XRD. The co-crystals were evaluated for the saturation solubility and dissolution studies. There was a 2-fold increase in the aqueous solubility and 4-8 fold increase in dissolution rate of co-crystals. Solid state characterizations indicated there was no change in the chemical nature of the co-crystals compared to pure drug. Presence of crystalline co-former induced crystallinity to the developed co-crystals. Thus, developed co-crystals were found to be a suitable alternative to increase the solubility and dissolution rate of IBS.

Solubility is defined as dissolution of a solute in a solvent to give a homogenous system. It is an important consideration which is required to achieve appropriate drug concentration in systemic circulation for a chosen pharmacological response. With innovation in technologies, the discoveries of drugs having better efficacy are restricted due to poor solubility, despite having clinical efficacy. Hence it has become a major challenge. More than 50% new chemical entities produced in pharmacy industry are practically insoluble in water. Nano crystals have potential to overcome this issue. They have size in nanometer range (mean diameter < 1000nm) which changes the drug properties dramatically. This review article summaries different methods of preparation, various production technologies available currently in industries; evaluation techniques, applications of nano crystal formulation, future trends and challenges of nano crystal formulation, and various marketed dosage forms developed using nano crystals are discussed.

Nowadays ophthalmic route of administration of drugs is rapidly progressing and more studies are going on in formulating ophthalmic drug delivery systems. There are many conventional dosage forms available in the market like ointments, eye drops etc. The main drawback with these types of formulations is rapid drainage of the instilled dose due to the lacrimal fluid secretions and blinking of the eye lids. In order to minimize this drainage and to increase the ocular residence time and corneal contact time, in situ gel forming formulations are developed. In these systems sol to gel transformation takes place due to the environmental changes like pH, temperature, ionic strength. Some polymers like sodium alginate, HPMC are frequently used to initiate these processes. These formulations can be assessed for viscosity, clarity, gel strength, gelling capacity, gelling time, texture, isotonicity, sterility, ocular irritancy, anti-microbial efficacy, in vitro drug release, ex vivo release, in vivo absorption, in vivo retention and stability.

Nabumetone is a Non-steroidal anti-inflammatory drug (NSAID) which belongs to a drug class which provide antipyretic and analgesic effects in lower doses and anti-inflammatory effects in higher doses. A simple, highly sensitive, accurate and isocratic RP-HPLC stability-indicating method was developed and validated for determination nabumetone by using Cosmosil C18(150x4.6mm, 5μm) column using Acetonitrile: water pH-5 (55:45 %v/v) as mobile phase at a flow rate of 0.8ml/min. The detection was done by using PDA(Photo diode array) detector at 229nm. Calibration curves for all drugs were in the range of 0.125-8 μg/ml and the linear regression coefficients were more than 0.999. Recovery rate was in the range 98.8% to 100.5%. The limits of detection was found to be 0.035μg/ ml. Also, the limits of quantification was 0.107 μg/ml. Repeatability and Intermediate precision was done and the % RSD was found to be less than 1%, by changing few method parameters robustness was evaluated which has shown %RSD of less than 2%. Study aimed to conduct forced degradation studies and develop a simple, effective method which can effectively separate drug from its degradation products. This study was conducted at multiple time points to estimate the rate of degradation. Stress testing was done for acidic degradation, basic degradation, neutral hydrolytic degradation, oxidative degradation,dry heat degradation and Photo stability study. The order of stability for Nabumetone was found to be H2O2

The approach for drug delivery has changed vastly with the use of nanotechnology, polymeric system and target drug delivery. One such a way to increase the bioavailability of a drug which is poorly water soluble, is nanoemulsion. Nanoemulsion is a system where one of immiscible liquid dispersed within another immiscible liquid as droplets leading to transparent emulsions. The surface characteristics of these droplets of nanoemulsion play an important role in the biological behavior of the formulation. The methods used for the preparation of nanoemulsions include high pressure homogenization, microfluidization, ultrasonication, and spontaneous emulsification. As application point of view nanoemulsions are crucial in different fields such as pharmaceutics, food technology and cosmetics. Here in this review, different features of nanoemulsion has been discussed along with the method of preparations,applications & advantages over other dosage forms.

The aim of the work was to prepare co-crystals of valsartan, a BCS Class II drug to enhance its aqueous solubility and bioavailability. The solvent evaporation method was used to prepare co-crystals by using different co-formers and varying the drug to co-former molar ratios. Succinic acid was found to be suitable co-former to prepare co-crystals with good physico-chemical properties. The solid state characterization of co-crystals were studied by FTIR, DSC and XRD. The co-crystals were evaluated for the saturation solubility and dissolution studies. Solubility study in distilled water indicated low solubility of valsartan (198.5 μg/ml), there was 2.6 fold increase in the solubility of co-crystals prepared using succinic acid, with 1: 5 drug to co-former ratio (520.6 μg/ml). Solid state characterizations indicated there was no change in the chemical nature of the co-crystals compared to pure drug. Presence of crystalline co-former induced crystallinity to the developed co-crystals. Thus developed co-crystals were found to be suitable alternative to increase the solubility and dissolution rate of valsartan.

Electronics is deemed to have tremendous scope in the improvement of diagnostic and drug delivery devices. Miniaturization of microprocessors, along with development of biocompatible semiconductor materials can offer breakthrough in drug therapy tomorrow. Controlled drug delivery systems based on polymeric materials have captured the market replacing the conventional formulations. The author discuss the current development in the field of bioelectronics towards electronic drug delivery systems (EDDS) proposing the emergence of new subject specialties in the field of electronics and pharmaceutics that may be termed as ‘pharmacoelectronics’ and ‘electro pharmaceutics’. Many technological advancements like ActipatchTM, Intellicap®, Smart bandages etc are discussed. The basic electronic components incorporated in an electronic drug delivery device may be the drug reservoir, a power source, pumping system, microcontroller, various sensors for ambient temperature, pH, osmotic pressure, light, ion concentrations etc. The study of basic electronics and these electronic components may be an integral part of training for a future pharmaceutical formulation scientist.

The purpose of this study was to develop dual-release bilayer tablets of fexofenadine HCl and montelukast sodium (MKS) to treat the individuals getting symptoms of asthma and allergic rhinitis at late night and early morning which may lead to breathing and respiratory problem. The bilayer tablet was designed to contain fexofenadine for the immediate release and MKS for the extended release matrix. MKS and fexofenadine tablets were prepared separately by direct compression method. The optimized tablets were compressed to obtain bilayer tablets. The tablets were evaluated for various physicochemical parameters and dissolution study. Further, the bilayer tablets were subjected to accelerated stability study. The fexofenadine tablet showing more than 75% release in 15 min and MKS tablet showing more than 90% release at the end of 7 h with 2 h of initial lag time were compressed one above the other to obtain bilayer tablet. The similar release pattern was observed with the bilayer tablets as that of individual tablets. The bilayer tablets were found to be stable at the end of 6 months storage period as per ICH guidelines. Both the layers of the bilayer formulation showed desired drug release at the end of time period, these could be effective formulations in late night and early morning symptoms of asthma and allergic rhinitis.

The Poor Solubility of Drugs is a major problem which limits the development of highly potent pharmaceutics. Solubility Enhancement is one of the important parameters which should be considered for those drugs having poor aqueous solubility. Drugs belonging to Biopharmaceutical Classification System (BCS) class II are characterized by low aqueous solubility and high physiological permeability. Solid Dispersion Method Technique and Effervescence Assisted Solid Dispersion Techniques using Modified Fusion Method are the process to enhance the solubility of poorly water soluble drugs. In this work, BCS class-II drugs Clarithromycin was used as a model drugs, having poor solubility but high permeability is individually incorporated with Mannitol, Citric acid, and Sodium bicarbonate (Hydrophilic Carriers used as Excipients) in different ratio respectively. SDMs of Clarithromycin were prepared melting (Fusion) method using Mannitol. EASDs of Clarithromycin were prepared using Modified Fusion Method. Mannitol was melted and in this molten mannitol Citric acid (organic acid) was added and uniformly mixed by continuous stirring. Solubility of Drug Powders, Solid Dispersion, and EASDs was determined at 25 C using shake flask method. The aqueous solubility of Clarithromycin were estimated using a U.V. spectrophotometer at 241nm (?max). Scanning electron Micrographs, FTIR, DSC and PXRD CLN of drug powders, solid dispersion, and EASDs were compared. Scanning electron micrographs of EASDs showed better uniform distribution of drug particles in the carrier matrix. The present technique is better suitable for drugs having a low melting point or melt without charring. Effervescence assisted fusion technique of preparing solid dispersions can be employed for enhancing solubility of poorly soluble drugs.

Epigallocatechin-3-gallate (EGCG) is a potent antioxidant and free radical scavenger present in green tea. It is extensively used as antioxidant, immunomodulator, anticancer, neuroprotective, cardioprotective, antiviral,antibacterial, photo protective and anti aging agent. The objective of the present work was to develop and validate an RP-HPLC method for determination of EGCG in lipid based nanoformulations. RP-HPLC analysis was performed by isocratic elution using a Phenomenex C18 column (4.6 × 250 mm, 5 µm) at 25 °C. A mixture of acetonitrile and 1% v/v acetic acid (25:75) of pH 2.8 was used as a mobile phase with a flow rate of 0.8 mL/min. The analysis was performed using a UV detector at 280 nm. The results showed that the peak area response was linear within the concentration range of 0.5-40 µg/mL (r =0.9998). The values of LOD (limit of detection) and LOQ (limit of quantification) were 0.125 µg/mL and 0.272 µg/mL respectively. The % RSD for peak area of intraday and interday precision was 0.08 and 0.2%, respectively. The results of accuracy for the different concentrations of EGCG (8, 10 and 12 μg/mL) were 100.29±0.19, 101.10±0.10 and 100.44±0.25 % respectively. The validated method was successfully applied for the estimation of EGCG content in lipid based nanoformulations.

Solubility of the drug plays a crucial role in the formulation and development of the drug. Assessing the solubility of the drug is one of the most important parameter in pre-formulation. Parenteral formulations require sufficient solubility of the drug molecules. Correspondingly bioavailability from solid formulations like tablets and capsules is also dependent on solubility and permeability. The objective of this study was to investigate the solubility of drug in different pH medium using UV visible spectrophotometer. The drug solubility was studied in the pH range 1.2 to 7.4. This study concludes that the naproxen has pH dependent solubility.

With the advent of modern technologies, a large number of drugs have been discovered which have a better efficiency but their clinical application is restricted due to poor water solubility. Nearly 40% of the drugs in the pipeline and around 60% of compounds coming directly from synthesis have poor solubility. Poor water solubility has become a leading challenge for the formulation of these compounds. Poor solubility is generally associated with poor bioavailability. Nanocrystals have the potential to overcome this issue. Change of materials into the nanodimension dramatically changes its physical properties which were used in pharmaceutics to develop a new innovative formulation principle for poorly soluble drugs: the drug nanocrystals. Drug nanocrystals are crystals with a size in the nanometer range (mean diameter < 1000 nm). The present article describe the details about the drug nanocrystals. Drug nanocrystals consist of poorly soluble drug without matrix material means carrier free drug delivery system. The review article includes method of preparation, properties, advantages of nanocrystals and application of nanocrystals through all routes of administration.