Current Drug Delivery - Volume 17, Issue 6, 2020

Eudragit® polymer has been widely used in film-coating for enhancing the quality of products over other materials (e.g., shellac or sugar). Eudragit® polymers are obtained synthetically from the esters of acrylic and methacrylic acid. For the last few years, they have shown immense potential in the formulations of conventional, pH-triggered, and novel drug delivery systems for incorporating a vast range of therapeutics including proteins, vitamins, hormones, vaccines, and genes. Different grades of Eudragit® have been used for designing and delivery of therapeutics at a specific site via the oral route, for instance, in stomach-specific delivery, intestinal delivery, colon-specific delivery, mucosal delivery. Further, these polymers have also shown their great aptitude in topical and ophthalmic delivery. Moreover, available literature evidences the promises of distinct Eudragit® polymers for efficient targeting of incorporated drugs to the site of interest. This review summarizes some potential researches that are being conducted by eminent scientists utilizing the distinct grades of Eudragit® polymers for efficient delivery of therapeutics at various sites of interest.

Drug nanocrystals offer an attractive approach for improving the solubility and dissolution rate of poorly soluble drugs which accounts for nearly 40 % newly discovered drug molecules. Both methods for manufacturing drug nanocrystals have high industrial acceptability for being simple and easy to scale which is evident from the number of approved products available in the market. Ability to modify multiple aspects of dosage form like bioavailability, release pattern and dosage form requirement along with flexibility in choosing final dosage form starting from the tablet, capsule, suspension to parenteral one, have made nanocrystal technology one of the very promising and adaptable technology for dosage form design.

Docosahexaenoic Acid (DHA) is an essential polyunsaturated omega-3 fatty acid, and a fundamental structural component of the phospholipid membranes, especially of neural and retinal cells. DHA is found to be critical for the normal development and functioning of neurons and synaptogenesis in the brain, and is required during pre- and post-natal stages of life. DHA has also been observed to exhibit neuroprotective, cardioprotective, and anti-inflammatory properties. However, geographical dietary variations and poor economic conditions lead to insufficient DHA levels resulting in various health deficits like improper brain development, cognitive disorders, and other clinical complications. Thus, to prevent its deficiency-induced derangements, several authorities recommend DHA as a supplement during pregnancy, infancy, and throughout adulthood. In past decades, the soft gelatin capsule was only feasible resolute of DHA, but due to their limitations and invention of new technologies; it led to the development of new dosage forms with improved physicochemical characteristics of DHA. This article will discuss in detail about the role of DHA in brain development, microalgae oil as an emerging source of DHA, clinical- and pharmacological-activities of DHA, issues related to DHA oil, current formulation of DHA along with their application, limitations, and strategies used for improvement and future prospectives.

Background: In many countries, hypertension in the pediatric population is considered a serious risk of mortality and morbidity. In this respect, it is central to design and develop new pharmaceutical forms for pediatric patients with hypertension. The development of Orodispersible Mini-Tablets (ODMTs) for pediatric use has gained importance in recent years. Therefore, regulations for developing suitable and palatable dosage forms for pediatric patients have been established by WHO authorities. Objective: This study aimed to design and develop orodispersible mini tablets of enalapril maleate (EnM ODMTs) for pediatric use. Methods: Five pharmaceutical formulations (A, B, C, D and E, shown in Table 1) were designed. The effects of different co-processed excipients and active pharmaceutical ingredients at different doses were studied. Lactose co-processed excipients selected were the following: Tablettose® 80, Microce- Lac® 100 and StarLac®. The micromeritic properties for all the physical mixtures were examined. The mini tablets were obtained by direct compression. Quality control parameters were determined in accordance with US Pharmacopeia. Results: Three OMDTs with StarLac® showed good results of hardness, flow ability and fast disintegration. The formulation with 0.1 mg of enalapril maleate presented the best results for the official parameters of hardness (4.0 kp), friability (< 1%), disintegration time (28 s), drug content uniformity (103.6 %), and wetting time (23 s). Conclusion: The three OMDTs with StarLac® showed good quality parameters, according to official requirements. Formulation A exhibited the best wetting time, complying with the dose recommended for pediatric patients. This formulation could be considered eligible for being manufactured at industrial scale.

Background: Mathematical modeling in modified drug release is an important tool that allows predicting the release rate of drugs in their surrounding environment and elucidates the transport mechanisms involved in the process. Objective: The aim of this work was to develop a mathematical model that allows evaluating the release profile of drugs from polymeric carriers in which the swelling phenomenon is present. Methods: Swellable matrices based on ionic complexes of alginic acid or carboxymethylcellulose with ciprofloxacin were prepared and the effect of adding the polymer sodium salt on the swelling process and the drug release was evaluated. Experimental data from the ciprofloxacin release profiles were mathematically adjusted, considering the mechanisms involved in each stage of the release process. Results: A proposed model, named “Dual Release” model, was able to properly fit the experimental data of matrices presenting the swelling phenomenon, characterized by an inflection point in their release profile. This entails applying the extended model of Korsmeyer-Peppas to estimate the percentage of drug released from the first experimental point up to the inflection point and then a model called Lumped until the final time, allowing to adequately represent the complete range of the drug release profile. Different parameters of pharmaceutical relevance were calculated using the proposed model to compare the profiles of the studied matrices. Conclusion: The “Dual Release” model proposed in this article can be used to predict the behavior of complex systems in which different mechanisms are involved in the release process.

Background: Developing a new excipient and obtaining its market approval is an expensive, time-consuming and complex process. Compared to that, the co-processing of already approved excipients has emerged as a more attractive option for bringing better characteristic excipients to the market. The application of the Design of Experiments (DoE) approach for developing co-processed excipient can make the entire process cost-effective and rapid. Objective: The aim of the present investigation was to demonstrate the applicability of the DoE approach, especially 32 full factorial design, to develop a multi-functional co-processed excipient for the direct compression of model drug - cefixime trihydrate using spray drying technique. Methods: The preliminary studies proved the significant effect of atomization pressure (X1) and polymer ratio (microcrystalline cellulose: mannitol - X2) on critical product characteristics, so they were selected as independent variables. The angle of repose, Carr’s index, Hausner’s ratio, tensile strength and Kuno’s constant were selected as response variables. Result: The statistical analysis proved a significant effect of both independent variables on all response variables with a significant p-value < 0.05. The desirability function available in Design Expert 11® software was used to prepare and select the optimized batch. The prepared co-processed excipient had better compressibility than individual excipients and their physical mixture and was able to accommodate more than 40 percent drug without compromising the flow property and compressibility. Conclusion: The present investigation successfully proved the applicability of 3² full factorial design as an effective tool for optimizing the spray drying process to prepare a multi-functional co-processed excipient.