Recent Patents on Drug Delivery & Formulation - Volume 12, Issue 1, 2018

Background: From the past few decades, remarkable awareness has laid on the use of herbal medicines in pharmaceutical research. Thymoquinone (TQ), the main chemical constituent of Nigella Sativa (NS) plant, has been extensively explored, and revealed an array of therapeutic benefits, in different in vitro, and in vivo conditions. This review provides brief outline of the diverse therapeutics actions of TQ, and NS, viz. anti-oxidant, anti-inflammatory, anti-cancer, anti-diabetic, gastroprotective, hepato-protective, anti-microbial and anti-histaminic. Besides, a special emphasis has given on the use of colloidal drug delivery systems exploited hitherto, for the effective delivery of TQ and NS. Objective: The main objective of the review was to include an intensive patent literature, available on TQ and NS, for its usefulness in different therapeutic conditions. Methods: We embarked an organized search of bibliographic databases for peer-reviewed research literature and patent databases. The characteristics of screened papers were described, and a rational qualitative content analysis approach was applied to analyze the interventions and findings of included studies using a theoretical framework. Results: In the past, various studies have carried out which undoubtedly vouch for the multifarious therapeutic roles of TQ in an array of different diseases. More than 670 research papers and around 50 review articles are available on TQ and NS in PubMed database until now, suggesting its high significance. Around 12 review articles published only on the anticancer potential, while the others on its anti- inflammatory and anti-oxidant potential. Around 120 papers included in the review revealed the therapeutic benefits of TQ. In addition to this, an intensive patent literature is also available on TQ and NS, for its usefulness in different therapeutic conditions. Conclusion: The findings of this review confirm the effectiveness of TQ in various pathologies viz. inflammation, cancer, diabetes, gastric, hepatic, microbial and allergies. However, the complete clinical benefit of TQ has not yet been realized, owing to its poor biopharmaceutical properties. Nevertheless, colloidal drug delivery carrier systems, could be impending in bringing forth this potential molecule to reality.

Introduction: Although considerable efforts have been made to develop effective therapeutic agents for Alzheimer's Disease (AD), neither a consensus concerning the pathogenesis of the disease nor a successful therapy for its treatment is yet available. The natural product chemistry brings tremendous diversity and abundant resource for medical needs. Objectives: The present review summarizes recent patents on natural extracts and derived drugs as agents for the prevention and treatment of AD. It also sums up the suggested mechanisms of action of the formulated natural remedies. Conclusion: It is now becoming well accepted that multiple factors contribute to the progression of AD. The pathogenesis of the disease involves amyloid-β cascade, tau hyperphosphorylation, oxidative stress, inflammation, mitochondrial dysfunction, protein misfolding, gene mutation, etc. It has been suggested that the multifactorial nature of AD pathogenesis requires the design of medicines with a wide spectrum of activity. Medicinal herbs are known to consist of multiple compounds and may implicate multiple mechanisms, thus being advantageous over the simple single-target drugs in the treatment of complex diseases. Indeed, natural products attract increased attention. In the last decades, they have become a major focus in the quest for AD remedies and may represent a real promise for curing the disease.

Background: Nanopharmaceutical is the field that arises gradually but many challenges are also still there. This review aims to identify these challenges and give the focus on their rectification. Methods: In this paper, we memorize the safety issues, patented manufacturing procedure, applications and regulatory aspects of the nanopharmaceuticals by using the peer-reviewed research literatures. All the screened literatures described the quality content of nanopharmaceuticals with relevancy to biomedical and pharmaceutical field. Results: Nanopharmaceuticals have great potential to resolve the different issues such as; site specific drug delivery however, many challenges are also arising in their commercialization. In the recent years, some nanopharmaceuticals have the desired quality and safety for the public, have been approved by the regulatory agencies but this field is still a thrust area that demands a lot of attention. Conclusion: The present review article confirms the importance of nanopharmaceuticals and impart the knowledge for making the significant approaches and strategies to overcome the manufacturing, safety, legal and regulatory issues related to nanopharmaceuticals.

Aims and Background: The fundamental objective of current study was to encapsulate Aripiprazole (ARP) within Pluronic F127 micelles to improve its aqueous solubility. The recent patents on Aripiprazole (JP2013136621) and micelles (WO2016004369A1) facilitated selection of drug and polymer. Materials and Methods: The drug-laden micelles were fabricated using thin-film hydration technique. Optimization of the micellar formulation was done by using response surface method (RSM). The Pluronic F127 concentration of 150 mg and 75 rpm rotational speed of rotary evaporator were found to be optimized conditions for formulating micelles. Results: The prepared batches were further characterized for PDI (polydispersity index), zeta potential, % DLC (% Drug loading content), % EE (% Entrapment Efficiency) and % drug release study; results of these parameters were found to be 0.228, −4.04 mV and 76.50 % and 18.56 % respectively. It was observed from the In vitro release study that 97.37 ± 1.81 % drug had released from micelles after 20h which were found about thrice as compared to that of pure drug. The optimized ARP micellar formulation was characterized using DSC (Differential Scanning Colorimetry), FT-IR (Fourier Transformed Infrared Spectroscopy), P-XRD (Powdered X-ray Diffraction Study) and TEM (Transmission Electronic Microscopy) studies. ARP-loaded micelles displayed a hydrodynamic diameter of 170.3 nm and a sphere-shaped morphology as determined by dynamic light scattering as well as TEM study. Conclusion: It is concluded that the prepared polymeric micellar system has an excellent potential to be used as a delivery carrier for Aripiprazole with increased solubility.

Aims and Background: The design and development of an effective medicine are, however, often faced with a number of challenges. One of them is the close relationship of drug's bioavailability with solubility, dissolution rate and permeability. The use of curcumin's (CUR) therapeutic potential is limited by its poor water solubility and low chemical stability. The purpose was to evaluate the effect of polymer and solid dispersion (SD) preparation techniques to enhance the aqueous solubility, dissolution rate and stability of the CUR. The recent patents on curcumin SD were reported as (i) curcumin with polyvinylpyrrolidone (CN20071 32500 20071214, WO2006022012 and CN20151414227 20150715), (ii) curcumin-zinc/polyvinylpyrrolidone (CN20151414227 20150715), (iii) curcumin-poloxamer 188 (CN2008171177 20080605), (iv) curcumin SD prepared by melting method (CN20161626746-20160801). Materials and Methods: SD obtained by co-preciptation or microwave fusion and the physical mixture of CUR with Poloxamer-407 (P-407), Hydroxypropylmetylcellulose-K4M (HPMC K4M) and Polyvinylpyrrolidone-K30 (PVP-K30) were prepared at the ratios of 1:2; 1:1 and 2:1. The samples were evaluated by solubility, stability, dissolution rate and characterized by SEM, PXRD, DSC and FTIR. Results: The solubility, stability (pH 7.0) and dissolution rate were significantly greater for SD (CUR:P-407 1:2). The PXRD,SEM and DSC indicated a change in the crystalline state of CUR. The enhancement of solubility was dependent on a combination of factors including the weight ratio, preparation techniques and carrier properties. The drug release data fitted well with the Weibull equation, indicating that the drug release was controlled by diffusion, polymer relaxation and erosion occurring simultaneously. Conclusion: Thus, these SDs, specifically CUR:P-407 1:2 w/w, can overcome the barriers of poor bioavailability to reap many beneficial properties.

Purpose: The solubility of drug is affected by various excipients present in formulation. In case of tablet formulation, the role of binders is very important for solubility of dosage form as well as drug. In this study, an attempt was made to improve the solubility and dissolution rate of a drug by the use of natural excipients. In this study, pear was selected for the extraction and isolation of starch. Then the extracted starch was used as a binder in different concentrations, in famotidine tablets and evaluates them. There are some recent patents on modified starch (WO2011002730A1), directly compressed starch (US6455069B1), pre-compacted starches (US4072535A), which helped in following the study. Methods: The starch was isolated from natural source. Then, the tablets were formulated by wet granulation method by using 2% w/v, 4% w/v, 6% w/v and 8% w/v of pear starch as binding agent. Then formulated famotidine tablets were further evaluated for various parameters i.e. weight variation, hardness, thickness, friability, disintegration time and in-vitro drug release. Results: The hardness and disintegration time of the tablets was found to be increased with increase in starch concentration. Tablets with the highest binder concentration showed maximum hardness (6.5 kg) and disintegration time (10min) and minimum friability (0.48%). After one hour, tablets with 4% w/v starch showed maximum drug release (80.69%). Conclusion: The pear fruit used for the isolation of starch was a natural and a newer source. The obtained starch was safe, natural, economic and easily isolated in laboratory. The results from various evaluations show that pear starch has significant binding characteristics. Hence it can be used as tablet binder in pharmaceutical formulations in future in place of other costly and synthetic starch.