Drug Delivery Letters - Volume 11, Issue 4, 2021

Poor solubility of the drug compounds is a significant problem in the pharmaceutical field; therefore, reducing particle size may be one of the most straightforward and efficient processes for enhancing the solubility of such compounds. Nanocrystal, a new carrier-free colloidal drug delivery system with a particle size ranging from 100 to 1000 nm, is thought as a viable drug delivery strategy to develop poorly soluble drugs. This review focuses on the nanocrystal approaches and their uses in pharmaceutical applications. Also, various preparation methods of the nanocrystal are briefly described in this review. The paper also describes several factors involved in producing stable drug nanocrystals and provides suggestions for overcoming instability-related issues, like aggregation and Ostwald ripening. Finally, the specific opportunities and challenges that apply to nanocrystal technology are summarized in this paper. In this paper, we summarize and discuss the unique features of drug nanocrystals, including enhancement of dissolution velocity, adhesiveness to the surface, and saturation solubility. Nowadays, pharmaceutical industries are using different approaches to prepare the nanocrystal, like the bottom-up approach (precipitation), the top-down approach (wet milling, high-pressure homogenization), and some other combinational approaches. Drug nanocrystals can be administered through different routes. Besides this, the various fabrication methods and characterization methods may be used to develop and scale up the production of drug nanocrystals. In this review article, the relevance of drug nanocrystals are presented and illustrated according to the research done by different researchers and finally concluded that marketed formulation related to nanocrystal are gradually in progression. However, some related and developed formulations are under clinical trial.

Erlotinib is a tyrosine kinase inhibitor and it can treat tumors, such as pancreatic and locally advanced lung cancer or metastatic cancer. The traditional formulation of erlotinib currently available is an oral delivery type that presents serious side effects such as hepatotoxicity, skin rashes, gastrointestinal disturbance, renal dysfunction, drug resistance and hematological symptoms. Besides this, other disadvantages of erlotinib provided mostly by oral administration are the comprehensive metabolism, low bioavailability, poor solubility and off-target impact. Overcoming such unfavorable attributes of the medication, innovative medication delivery mechanisms like nanocapsules, liposomes, microspheres, microparticles solid lipid nanoparticles, nanosponge, and nanoparticles have been studied that have really shown their lead over traditional formulations. This article summarizes the novel erlotinib drug delivery systems to boost its clinical efficacy and reduce systemic toxicity. Novel formulations of erlotinib will offer positive outcomes in cancer therapy and will play an important part in improving the drug's therapeutic potential.

Background: Rosuvastatin calcium is a statin class of drug having limited oral bioavailability of about 20%. Bioavailability can be enhanced by using a biform complex of the drug with cow ghee. Methods: A precise thermal fractionation technique was adopted to separate different fatty acids from cow ghee. The collected fraction was characterized for fatty acid content. LC-MS and FTIR confirm the content variation in the collected fraction. Biform complex was prepared by fusion method with a constant ratio of drug and cow ghee fraction. The prepared complex was subjected to FTIR, DSC, and LC-MS studies to confirm chemical composition characteristics. For evaluation of the drug content, in-vitro and ex-vivo permeation studies were also performed. The antiinflammatory response was measured using the carrageenan paw-induced edema rat model. To determine the lipid-lowering effect, inflammation marker analysis was also performed using ELISA specific kit. Results: The biform complex prepared with a thermal fraction at 30°C of cow ghee showed the highest in-vitro and ex-vivo permeation. The anti-inflammation response of the biform complex F1 was higher than other tested formulations with a significant decrease in lipid and lipoprotein content. Conclusion: This study confirms that the thermal fractionation method is able to separate cow ghee as per the fatty acid content. The complexion of rosuvastatin calcium with cow ghee thermal fraction could enhance the oral bioavailability and improve anti-inflammatory and lipid-lowering activities.

Introduction: Conventional enteric coating is very challenging in soft gel capsules because of their shell nature (smooth surfaces and elasticity). Soft gelatin capsules are highly sensitive to temperature, humidity and they can lose their tensile strength during the conventional coating process. Materials and Methods: Enteric soft gel capsules were prepared by the addition of enteric polymer in the gelatin shell composition by inducing the cross-linking of gelatin through chemical treatment. Results: This dual approach makes the soft gelatin capsules resist the drug release in the stomach and reliably release their contents in the intestine within a predetermined time without affecting the physical properties of soft gel capsules. Conclusion: Enteric effects of soft gel capsules are brought by a specialized synergetic technique, which is unique for the molecules, requiring intestinal drug release.

Objectives: Acne vulgaris is a very common skin disorder that peaks in teenagers, but many men and women between 20-40 years of age are also affected by the disorder. For the treatment of acne, herbal medications are considered safer than allopathic medicines as allopathic medicines are associated with side effects, such as contact allergy, local irritation, scaling, photosensitivity, itching, and redness of the skin, etc. The present research work was performed to check the effectiveness of foaming face wash formulation containing Curcuma longa along with herbals excipient Aloe vera, Rosa centifolia, and Citrus sinensis. Curcuma longa has been reported to contain active phytoconstituents having significant anti-microbial activity and being used locally for acne. Methods: The plant materials Curcuma longa, Aloe vera, Rosa centifolia, and Citrus sinensis were authenticated, and their extracts have been prepared using Soxhlet Apparatus and the resulting essential oil was analyzed for its physical properties. The foaming face wash was then prepared by using the herbal extracts with excipients that were free from sulfates, parabens, silicone, and petroleum products. Two formulations, A1and A2, have been prepared and their physicochemical studies were performed. The presence and efficacy of Curcuma longa in the suppression of Propionibacterium acnes were assessed by analytical methods and anti-microbial techniques, respectively. Skin irritation studies were conducted using Wistar rats by the scoring method. Accelerated stability studies were also performed for 60 days. Result: The physicochemical properties were evaluated and found to be satisfactory. Analytical techniques like High-Performance Liquid Chromatography, High-Performance Thin Layer Chromatography, and Infra-Red spectral analysis confirmed the qualitative presence of Curcuminoid, which is a mixture of curcumin, desmethoxycurcumin (4-hydroxycinnamoyl-(4-hydroxy-3-methoxycinnamoyl) methane), and Bis- demethoxycurcumin (bis-(4-hydroxy cinnamoyl) methane) in the sample. The antibacterial activity of developed face wash assessed against Propionibacterium acnes was more than that of Clindamycin (10μg/ml). Also, the developed formulation showed very high activity against Staphylococcus epidermidis concerning the activity of the standard clindamycin. The prepared formulation showed no sign of localized reactions, which were confirmed by a skin irritation study, indicating the formulation was safe and compatible with the skin. Conclusion: Based on our study, it could be stated that the formulation has antimicrobial activity and could be used safely on human skin.