Recent Patents on Drug Delivery & Formulation - Volume 14, Issue 3, 2020

Current Development in drug delivery system has been employed with an endeavour to enhance the bioavailability of the drug, mask its taste, induce the rapid onset of action and improve patient compliance. An alternative approach to the conventional dosage form is being employed to triumph over all these issues named as Orodispersible system. Over the past three decades, this novel dosage form has gained considerable attention as compared to other conventional solid dosage forms such as tablets and capsules. ODTs dissolve or disintegrate within a few seconds or a minute when put on the tongue, without the need for water. ODT has an advantageous effect on paediatrics and geriatrics patients with dysphagia. Over the last decade, widespread advances in the formulation of ODTs have been executed in academia and industry that resulted in the emergence of a large number of patents. Products developed from ODT mechanics launched in the market in the 1980s have grown bit by bit in demand and their products are rapidly escalating. Expanding in the technology forum based on industrialization, these systems include the use of lyophilization, cotton candy, sublimation, melt extrusion and direct compression in addition to the conventional wet granulation processes and patent techniques. The present study focused on non-patent and patent citations concerning ODT along with active ingredients, techniques used and results of the innovations.

Atopic dermatitis is a chronic inflammatory disease of the skin, which is characterized by itching, erythema, and eczematous lacerations. It affects about 10 % of adults and approximately 15-20 % of children worldwide. As a result of genetic, immunologic, and environmental factors, the disease manifests itself with the impaired stratum corneum barrier and then immunological responses. Topical administration of corticosteroids and calcineurin inhibitors are currently used as the first strategy in the management of the disease. However, they have low skin bioavailability and some side effects. The nanocarriers as novel drug delivery systems could overcome limitations of conventional dosage forms, owing to increment of poorly soluble drug' solubility, then its thermodynamic activity and, consequently, its skin permeation. Also, side effects of the drug substances on the skin could be reduced by the nano-sized drug delivery systems due to encapsulation of the drug in the nanocarriers and targeted drug delivery of drug substances to the inflammated skin areas. Thereby, there have been available numerous research studies and patents regarding the use of nanocarriers in the management of atopic dermatitis. This review focuses on the mechanism of disease and development of nanocarrier based on novel drug release systems in the management of atopic dermatitis.

Nanotechnology is one of the emerging fields in drug delivery for targeting the drug to the site of action. The polymeric nanoparticles as drug delivery systems have gained importance for the last few decades. They offer advantages over liposomes, dendrimers, emulsions etc. Surface engineering of polymeric nanoparticles is widely utilized to effectively target the cells in various diseases such as cancer, HIV infection. Surface modified nanoparticles offer various advantages such as targeted drug delivery, reduction in side effects, dose reduction and improved therapeutic efficacy. Moreover, they can aid in improving physical and biochemical properties, pharmacokinetic and pharmacodynamic profiles of the drug. Surface modified polymeric nanoparticles can provide targeted delivery of drugs into specific cells, especially when targets are intracellularly localized. This approach of surface modification would be more advantageous for the delivery of various anticancer, anti-inflammatory, anti-HIV drugs for more effective therapy. This review focuses on the techniques used for the fabrication of polymeric nanoparticles, the material used for surface modification and their applications.

Aim: The manuscript aims to describe the techniques of modification of gums and mucilages and their effect on hydrophilicity and drug release. Discussion: The interest is increased in the fields of polymers which are obtained from natural origin and used in the preparation of pharmaceuticals. Mucilage and gum are natural materials widely used in the preparation of novel dosage and conventional dosage forms. They are used in the pharmaceutical industry for various purposes like suspending, emulsifying, bio-adhesive, binding, matrix-forming, extended release and controlled release agent. Gum and mucilage are biodegradable, less toxic, cheap and easily available. Moreover, mucilage and gum can be changed to acquire tailored materials for the delivery of drugs and allow them to compete with commercially available synthetic products. These polysaccharides have unique swellability in an aqueous medium that can exert a retardant effect on drug release or act as a super disintegrant, depending on the concentration utilized in the preparation. Drug release mechanism from hydrophilic matrices consisting of gums and mucilages is based on solvent penetration-induced polymer relaxation, diffusion of entrapped drug followed by degradation or erosion of the matrix. Conclusion: The present manuscript highlights the advantages, modifications of gum and mucilage, their effects on hydrophilicity and drug release as well as aspects of the natural gums which can be assumed to be bifunctional excipient because of their concentration-dependent effect on drug release and their high degree of swellability.

Background: Many topical agents are available in the market, which interfere with the pigmentation process at different levels. They are often known to cause side effects ranging from irritation to tumor over chronic use. Objective: The present study was designed to develop and characterize an anti blemish cream containing herbal oils. Methods: A herbal cream was formulated using dill, nagarmotha and black cumin oil and subjected to evaluation of its anti blemish potential against stress augmented UV-B rays-induced hyperpigmentation. Topical oil in water type of creams containing 2%, 4% and 6% of each oil was formulated using herbal oils. The formulated cream was characterized for solubility, pH, particle size, grittiness, viscosity, stability, phase separation, shelf life and spreadability, and found to be stable. Acute dermal toxicity was carried out individually for dill, nagarmotha and black cumin oil according to the OECD guidelines 402. Hyperpigmentation was induced in all the experimental animals by stress-augmented UV-B irradiation method. The animals were treated for 30 days (twice daily) with standard and test formulations by topical administration, whereas the disease group was left untreated. The skin of the animals was subjected to photographical study as well as grading for pigmentation and irritation before and after treatment. After the treatment period, the serum antioxidant levels were estimated and histopathology, histochemical studies of skin were performed. Results: The animals treated with test formulations containing 2%, 4%, and 6% of herbal oil showed significant improvement in pigmentation compared to disease control as it is evident in photographic biochemical, histopathological and histochemical studies. Conclusion: Thus, it was concluded that the developed anti-blemish cream containing herbal oils possesses significant anti-blemish potential. This study necessitates further evaluations in human subjects as it could have a high positive therapeutic value in the treatment of hyperpigmentation.

Introduction: The purpose of this study was to determine if pharmacological treatment could increase progenitor cell proliferation in the Sub-ventricular Zone of aged rats. Previous work had shown that increasing progenitor cell proliferation in this region correlated well (R2=0.78; p= 0.0007) with functional recovery in a damaged corpus callosum (white matter tract), suggesting that progenitor cell proliferation results in oligodendrocytes in this region. Methods: 10 month old male and female Sprague Dawley rats were fed the drugs for 30 days in cookie dough, then immunocytochemistry was performed on coronal brain sections, using Ki67 labeling to determine progenitor cell proliferation. Results: Female rats showed low endogenous (control) progenitor cell proliferation, significantly different from male rats (P<0.0001), at this age. Ascorbic Acid (20 mg/kg, daily for 30 days) increased progenitor cell proliferation overall, but maintained the innate gender difference in stem cell proliferation (P=0.001). Prozac (5 mg/kg, daily for 30 days) increased progenitor cell proliferation for females but decreased stem cell proliferation for males, again showing a gender difference (P<0.0001). Simvastatin (1 mg/kg for 30 days) also increased progenitor cell proliferation in females and decreased progenitor cell proliferation in males, leading to a significant gender difference. Discussion: The three drug combinations (fluoxetine, simvastatin, and ascorbic acid, patent # 9,254,281) led to ~ 4 fold increase in progenitor cell proliferation in females, while male progenitor cell proliferation was highest with 50 mg/kg ascorbic acid. However, the ascorbic acid increase in proliferation appears to be only on the sides of the ventricles, which is not the region that normally gives rise to oligodendrocytes. Conclusion: There are innate gender differences in progenitor cell proliferation at the Sub-Ventricular Zone at middle age in rats, possibly due to the loss of estrogen in females. We also see notable gender differences in progenitor cell proliferation in the Sub ventricular Zone in response to common drugs, such as fluoxetine, simvastatin and Vitamin C (ascorbic acid).