Recent Patents on Drug Delivery and Formulation最新文献

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.

Skin cancer, among the various kinds of cancers, is a type that emerges from skin due to the growth of abnormal cells. These cells are capable of spreading and invading the other parts of the body. The occurrence of non-melanoma and melanoma, which are the major types of skin cancers, has increased over the past decades. Exposure to ultraviolet radiations (UV) is the main associative cause of skin cancer. UV exposure can inactivate tumor suppressor genes while activating various oncogenes. The conventional techniques like surgical removal, chemotherapy and radiation therapy lack the potential for targeting cancer cells and harm the normal cells. However, the novel therapeutics show promising improvements in the effectiveness of treatment, survival rates and better quality of life for patients. Different methodologies are involved in the skin cancer therapeutics for delivering the active ingredients to the target sites. Nano carriers are very efficient as they have the ability to improve the stability of drugs and further enhance their penetration into the tumor cells. The recent developments and research in nanotechnology have entitled several targeting and therapeutic agents to be incorporated into nanoparticles for an enhancive treatment of skin cancer. To protect the research works in the field of nanolipoidal systems various patents have been introduced. Some of the patents acknowledge responsive liposomes for specific targeting, nanocarriers for the delivery or co-delivery of chemotherapeutics, nucleic acids as well as photosensitizers. Further recent patents on the novel delivery systems have also been included here.

Onychomycosis is a fungal infection of the nail plate or nail bed that leads to the gradual destruction of the nail. The main difficulties in the treatment of onychomycosis refer to the duration of treatments and their side effects. Thus, it becomes relevant to look for new therapeutic alternatives in the treatment of such common diseases that are efficient without causing the undesirable side effects on the patient's body. In this way, the objective of this study was to develop an anthroposophical formula for the treatment of onychomycosis, based on Phosphorus and Formica rufa, from an extensive bibliographic survey on the functions of these components, evaluating within the principles of Anthroposophy. Considering the set of knowledge and practices on the use of these components, it was possible to arrive at a proposal therapy that can be effective for the treatment of onychomycosis. After an extensive review of several existing patents, it was observed that formulations containing Phosphorus and Formica rufa together have not been described in other studies. Subsequently, our research group published a patent of the anthroposophical formula using these two components, with the number BR1020180750755, which will be efficient to help the recovery of nails, and facilitate normal growth.

Background: Febuxostat is a novel, orally-administered, powerful, non-purine, xanthine oxidase inhibitor used for treating gout and ceaseless tophaceous gout. The drug exhibits low bioavailability (about 49%) which is ascribed to its dissolution rate-limited absorption.

Objective: The current work is aimed to provide a novel strategy to improve the dissolution profile and thus, the bioavailability of Febuxostat.

Methods: Formulation of Fast Dissolving Tablets (FDT) is anticipated to provide immediate release of the drug, which in turn, will improve its dissolution profile to provide the initial surge in plasma concentration required in an acute gout attack. Incorporation of co-processed excipients in a tablet is known to improve the compressibility and disintegration characteristics of the tablets, which, in turn, result in enhanced in vitro drug release and improved bioavailability. A combination of crospovidone (it rapidly wicks saliva into the tablet to create the volume development and hydrostatic weight important to give quick disintegration) and microcrystalline cellulose (a highly compressible ingredient with good wicking and absorbing capacity) was, therefore, used as co-processed excipients.

Results: The tablets were prepared by direct compression technique with the application of a 32 randomized full factorial design. The prepared tablets were able to release more than 80% of the drug within 10 minutes of the start of dissolution testing and were able to show a better drug release profile in comparison to available marketed formulation.

Conclusion: So, it can be concluded that the developed fast release formulation was found to exhibit convincing in vitro results and may prove a boon in the treatment of acute gout attack after establishing in vivo potential.

3D printing technique has been utilised to develop novel and complex drug delivery systems that are almost impossible to produce by employing conventional formulation techniques. For example, this technique may be employed to produce tablets or Fast Dissolving oral Films (FDFs) with multilayers of active ingredients, which are personalised to patient's needs. In this article, we compared the production of FDFs by 3D printing to conventional methods such as solvent casting. Then, we evaluated the need for novel methods of producing fast dissolving oral films, and why 3D printing may be able to meet the shortfalls of FDF production. The challenges of producing 3D printed FDFs are identified at commercial scale by referring to the identification of suitable materials, hardware, qualitycontrol tests and Process Analytical Technology. In this paper, we discuss that the FDF market will grow to more than $1.3 billion per annum in the next few years and 3D printing of FDFs may share part of this market. Although companies are continuing to invest in technologies, which provide alternatives to standard drug delivery systems, the market for thin-film products is already well established. Market entry for a new technology such as 3D printing of FDFs will, therefore, be hard, unless, this technology proves to be a game changer. A few approaches are suggested in this paper.

Background: Transdermal drug delivery has many advantages compared to other routes. However, the barrier function of the stratum corneum limits the use of the skin as an administrative route for medications. Different methods were investigated to alter the barrier function of the stratum corneum and it was found that applying different ultrasound waves could enhance the skin's permeability.

Objective: The aim of this work is to study the effect of ultrasonic waves on the alteration of skin natural barrier function, to improve the permeability of the skin to Piroxicam using three-dimension skin (EpiDermTM) as a skin model for the investigation.

Method: The effect of ultrasound at 1 MHz and 20 kHz on the permeation of Piroxicam across the three-dimensional skin equivalent using a Franz diffusion cell, was evaluated and the concentration of Piroxicam in the receiving compartment was determined using liquid chromatography method.

Results: The permeation of Piroxicam enhanced by 199% when therapeutic ultrasound at 1 MHz frequency was used. Significant permeation enhancement was also found upon utilizing low frequency sonophoresis at 20 kHz (427%) with no apparent damage to the membrane.

Conclusion: Sonophoresis has a positive effect on enhancing skin permeability. The enhancement level was largely dependent on the sonication factors; frequency, intensity and length of treatment. Multiple mechanisms of action might be involved in permeation improvement of the piroxicam molecule. Those mechanisms are largely dependent on the ultrasonic conditions.

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.