Solubility-permeability interplay of hydrotropic solubilization of piroxicam.

OBJECTIVES: In this research paper, an investigation has been made to assess the simultaneous effect of a solubility enhancement approach, i.e., hydrotropy on the solubility and apparent permeability of piroxicam. The solubility of piroxicam (PRX) a BCS (biopharmaceutics classification system) class II drug has been increased using a mixed hydrotropy approach. This study is based on identifying the pattern of solubility-permeability interplay and confirming whether every solubility gain results in a concomitant decrease in permeability or permeability remains unaffected. METHOD: Solid dispersions of PRX were formulated using two hydrotropes, viz., sodium benzoate (SB) and piperazine (PP) by solvent evaporation method. A comprehensive 32factorial design was employed to study the effect of hydrotropes on the solubility and permeability of PRX. Subsequently, PRX tablets containing these solid dispersions were formulated and evaluated. KEY FINDINGS: SB and PP displayed a significant increase in the solubility of PRX ranging from 0.99 to 2.21 mg/mL for F1-F9 batches attributed to the synergistic effect of hydrotropes. However, there is a reduction in PRX permeability with increasing hydrotrope levels. The decline in permeability was notably less pronounced compared to the simultaneous rise in aqueous solubility of PRX. CONCLUSION: An evident tradeoff between permeability and solubility emerged through the mixed hydrotropic solubilization for PRX. As PRX has generally higher intrinsic permeability, it has been assumed that this permeability loss will not affect the overall absorption of PRX. However, it may affect the absorption of drugs with limited permeability. Therefore, solubility permeability interplay should be investigated during solubility enhancement.

Clinical applications of Sunscreens and formulation advancements.

Sunscreens cover the big market ratio in terms of cosmetic applications, but the therapeutic necessity of sunscreen still needs to be uncovered in the clinical context. Clinically, sunscreens are being employed more often nowadays as a result of the rising consequences of skin malignancies and the photodamaging effects of UV radiation. Sunscreens are essential to prevent aging by shielding the skin from the harmful effects of ultraviolet (UV) radiation. Over the recent decades, there has been a significant evolution in the usage of sunscreens as photo protectants. The demand for sunscreen formulations will inevitably rise as more people become aware of the protection that sunscreens provide against tanning, photoaging, non-melanoma skin cancers, pre-malignant skin lesions, and skin melanomas. The novel contemporary formulation techniques are also beneficial in enhancing the product's aesthetic look and quality. Recently, regulatory agencies have also started paying attention to the regulation of the clinical application, efficacy, and safety parameters related to sunscreen. This review underlines the pathophysiological response of UV exposure with the therapeutic applications of sunscreen in various dermatological conditions and the recent formulation advancements in the development of sunscreen.

Neurotoxic Effects of Nanoparticles and Their Pathogenesis.

A recent study on the deployment of nanoparticles in the consumer and healthcare sectors has shown highly serious safety concerns. This is despite the fact that nanoparticles offer a vast array of applications and great promise. According to studies on how nanoparticles interact with neurons, the central nervous system experiences both negative and positive impacts (CNS). With a maximum concentration of 0.1-1.0 wt.%, nanoparticles can be incorporated into materials to impart antibacterial and antiviral properties. Depending on the host or base materials utilised, this concentration may be transformed into a liquid phase release rate (leaching rate). For instance, nanoparticulate silver (Ag) or copper oxide (CuO)-filled epoxy resin exhibits extremely restricted release of the metal ions (Ag+ or Cu2+) into their surroundings unless they are physically removed or deteriorated. Nanoparticles are able to traverse a variety of barriers, including the blood-brain barrier (BBB) and skin, and are capable of penetrating biological systems and leaking into internal organs. In these circumstances, it is considered that the maximum drug toxicity test limit (10 g ml 1), as measured in artificial cerebrospinal solution, is far lower than the concentration or dosage. As this is a fast-increasing industry, as the public's exposure to these substances increases, so does their use. Thus, neurologists are inquisitive about how nanoparticles influence human neuronal cells in the central nervous system (CNS) in terms of both their potential benefits and drawbacks. This study will emphasise and address it.

The Solubility-Permeability Interplay for Solubility-Enabling Oral Formulations.

The Biopharmaceutical classification system (BCS) classifies the drugs based on their intrinsic solubility and intestinal permeability. The drugs with good solubility and intestinal permeability have good bioavailability. The drugs with poor solubility and poor permeability have solubility dependent and permeability dependent bioavailability, respectively. In the current pharmaceutical field, most of the drugs have poor solubility. To solve the problem of poor solubility, various solubility enhancement approaches have been successfully used. The effects of these solubility enhancing approaches on the intestinal permeability of the drugs are a matter of concern, and must not be overlooked. The current review article focuses on the effect of various solubility enhancing approaches viz. cyclodextrin, surfactant, cosolvent, hydrotropes, and amorphous solid dispersion, on the intestinal permeability of drugs. This article will help in the designing of the optimized formulations having balanced solubility enhancement without affecting the permeability of drugs.

Transdermal applications of ethosomes - a detailed review.

Skin, the largest organ of the body serves as a potential route of drug delivery for local and systemic effects. However, the outermost layer of skin, the stratum corneum (SC) acts as a tough barrier that prevents penetration of hydrophilic and high molecular weight drugs. Ethosomes are a novel phospholipid vesicular carrier containing high ethanol concentrations and offer improved skin permeability and efficient bioavailability due to their structure and composition. This article gives a review of ethosomes including their compositions, types, mechanism of drug delivery, stability, and safety behaviour. This article also provides a detailed overview of drug delivery applications of ethosomes in various diseases.