Ultraflexible Liposome Nanocargo as a Dermal and Transdermal Drug Delivery System.

A selected active pharmaceutical ingredient must be incorporated into a cargo carrier in a particular manner so that it achieves its goal. An amalgamation of active pharmaceutical ingredients (APIs) should be conducted in such a manner that it is simple, professional, and more beneficial. Lipids/polymers that are known to be used in nanocarriers for APIs can be transformed into a vesicular formulation, which offers elegant solutions to many problems. Phospholipids with other ingredients, such as ethanol and water, form suitable vesicular carriers for many drugs, overcoming many problems related to poor bioavailability, poor solubility, etc. Ultraflexible liposomes are novel carriers and new frontiers of drug delivery for transdermal systems. Auxiliary advances in vesicular carrier research have been made, enabling polymer-coated ethanolic liposomes to avoid detection by the body's immune system-specifically, the cells of the reticuloendothelial system. Ultraflexible liposomes act as a cargo system and a nanotherapeutic approach for the transport of therapeutic drugs and bioactive agents. Various applications of liposome derivatives in different diseases are emphasized in this review.

Aptamers in Drug Design: An Emerging Weapon to Fight a Losing Battle.

Implementation of novel and biocompatible polymers in drug design is an emerging and rapidly growing area of research. Even though we have a large number of polymer materials for various applications, the biocompatibility of these materials remains as a herculean task for researchers. Aptamers provide a vital and efficient solution to this problem. They are usually small (ranging from 20 to 60 nucleotides, single-stranded DNA or RNA oligonucleotides which are capable of binding to molecules possessing high affinity and other properties like specificity. This review focuses on different aspects of Aptamers in drug discovery, starting from its preparation methods and covering the recent scenario reported in the literature regarding their use in drug discovery. We address the limitations of Aptamers and provide valuable insights into their future potential in the areas regarding drug discovery research. Finally, we explained the major role of Aptamers like medical imaging techniques, application as synthetic antibodies, and the most recent application, which is in combination with nanomedicines.

Fixed-dose combinations banned in India: is it the right decision? An eye-opening review.

Introduction: Fixed-dose combination (FDC) medicines contain more than one approved active pharmaceutical ingredient (API), are manufactured as a fixed-dose and packed in a single dosage form. FDCs have been drawing attention from the pharmaceutical industries because of the government's ban on 328 irrational FDCs in September 2018. The Drug Technical Advisory Board (DTAB) recommended that 'there is no therapeutic justification' for the active ingredients in the banned FDCs and accordingly these combinations 'may involve a risk to human beings'. Areas covered: The review illustrates the present status of FDCs, its regulatory framework, approvals in India and discusses the substantive cause behind the ban on FDCs in India. Expert opinion: The expert stress to establish a robust regulatory system for the approval of FDCs in India. The pharmaceutical industries should not perceive the ban against irrational FDCs as an impediment; rather, they should view as an opportunity to establish a stronger healthcare system. The current review is an eye-opener for the section of people who consider that the ban on FDCs is irrational. However, the ban on 328 FDCs may prove a landmark decision for the development of stronger healthcare policy in India.

Regulating E-cigarettes in India: A conundrum for the global giant in tobacco production.

Electronic cigarettes which are termed as e-cigarettes, e-cigs or e-vaporizers are used by the people for creating the inhalable aerosol which carries nicotine in it. Also, commonly referred as vaping. E-cigarettes are used as an alternative to the regular cigarettes and aids in the cessation of smoking. However, there has been tough strife and debate regarding e-cigarettes that are accompanied in the media stories which bring different opinions among consumers, experts as well as regulators who are involved in making decisions from no regulation to regulating e-cigarettes to banning of e-cigarettes which will bring direct impact on public health. In this article, an overview about the controversy of e-cigarettes with respect to the device, its market, regulation norms of e-cigarettes at different platforms and amidst the debate over e-cigarettes banning in India has been portrayed. It is surveyed that India being a hub of around 110 million tobacco smokers and a global giant in tobacco production, where the Indian government is planning to bring a complete ban over e-cigarettes throughout the country propels an elementary question of banning safer alternatives and not regular cigarettes which makes no sense from the point of banning e-cigarettes until or unless regular cigarettes are banned. Varying point of views from experts, scientists, users with respect to e-cigarettes has been addressed which shares a mix opinion with the supporters promoting ban as well as the antagonist with the concept of regulating the e-cigarettes in India.

Novel ethosomal gel of clove oil for the treatment of cutaneous candidiasis.

BACKGROUND: Dual-release mechanism of ethosomal gels (ie, ethosomes and gel) makes them as versatile drug delivery systems for topical applications. Clove oil is obtained from the clove buds exhibited broad antifungal and antibacterial activity. Cutaneous candidiasis is the infection caused by Candida albicans or other Candida species. AIM: The aim of the present study was to prepare ethosomal gel of clove oil and evaluate its effectiveness in the treatment of cutaneous candidiasis. METHODS: Ethosomes of clove oil was formulated by using varying concentrations of soyaphosphotidyl choline and ethanol, and later, it was incorporated into carbapol 974 base gels to form ethosomal gel. The prepared ethosomal gels were also evaluated for spreadability, drug release studies, ex vivo permeation study, and antifungal activity. RESULTS: The optimized formulation did not cause any irritation to the skin since the pH of formulation was in the pH range of skin. The ethosomal gel showed satisfactory antifungal activity against the fungus C. albicans compared to pure clove oil. CONCLUSIONS: The results showed that developed formulation could be promising one in the topical delivery of clove oil for the treatment of cutaneous candidiasis.

Nano-lipid Complex of Rutin: Development, Characterisation and In Vivo Investigation of Hepatoprotective, Antioxidant Activity and Bioavailability Study in Rats.

The current study was aimed to develop an amphiphilic drug-lipid nano-complex of rutin:egg phosphatidylcholine (EPC) to enhance its poor absorption and bioavailability, and investigated the impact of the complex on hepatoprotective and antioxidant activity. Rutin nano-complexes were prepared by solvent evaporation, salting out and lyophilisation methods and compared for the complex formation. For the selected lyophilisation method, principal solvent DMSO, co-solvent (t-butyl alcohol) and rutin:EPC ratios (1:1, 1:2 and 1:3) were selected after optimisation. The properties of the nano-complexes such as complexation, thermal behaviour, surface morphology, molecular crystallinity, particle size, zeta potential, drug content, solubility, in vitro stability study, in vitro drug release, in vitro and in vivo antioxidant study, in vivo hepatoprotective activity and oral bioavailability/pharmacokinetic studies were investigated. Rutin nano-complexes were developed successfully via the lyophilisation method and found to be in nanometric range. Rutin nano-complexes significantly improved the solubility and in vitro drug release, and kinetic studies confirmed the diffusion-controlled release of the drug from the formulation. The nano-complex showed better antioxidant activity in vitro and exhibited well in vitro stability in different pH media. The in vivo study showed better hepatoprotective activity of the formulation compared to pure rutin at the same dose levels with improved oral bioavailability. Carbon tetrachloride (CCl4)-treated animals (group II) failed to restore the normal levels of serum hepatic marker enzymes and liver antioxidant enzyme compared to the nano-complex-treated animals. The results obtained from solubility, hepatoprotective activity and oral bioavailability studies proved the better efficacy of the nano-complex compared to the pure drug.

Prolonged drug delivery system of an antifungal drug by association with polyamidoamine dendrimers.

INTRODUCTION: The potent antifungal agent amphotericin B (AmB) is not freely soluble in water. The clinical use of AmB is limited by nephrotoxicity and poor water solubility. Polyamidoamine (PAMAM) dendrimer offers an identical carrier for drug binding that has the capacity to attach and discharge drugs in numerous ways. MATERIALS AND METHODS: In this research work, we explored the potential of PAMAM dendrimers to improve the solubility of AmB. RESULTS AND DISCUSSION: The experimental results indicated that the solubility of AmB was greatly enhanced in the presence of PAMAM dendrimer solutions. Results indicated that the solubility of AmB enhanced with increase in dendrimer generations as well as concentration. In vitro release studies of AmB in the presence of the third generation of PAMAM dendrimers was performed by the dialysis method. Our research work revealed that binding of drug into dendrimers led to sustained release of AmB in vitro. CONCLUSION: Based on the stability studies, it was concluded that the drug dendrimer complex should be stored in a dark place at a cool temperature.

In vitro and in vivo evaluation of chitosan buccal films of ondansetron hydrochloride.

Buccal films of ondanstron hydrochloride were fabricated from mucoadhesive polymer, chitosan, and polyvinyl pyrrolidone (PVP K30) for the purpose of prolonging drug release and improving its bioavailability. All fabricated film formulations prepared were smooth and translucent, with good flexibility. The weight and thickness of all the formulations were found to be uniform. Drug content in the films ranged from 98 - 99%, indicating favorable drug loading and uniformity. The inclusion of PVP K30, a hydrophilic polymer, significantly reduced the bioadhesive strength and in vitro mucoadhesion time of the films, although the degree of swelling increased. In vitro drug release studies in simulated saliva showed a prolonged release of over five to six hours for all formulations, except C4, with 99.98% release in 1.5 hours. Kinetic analysis of the release data indicated that the best fit model with the highest correlation coefficient for all formulations was the Peppas model. In vivo studies, on selected films in rabbits, were conducted, to determine the pharmacokinetic parameters such as C(max), T(max), and AUC(0-∞), using model-independent methods with nonlinear least-squares regression analysis. The AUC and values of C(max) of ondansetron hydrochloride were found to be significantly greater (P < 0.005) than the selected films C2 and C3, as compared to those from the oral solution, thereby confirming improved bioavailability via the buccal route. The T(max) values were also significantly greater (P < 0.005), indicating the slower release of the drug from buccal films, thereby, providing prolonged effects. Good in vitro-in vivo correlation was observed with R(2) values exceeding 0.98, when the percentage of drug released was correlated with the percentage of drug absorbed.