Recent Advances in Drug Delivery and Formulation - Volume 17, Issue 2, 2023

Kojic acid (KA), a fungal secondary metabolite, is commonly used in the cosmetic industry as a skin-whitening agent because of its ability to inhibit tyrosinase, the enzyme involved in melanin production. However, KA has shown poor depigmenting effects and becomes unstable after prolonged storage. Its use in cosmetics products has also been restricted due to its hydrophilic nature. To overcome these limitations, the structure of KA can be altered to form KA derivatives, such as KA ester (KAE), with improved chemical and biological properties. For instance, multiple studies have shown that KAE is more effective at inhibiting tyrosinase, is less toxic and more stable than KA, thus making it more beneficial. Aside from structural modification, nanotechnology applications such as nanoemulsion, and others have shown the ability to strengthen the efficacy of both KA and KAE by increasing skin permeability and delivering the drug more precisely to the targeted site with better controlled release rate. Therefore, the aim of this review article is to discuss the importance of modifying KA’s chemical structure as well as the role of nanoemulsion, solid lipid nanoparticles (SLN), nanostructured lipid carrier (NLC), liposomes and ethosomes in improving topical delivery of KA and KAE for cosmetic and pharmaceutical applications.

The pulmonary drug delivery system is a minimally invasive method of administering drugs with systemic and localised activity. Since 4000 BC, inhalation therapy has been known to the Indians. The most effective and suitable pulmonary drug delivery methods have been used for controlling diseases like asthma, chronic obstructive pulmonary disorder (COPD), TB(Tuberculosis), lung cancer, cystic fibrosis, and pulmonary hypertension. Examples of pulmonary medication delivery devices- Metered dose inhalers (MDIs), nebulizers, and dry powder inhalers (DPIs) in the latest patent 2022 that have undergone numerous advancements over the years have been focused on in this article. Some promising patented design advancements of nebulizers are humidifier breathing circuits to control liquid contamination, technologically advanced nebulizers to increase pressure detection and nebulizer disinfection system to decrease or eliminate contagions in expelled air are highlighted in this article. Some noticed formulation- related advancements for inhalational dry powder patented in the year 2022, are mentioned in this article. Development of heat-stable dry powder to solve instability of inhaled protein and peptide powder at high temperatures. The inability of dry powder inhaler devices to administer low doses is solved by designing an affordable and side effects-free inhaler. pMDI manufacturing process is simplified by manufacturing tablets to be administered in pMDI. An aid is developed to lessen the activation force and keep the dose count within budget. The patented advancement in the pulmonary drug delivery system can help in the improvement of patient compliance and drug delivery efficacy.

Over the last few decades, hot melt extrusion (HME) has found extensive adaptability and utility as a viable drug delivery option in the pharmaceutical industry. HME has already been validated as a robust, novel technique mainly used for the correction of solubility and bioavailability of poorly soluble drugs. In line with the scope of the current issue, this review appraises the value of HME as a means of solubility enhancement of BCS class II drugs and presents an influential tool for the manufacturing or production of drugs or chemicals. The drug development process can be shortened with the use of hot melt extrusion technology, and the application of this process to analytical technology can ease the manufacturing process. This review focuses on the tooling, utility, and manufacturing aspects associated with hot melt extrusion technology.

Treatment modalities of various cancers and the delivery strategies of anticancer agents have evolved significantly in the recent past. The severity and fatality of the disease and hurdles to the effective delivery of therapeutic agents have drawn the attention of researchers across the world for proposing novel and effective drug delivery strategies for anticancer therapeutics. Attempts have been made to propose solutions to the diverse limitations like poor pharmacokinetics and higher systemic toxicities of the traditional delivery of anticancer agents. Nanotechnology-based drug delivery systems including lipid-based nanocarriers have demonstrated significant efficiency in this scenario. The review critically assessed the different types of lipid nanocarrier systems for the effective and optimal delivery of anticancer therapeutic agents. The diverse synthesis approaches are discussed for the laboratory scale and commercial development of different categories of lipid nanocarriers. Further, their application in anticancer drug delivery is illustrated in detail followed by a critical appraisal of their safety and toxicity.

Background: In pediatrics, developing new pharmaceutical forms that offer safety and efficacy is crucial to improve pediatric pharmaceutical care. Orodispersible tablets do not require swallowing because orodispersible tablets dissolve quickly in the mouth, reducing the risk of choking and making medication administration safer and more straightforward. There is no solid dosage form in the pharmaceutical market offering a unit dose of Levothyroxine for pediatric hypothyroidism patients. Objective: The objective of this study is to design and develop Orodispersible mini tablets of Levothyroxine Sodium (LT4 ODMTs) for pediatric doses. Methods: LT4 ODMTs were prepared by direct compression with 10 and 15 μg, respectively, using StarLac® and Disolcel® as excipients. United States Pharmacopeia (USP-43) guidelines evaluated and determined pre-compression properties and quality control parameters. Results: The LT4 ODMTs met the specified limits for quality controls. The Drug Content Uniformity was 97%, Hardness was less than 2.5 N, Friability was less than 0.3%, Disintegration time was less than 25 s, and dissolution profiles (Q 80% > 45 s) followed the USP requirements. Additionally, stability and microbiology assays were realized. Conclusion: These formulations are optimal for developing new LT4 ODMTs suitable for treating pediatric hypothyroidism.

Background: Films used for wound healing have many advantages, but should be flexible, robust, adherable and prevent maceration. Both Chitosan (CS) and Titanium dioxide nanopowder (TiO2NP) have good properties to accelerate wound healing and can be used in preparing films. Objective: CS and TiO2NP are combined to formulate films for wound healing. The physical, thermal, chemical, and mechanical characteristics of these films are to be assessed. The antibacterial activity of the films and their performance on wounded rats will be explored. Methods: Films made of CS and TiO2NP were characterized by FTIR, TGA, DSC, XRD, and SEM. The films' mechanical characteristics and antimicrobial activity were tested. Films with acceptable mechanical properties were evaluated on rats. Results: Generally, CS-TiO2films had higher weight and thickness but lowered flexibility compared to films prepared using CS only. The chosen film showed excellent folding endurance with weight and thickness of around 21.98 mg and 0.16 mm. The surface pH for CS-TiO2films was acidic, and for the selected film, it was 5.18. CS-TiO2film was active against all studied bacteria and significantly higher than CS films. The antimicrobial activity of Gram-negative bacteria (P. aeruginosa and E. coli) was higher than that of Gram-positive bacteria (S. aureus). Finally, adding TiO2NP to the films accelerated the healing process of the created wounds in a murine model, compared to control and CS-treated groups. Conclusion: Films of TiO2NP and CS have suitable properties to be used in wound healing and can be further used in the future to load drugs.