Department of Pharmacy
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Item Enhancing 3-acetyl-11-keto-β-boswellic acid skin permeation via nanostructured lipid carriers: integrating quality by design principles for risk estimation and optimization(RSC, 2025-10) Taliyan, Rajeev; Singhvi, Gautam3-Acetyl-11-keto-β-boswellic acid (AKBA), a bioactive compound derived from Boswellia serrata, exhibits significant anti-inflammatory and antioxidant properties, making it a promising candidate for treating inflammatory skin disorders. Its hydrophobic nature makes topical administration challenging. By developing nanostructured lipid carriers (NLCs), this work sought to enhance the skin penetration of AKBA. Quality-by-design principles were applied for the development of a robust formulation, where AKBA-NLCs were developed using a three-factor, three-level Box–Behnken design. AKBA-NLCs were prepared by the hot homogenization technique. The optimized formulation was further loaded into a gelling system, and its rheological parameters were evaluated. Further evaluation for ex vivo skin permeation and retention, along with other characteristics such as occlusivity, extrudability, and spreadability, was performed. Quality-by-design through p-value assessment highlighted that all three factors significantly affected particle size, and in the case of PDI, only lipid content showed a significant impact, whereas for entrapment efficiency, lipid and surfactant content were the governing factors. Based on the set constraints, the optimized batch of AKBA-NLCs exhibited a particle size of 173.700 ± 1.165 nm, a PDI of 0.323 ± 0.012, a zeta potential of −19.533 ± 0.493 mV, and an entrapment efficiency of 82.349 ± 3.223%. The in vitro release showed a prolonged release profile up to 56 h. When tested for cytotoxicity in the HaCaT cell line, the formulation was observed to be non-cytotoxic. The rheological data of the gel demonstrated a non-Newtonian, pseudo-plastic nature and indicated good structural strength. The ex vivo skin permeation of AKBA-NLCs was found to be 1.34 times higher than that via plain gel. Based on consistent results of viscosity, particle size integrity, and assay after one year of storage, the formulation was found to be stable. The formulation method used was simple and cost-effective, allowing for possible industrial scale-up. According to the findings, the NLC-loaded gel may prove to be a useful delivery strategy for the management of inflammatory skin conditions.Item The role of diet and nutraceuticals in the amelioration of multidrug resistance amongst cancer patients(Springer, 2025-11) Singhvi, Gautam; Taliyan, RajeevCancer is one of the leading causes of death globally, with the reported numbers rising every year. Although the medical fraternity has made considerable progress in early detection and treatment interventions, the numbers are expected to increase drastically by 2040. The most prevalent cause of mortality in people with diverse cancer types is likely multidrug resistance (MDR). As per recent reports, there have been increased incidences of cancer being reported globally, with projections of low-Human Development Index (HDI) countries being affected more in the near future.Item Immunological challenges and opportunities in glioblastoma multiforme: A comprehensive view from immune system lens(Elsevier, 2024-11) Singhvi, Gautam; Taliyan, RajeevGlioblastoma multiforme (GBM), also known as grade IV astrocytoma, is the most common and deadly brain tumour. It has a poor prognosis and a low survival rate. GBM cells' immunological escape mechanism helps them resist advanced multimodal therapy. In physiological homeostasis, brain astrocytes and microglia suppress infections and clear the potential pathogen from the system. However, in severe pathological conditions like cancer, the immune response fails to eliminate mutated and rapidly over-proliferating GBM cells. The malignant cells' interactions with immune cells and the neoplasm's immunosuppressive environment enable the avoidance and their clearance. Immunotherapy efficiently addresses these difficulties, as shown by sufficient evidence. This review discusses how GBM cells inhibit and elude the immune system. These include MHC molecule expression alteration and PD-L1 and CTLA-4 immune checkpoint overexpression. Without co-stimulation, these changes induce effector T-cell tolerance and anergy. The review also covers how MDSCs, TAMs, Herpes Virus Entry Mediators, and Human cytomegalovirus protein decrease the effector immune response against glioblastoma. The latter part discusses various therapies that are available in the market or under clinical trials which revolves around combating resistance against the available multimodal therapies. The recent trends indicate that there are various monoclonal antibodies and peptide-based vaccines that can be utilized to overcome the immune evasion technique harbored by GBM cells.Item UV Spectrophotometric method for characterization of curcumin loaded nanostructured lipid nanocarriers in simulated conditions: Method development, in-vitro and ex-vivo applications in topical delivery(Elsevier, 2020-01) Pandey, Murali Monohar; Singhvi, GautamCurcumin the extract obtained from the dried rhizome of turmeric, Curcuma longa is a hydrophobic phenol that delivers numerous pharmacological actions like anti-inflammatory, anti-microbial and anti-oxidant, anti-psoriasis, antidiabetic, anticancer. But curcumin has low bioavailability issues that accompany low aqueous solubility, further, when administered orally, >90% of the drug degrades rapidly in the alkaline medium. Administering the drug topically can bypass the problem as well as first-pass metabolism and therefore delivering the drug at the targeted site of action. Encapsulating curcumin in nanostructured lipid nanocarriers (NLC) is an excellent novel strategy. Further, these NLC provides both the controlled release and helps in the enhanced permeation of the drug through the skin's physiological barrier, stratum corneum. For the NLC characterization, a reliable method must be developed that can accurately and precisely determine the drug content in the formulation and also for its in-vitro and ex-vivo characterization. This experiment describes the analytical validation parameters described as per International Conference of Harmonization guidelines to develop a method using the UV–Visible spectroscopy. The method was developed in two solvent systems i.e. methanol and 6.4 pH phosphate buffer with 1.5% polysorbate 80. Methanol solvent was used for the determination of curcumin in the NLC formulation via determining the encapsulation efficiency and 6.4 pH phosphate buffer with 1.5% polysorbate 80 solvent was used for in-vitro and ex-vivo characterization of the developed NLC formulation (cream and gel). These methods were validated in response to linearity, the limit of detection, the limit of quantification, precision, accuracy, repeatability, and specificity.Item UV Spectrophotometric method for characterization of curcumin loaded nanostructured lipid nanocarriers in simulated conditions: Method development, in-vitro and ex-vivo applications in topical delivery(Elsevier, 2020-01) Pandey, Murali Monohar; Singhvi, GautamCurcumin the extract obtained from the dried rhizome of turmeric, Curcuma longa is a hydrophobic phenol that delivers numerous pharmacological actions like anti-inflammatory, anti-microbial and anti-oxidant, anti-psoriasis, antidiabetic, anticancer. But curcumin has low bioavailability issues that accompany low aqueous solubility, further, when administered orally, >90% of the drug degrades rapidly in the alkaline medium. Administering the drug topically can bypass the problem as well as first-pass metabolism and therefore delivering the drug at the targeted site of action. Encapsulating curcumin in nanostructured lipid nanocarriers (NLC) is an excellent novel strategy. Further, these NLC provides both the controlled release and helps in the enhanced permeation of the drug through the skin's physiological barrier, stratum corneum. For the NLC characterization, a reliable method must be developed that can accurately and precisely determine the drug content in the formulation and also for its in-vitro and ex-vivo characterization. This experiment describes the analytical validation parameters described as per International Conference of Harmonization guidelines to develop a method using the UV–Visible spectroscopy. The method was developed in two solvent systems i.e. methanol and 6.4 pH phosphate buffer with 1.5% polysorbate 80. Methanol solvent was used for the determination of curcumin in the NLC formulation via determining the encapsulation efficiency and 6.4 pH phosphate buffer with 1.5% polysorbate 80 solvent was used for in-vitro and ex-vivo characterization of the developed NLC formulation (cream and gel). These methods were validated in response to linearity, the limit of detection, the limit of quantification, precision, accuracy, repeatability, and specificity.Item Emerging trends of nanotechnology in advanced cosmetics(Elsevier, 2022-06) Pandey, Murali Monohar; Singhvi, GautamThe cosmetic industry is dynamic and ever-evolving. Especially with the introduction and incorporation of nanotechnology-based approaches into cosmetics for evincing novel formulations that confers aesthetic as well as therapeutic benefits. Nanocosmetics acts via numerous delivery mechanisms which involves lipid nanocarrier systems, polymeric or metallic nanoparticles, nanocapsules, dendrimers, nanosponges,etc. Each of these, have particular characteristic properties, which facilitates increased drug loading, enhanced absorption, better cosmetic efficacy, and many more. This article discusses the different classes of nanotechnology-based cosmetics and the nanomaterials used for their formulation, followed by outlining the categories of nanocosmetics and the scope of their utility pertaining to skin, hair, nail, lip, and/or dental care and protection thereof. This review also highlights and discusses about the key drivers of the cosmetic industry and the impending need of corroborating a healthy regulatory framework, refocusing attention towards consumer needs and trends, inculcating sustainable techniques and tenets of green ecological principles, and lastly making strides in nano-technological advancements which will further propel the growth of the cosmetic industry.Item Development of a tumor extracellular pH-responsive nanocarrier by terminal histidine conjugation in a star shaped poly(lactic-co-glycolic acid)(Elsevier, 2021-06) Roy, Aniruddha; Singhvi, GautamThe present work aimed to develop topical solid lipid nanocarriers (SLN) loaded hydrogel of apremilast (API) for psoriasis therapy to minimize the systemic adverse effects. The quality by design approach was implemented for the optimization of API loaded SLN using Box-Behnken design. SLN were prepared using hot emulsification followed by size reduction using probe sonication. The size and entrapment were found to be 167.70 nm ± 1.5 (0.238 PDI) and 63.84 ± 0.93%, respectively. The FESEM images of SLN dispersion portrayed the spherical shape of nanocarriers. The in vitro drug release of SLN dispersion showed extended-release up to 18 h and followed the Korsmeyyar-Peppas model with a regression value of 0.958 (n = 0.330), and Akaike index criteria was 63.69. In vitro cell line study, the MTT assay depicted the formulation excipients had minimal effect, and high internalization was observed with SLN dispersion (1.4-fold). The Ct value reduction in the relative expression of TNF-α miRNA was 3-fold higher with SLN dispersion compared to the positive control. The ex vivo skin retention and dermal distribution study by Coumarin-6 dye depicted an increase in permeation and retention with SLN formulation compared to free drug-loaded gel. The dermato-pharmacokinetic study of SLN formulation exhibited 2-fold higher drug retention in the epidermis and 5-fold higher in the dermis compared to free drug. This were stable for 3 months without significant changes. The results suggest that API loaded SLN can be utilized for topical delivery for effective treatment of psoriasis by targeting skin layers. The API loaded SLN based topical gel formulation showed improved permeation, skin deposition and prolonged release compared to conventional preparation. The designed preparation can signify a potential alternative for psoriasis treatment after clinical evaluation in near future.Item Exploring temozolomide encapsulated PEGylated liposomes and lyotropic liquid crystals for effective treatment of glioblastoma: in-vitro, cell line, and pharmacokinetic studies(Elsevier, 2023-05) Singhvi, Gautam; Roy, AniruddhaTemozolomide (TMZ) is one of the best choices for treating glioblastoma. However, due to the short plasma half-life, only 20–30 % brain bioavailability can be achieved using traditional formulations. In the present study, PEGylated liposomes and lyotropic liquid crystals (LLCs) were developed and investigated to prolong the plasma circulation time of TMZ. Industrially feasible membrane extrusion and modified hot melt emulsification techniques were utilized during the formulation. Liposomes and LLCs in the particle size range of 80–120 nm were obtained with up to 50 % entrapment efficiency. The nanocarriers were found to show a prolonged release of up to 72 h. The cytotoxicity studies in glioblastoma cell lines revealed a ∼1.6-fold increased cytotoxicity compared to free TMZ. PEGylated liposomes and PEGylated LLCs were found to show a 3.47 and 3.18-fold less cell uptake in macrophage cell lines than uncoated liposomes and LLCs, respectively. A 1.25 and 2-fold increase in the plasma t1/2 was observed with PEGylated liposomes and PEGylated LLCs, respectively, compared to the TMZ when administered intravenously. Extending plasma circulation time of TMZ led to significant increase in brain bioavailability. Overall, the observed improved pharmacokinetics and biodistribution of TMZ revealed the potential of these PEGylated nanocarriers in the efficient treatment of glioblastoma.Item Apremilast loaded lyotropic liquid crystalline nanoparticles embedded hydrogel for improved permeation and skin retention: An effective approach for psoriasis treatment(Elsevier, 2023-06) Singhvi, Gautam; Roy, AniruddhaThe present work aimed to prepare and evaluate Apremilast loaded lyotropic liquid crystalline nanoparticles (LCNPs) formulation for skin delivery to enhance the efficacy with reduced adverse effects of the oral therapy in psoriasis treatment. The LCNPs were prepared using the emulsification using a high shear homogenizer for size reduction and optimized with Box Behnken design to achieve desired particle size and entrapment efficiency. The selected LCNPs formulation was evaluated for in-vitro release, in-vitro psoriasis efficacy, skin retention, dermatokinetic, in-vivo skin retention, and skin irritation study. The selected formulation exhibited 173.25 ± 2.192 nm (polydispersity 0.273 ± 0.008) particle size and 75.028 ± 0.235% entrapment efficiency. The in-vitro drug release showed the prolonged-release for 18 h. The ex-vivo studies revealed that LCNPs formulation exhibited drug retention up to 3.2 and 11.9-fold higher, in stratum corneum and viable epidermis compared to conventional gel preparation. In-vitro cell line studies performed on immortal keratinocyte cells (HaCaT cells) demonstrated non-toxicity of selected excipients used in designed LCNPs. The dermatokinetic study revealed the AUC0–24 of the LCNPs loaded gel was 8.4 fold higher in epidermis and 2.06 fold in dermis, respectively compared to plain gel. Further, in-vivo animal studies showed enhanced skin permeation and retention of Apremilast compared to conventional gel.Item Nanoscale Pluronic® micellar templates with varying %EO content for controlled drug release and cytotoxicity(Elsevier, 2023-08) Roy, Aniruddha; Singhvi, GautamThis study investigates the self-assembly in ethylene oxide (EO)-propylene oxide (PO)-based block copolymers (BCPs) with various molecular features like molecular weight, EO/PO ratio, HLB (Hydrophobic lipophilic balance) in aqueous solution environment. Our BCP solution systems exhibit significant changes in solution behaviour that showed micellization, micelle growth/ transition, and progressively phase separation (2ϕ), all of which are well explained by clear solution, blue point (BP) and cloud Point (CP) respectively. The solubilization of the highly hydrophobic anticancer drug-Quercetin (QCT) in such BCPs is examined using UV–Visible spectroscopy. The spectral findings inferred the dissolution capability of QCT in the examined copolymeric micellar systems in terms of drug loading efficiency (DL%), encapsulation efficiency (EE%), partition coefficient (P), and standard free energy of solubilization (ΔGo). Amongst the varied tested BCPs, it was observed that Pluronics® P123 and F127 exhibited an enhanced QCT solubilization capability than others and is explained in terms of hydrophobicity and hydrophilicity. The micellar size distribution profile expressed as hydrodynamic diameter (Dh) was determined for QCT-loaded and QCT-unloaded BCP micelles employing dynamic light scattering (DLS). The drug release profile was fitted employing various kinetic models, allowing this study to serve as an excellent foundation for QCT delivery. Reversed-phase High-performance liquid chromatography (HPLC) system determined the retention period in the QCT-loaded micelle while the structural alterations involved in Pluronics®-QCT system is inferred using small-angle neutron scattering (SANS). Fourier transform infrared spectroscopy (FT-IR) depicted the compatibility between Pluronics® and QCT which was validated further from the evaluated optimum descriptors using Gaussian 09 computational simulation framework. It was discovered that the QCT-loaded micelles exhibited a greater anticancer effect than free drug when tested in vivo on cancer cells. The anticancer activity of QCT-loaded F127 micelles was determined to be the strongest. Thus, the current study on QCT solubilization in Pluronics® will benefit considerably from its investigated outcomes.