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  1. Article: Nasal Delivery to the Brain: Harnessing Nanoparticles for Effective Drug Transport.

    Gandhi, Shivani / Shastri, Divyesh H / Shah, Jigar / Nair, Anroop B / Jacob, Shery

    Pharmaceutics

    2024  Volume 16, Issue 4

    Abstract: The nose-to-brain drug-delivery system has emerged as a promising strategy to overcome the challenges associated with conventional drug administration for central nervous system disorders. This emerging field is driven by the anatomical advantages of the ...

    Abstract The nose-to-brain drug-delivery system has emerged as a promising strategy to overcome the challenges associated with conventional drug administration for central nervous system disorders. This emerging field is driven by the anatomical advantages of the nasal route, enabling the direct transport of drugs from the nasal cavity to the brain, thereby circumventing the blood-brain barrier. This review highlights the significance of the anatomical features of the nasal cavity, emphasizing its high permeability and rich blood supply that facilitate rapid drug absorption and onset of action, rendering it a promising domain for neurological therapeutics. Exploring recent developments and innovations in different nanocarriers such as liposomes, polymeric nanoparticles, solid lipid nanoparticles, dendrimers, micelles, nanoemulsions, nanosuspensions, carbon nanotubes, mesoporous silica nanoparticles, and nanogels unveils their diverse functions in improving drug-delivery efficiency and targeting specificity within this system. To minimize the potential risk of nanoparticle-induced toxicity in the nasal mucosa, this article also delves into the latest advancements in the formulation strategies commonly involving surface modifications, incorporating cutting-edge materials, the adjustment of particle properties, and the development of novel formulations to improve drug stability, release kinetics, and targeting specificity. These approaches aim to enhance drug absorption while minimizing adverse effects. These strategies hold the potential to catalyze the advancement of safer and more efficient nose-to-brain drug-delivery systems, consequently revolutionizing treatments for neurological disorders. This review provides a valuable resource for researchers, clinicians, and pharmaceutical-industry professionals seeking to advance the development of effective and safe therapies for central nervous system disorders.
    Language English
    Publishing date 2024-04-01
    Publishing country Switzerland
    Document type Journal Article ; Review
    ZDB-ID 2527217-2
    ISSN 1999-4923
    ISSN 1999-4923
    DOI 10.3390/pharmaceutics16040481
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Orodispersible Films: Current Innovations and Emerging Trends.

    Jacob, Shery / Boddu, Sai H S / Bhandare, Richie / Ahmad, Samiullah Shabbir / Nair, Anroop B

    Pharmaceutics

    2023  Volume 15, Issue 12

    Abstract: Orodispersible films (ODFs) are thin, mechanically strong, and flexible polymeric films that are designed to dissolve or disintegrate rapidly in the oral cavity for local and/or systemic drug delivery. This review examines various aspects of ODFs and ... ...

    Abstract Orodispersible films (ODFs) are thin, mechanically strong, and flexible polymeric films that are designed to dissolve or disintegrate rapidly in the oral cavity for local and/or systemic drug delivery. This review examines various aspects of ODFs and their potential as a drug delivery system. Recent advancements, including the detailed exploration of formulation components, such as polymers and plasticizers, are briefed. The review highlights the versatility of preparation methods, particularly the solvent-casting production process, and novel 3D printing techniques that bring inherent flexibility. Three-dimensional printing technology not only diversifies active compounds but also enables a multilayer approach, effectively segregating incompatible drugs. The integration of nanoparticles into ODF formulations marks a significant breakthrough, thus enhancing the efficiency of oral drug delivery and broadening the scope of the drugs amenable to this route. This review also sheds light on the diverse in vitro evaluation methods utilized to characterize ODFs, ongoing clinical trials, approved marketed products, and recent patents, providing a comprehensive outlook of the evolving landscape of orodispersible drug delivery. Current patient-centric approaches involve developing ODFs with patient-friendly attributes, such as improved taste masking, ease of administration, and enhanced patient compliance, along with the personalization of ODF formulations to meet individual patient needs. Investigating novel functional excipients with the potential to enhance the permeation of high-molecular-weight polar drugs, fragile proteins, and oligonucleotides is crucial for rapid progress in the advancing domain of orodispersible drug delivery.
    Language English
    Publishing date 2023-12-11
    Publishing country Switzerland
    Document type Journal Article ; Review
    ZDB-ID 2527217-2
    ISSN 1999-4923
    ISSN 1999-4923
    DOI 10.3390/pharmaceutics15122753
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article: Advances in Nanocarrier Systems for Overcoming Formulation Challenges of Curcumin: Current Insights.

    Jacob, Shery / Kather, Fathima Sheik / Morsy, Mohamed A / Boddu, Sai H S / Attimarad, Mahesh / Shah, Jigar / Shinu, Pottathil / Nair, Anroop B

    Nanomaterials (Basel, Switzerland)

    2024  Volume 14, Issue 8

    Abstract: Curcumin, an organic phenolic molecule that is extracted from the rhizomes ... ...

    Abstract Curcumin, an organic phenolic molecule that is extracted from the rhizomes of
    Language English
    Publishing date 2024-04-12
    Publishing country Switzerland
    Document type Journal Article ; Review
    ZDB-ID 2662255-5
    ISSN 2079-4991
    ISSN 2079-4991
    DOI 10.3390/nano14080672
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Cyclodextrin complexes: Perspective from drug delivery and formulation.

    Jacob, Shery / Nair, Anroop B

    Drug development research

    2018  Volume 79, Issue 5, Page(s) 201–217

    Abstract: Cyclodextrins (CDs) have been widely investigated as a unique pharmaceutical excipient for past few decades and is still explored for new applications. They are highly versatile oligosaccharides which possess multifunctional characteristics, and are ... ...

    Abstract Cyclodextrins (CDs) have been widely investigated as a unique pharmaceutical excipient for past few decades and is still explored for new applications. They are highly versatile oligosaccharides which possess multifunctional characteristics, and are mainly used to improve the physicochemical stability, solubility, dissolution rate, and bioavailability of drugs. Stability constant, factors affecting complexation, techniques to enhance complexation efficiency, the preparation methods for molecular inclusion complexes and release of guest molecules are discussed in brief. In addition, different CD derivatives and their pharmacokinetics are elaborated. Further, the significance of CD complex in aqueous solubility, dissolution and bioavailability, stability, and taste masking is explained. The recent advancement of CDs in developing various drug delivery systems is enlightened. Indeed, the potential of CDs by means of inclusion complex formation have widen the applicability of these materials in various drug delivery systems including ocular, osmotic, mucoadhesive, transdermal, nasal, and targeted delivery systems. Feasibility studies have been performed on the benefit of these cyclic oligomers as nanocarriers, a strategy that can modify the drugs with improved physicochemical properties. Studies also demonstrated the feasibility of CDs to self-assemble in the form of stable nanoaggregates, which may extend the scope of CDs in drug delivery to the continually expanding list of new drug entities.
    MeSH term(s) Animals ; Biological Availability ; Chemistry, Pharmaceutical ; Cyclodextrins/chemistry ; Drug Carriers/chemistry ; Drug Compounding/methods ; Drug Liberation ; Excipients/chemistry ; Humans ; Nanoparticles/chemistry ; Pharmaceutical Preparations/administration & dosage
    Chemical Substances Cyclodextrins ; Drug Carriers ; Excipients ; Pharmaceutical Preparations
    Language English
    Publishing date 2018-08-21
    Publishing country United States
    Document type Journal Article ; Review
    ZDB-ID 604587-x
    ISSN 1098-2299 ; 0272-4391
    ISSN (online) 1098-2299
    ISSN 0272-4391
    DOI 10.1002/ddr.21452
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: An updated overview with simple and practical approach for developing in vitro-in vivo correlation.

    Jacob, Shery / Nair, Anroop B

    Drug development research

    2018  Volume 79, Issue 3, Page(s) 97–110

    Abstract: Preclinical Research & Development An in vitro-in vivo correlation (IVIVC) is as a predictive mathematical model that demonstrates a key role in the development, advancement, evaluation and optimization of extended release, modified release and immediate ...

    Abstract Preclinical Research & Development An in vitro-in vivo correlation (IVIVC) is as a predictive mathematical model that demonstrates a key role in the development, advancement, evaluation and optimization of extended release, modified release and immediate release pharmaceutical formulations. A validated IVIVC model can serve as a surrogate for bioequivalence studies and subsequently save time, effort and expenditure during pharmaceutical product development. This review discusses about different levels of correlations, general approaches to develop an IVIVC by mathematical modelling, validation, data analysis and various applications. In the current setting, the dearth of success associated with IVIVC is due to complexity of underlying scientific principles as well as the practice of fitting/matching in vivo plasma level-time data with in vitro dissolution profile. Hence, a simple, straightforward practical means to predict plasma drug levels by convolution technique and percentage drug absorbed computed from in vitro dissolution profile based on deconvolution method are illustrated. The bioavailability/bioequivalence assessment and evaluation are frequently validated by the pharmacokinetic parameters such as maximum concentration, time to reach maximum concentration, and area under the curve. The implementation of a quality by design manufacturing based on in vivo bioavailability and clinically relevant dissolution specification are recommended because corresponding design safe space will guarantee that all batches from relevant products are met with sufficient quality and bioperformance. Recently, United States Food and Drug Administration and European Medicines Agency have proposed that in silico/physiologically based pharmacokinetic modelling can be used in decision making during preclinical experiments as well as to recognize the dissolution profiles that can forecast and ensure the desired clinical performance.
    MeSH term(s) Animals ; Biopharmaceutics ; Humans ; Models, Theoretical ; Pharmaceutical Preparations/chemistry ; Pharmaceutical Preparations/classification ; Pharmaceutical Preparations/metabolism ; Pharmacokinetics ; United States ; United States Food and Drug Administration
    Chemical Substances Pharmaceutical Preparations
    Language English
    Publishing date 2018-04-26
    Publishing country United States
    Document type Journal Article ; Review
    ZDB-ID 604587-x
    ISSN 1098-2299 ; 0272-4391
    ISSN (online) 1098-2299
    ISSN 0272-4391
    DOI 10.1002/ddr.21427
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article: Emerging role of nanosuspensions in drug delivery systems.

    Jacob, Shery / Nair, Anroop B / Shah, Jigar

    Biomaterials research

    2020  Volume 24, Page(s) 3

    Abstract: Rapid advancement in drug discovery process is leading to a number of potential new drug candidates having excellent drug efficacy but limited aqueous solubility. By virtue of the submicron particle size and distinct physicochemical properties, ... ...

    Abstract Rapid advancement in drug discovery process is leading to a number of potential new drug candidates having excellent drug efficacy but limited aqueous solubility. By virtue of the submicron particle size and distinct physicochemical properties, nanosuspension has the potential ability to tackle many formulation and drug delivery issues typically associated with poorly water and lipid soluble drugs. Conventional size reduction equipment such as media mill and high-pressure homogenizers and formulation approaches such as precipitation, emulsion-solvent evaporation, solvent diffusion and microemulsion techniques can be successfully implemented to prepare and scale-up nanosuspensions. Maintaining the stability in solution as well as in solid state, resuspendability without aggregation are the key factors to be considered for the successful production and scale-up of nanosuspensions. Due to the considerable enhancement of bioavailability, adaptability for surface modification and mucoadhesion for drug targeting have significantly expanded the scope of this novel formulation strategy. The application of nanosuspensions in different drug delivery systems such as oral, ocular, brain, topical, buccal, nasal and transdermal routes are currently undergoing extensive research. Oral drug delivery of nanosuspension with receptor mediated endocytosis has the promising ability to resolve most permeability limited absorption and hepatic first-pass metabolism related issues adversely affecting bioavailability. Advancement of enabling technologies such as nanosuspension can solve many formulation challenges currently faced among protein and peptide-based pharmaceuticals.
    Language English
    Publishing date 2020-01-15
    Publishing country England
    Document type Journal Article ; Review
    ZDB-ID 2775188-0
    ISSN 2055-7124 ; 1226-4601
    ISSN (online) 2055-7124
    ISSN 1226-4601
    DOI 10.1186/s40824-020-0184-8
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  7. Article: Design, Development, and Evaluation of Constant Voltage Iontophoresis for the Transungual Delivery of Efinaconazole.

    Nair, Anroop B / Aldhubiab, Bandar / Shah, Jigar / Jacob, Shery / Attimarad, Mahesh / Sreeharsha, Nagaraja / Venugopala, Katharigatta N / Joseph, Alex / Morsy, Mohamed A

    Pharmaceutics

    2023  Volume 15, Issue 5

    Abstract: The efficacy of topical antifungal therapy in onychomycosis has been hindered by the failure of the antimycotic to permeate the nail plate. This research aims to design and develop a transungual system for the effective delivery of efinaconazole ... ...

    Abstract The efficacy of topical antifungal therapy in onychomycosis has been hindered by the failure of the antimycotic to permeate the nail plate. This research aims to design and develop a transungual system for the effective delivery of efinaconazole utilizing constant voltage iontophoresis. Seven prototype drug-loaded hydrogel formulations (E1-E7) were prepared to assess the influence of solvent (ethanol) and cosolvent (Labrasol
    Language English
    Publishing date 2023-05-06
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2527217-2
    ISSN 1999-4923
    ISSN 1999-4923
    DOI 10.3390/pharmaceutics15051422
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  8. Article: Design, Development, Evaluation, and In Vivo Performance of Buccal Films Embedded with Paliperidone-Loaded Nanostructured Lipid Carriers.

    AlMulhim, Fahad Mohammed / Nair, Anroop B / Aldhubiab, Bandar / Shah, Hiral / Shah, Jigar / Mewada, Vivek / Sreeharsha, Nagaraja / Jacob, Shery

    Pharmaceutics

    2023  Volume 15, Issue 11

    Abstract: The therapeutic effectiveness of paliperidone in the treatment of schizophrenia has been limited by its poor oral bioavailability; hence, an alternative route could be appropriate. This study investigates the feasibility of developing a buccal film ... ...

    Abstract The therapeutic effectiveness of paliperidone in the treatment of schizophrenia has been limited by its poor oral bioavailability; hence, an alternative route could be appropriate. This study investigates the feasibility of developing a buccal film impregnated with paliperidone-loaded nanostructured lipid carriers (NLCs) and assesses the potential to enhance its bioavailability. Box-Behnken-based design optimization of NLCs was performed by examining the particles' physical characteristics. The polymeric film was used to load optimized NLCs, which were then assessed for their pharmaceutical properties, permeability, and pharmacokinetics. The optimization outcomes indicated that selected formulation variables had a considerable (
    Language English
    Publishing date 2023-10-25
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2527217-2
    ISSN 1999-4923
    ISSN 1999-4923
    DOI 10.3390/pharmaceutics15112530
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  9. Article: Design, Development, and Evaluation of Treprostinil Embedded Adhesive Transdermal Patch.

    Alissa, Ibrahim / Nair, Anroop B / Aldhubiab, Bandar / Shah, Hiral / Shah, Jigar / Mewada, Vivek / Almuqbil, Rashed M / Jacob, Shery

    Pharmaceutics

    2023  Volume 15, Issue 4

    Abstract: Clinical application of treprostinil in pulmonary arterial hypertension is hampered by adverse effects caused by its high dosing frequency. The objective of this investigation was to Formulate an adhesive-type transdermal patch of treprostinil and ... ...

    Abstract Clinical application of treprostinil in pulmonary arterial hypertension is hampered by adverse effects caused by its high dosing frequency. The objective of this investigation was to Formulate an adhesive-type transdermal patch of treprostinil and evaluate it both in vitro and in vivo. A 3
    Language English
    Publishing date 2023-04-12
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2527217-2
    ISSN 1999-4923
    ISSN 1999-4923
    DOI 10.3390/pharmaceutics15041226
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  10. Article ; Online: Percutaneous absorption and Skin accumulation of Lorazepam-Diphenhydramine- Haloperidol Carbopol gel in Porcine Ear Skin.

    Neupane, Rabin / Boddu, Sai H S / Al-Tabakha, Moawia M / Jacob, Shery / Babu, R Jayachandra / Tiwari, Amit K

    AAPS PharmSciTech

    2023  Volume 24, Issue 7, Page(s) 183

    Abstract: This study presents the formulation and evaluation of an ABH Carbopol gel containing lorazepam (Ativan®), diphenhydramine hydrochloride (Benadryl®), and haloperidol (Haldol®) for treating chemotherapy-induced nausea and vomiting (CINV) in hospice ... ...

    Abstract This study presents the formulation and evaluation of an ABH Carbopol gel containing lorazepam (Ativan®), diphenhydramine hydrochloride (Benadryl®), and haloperidol (Haldol®) for treating chemotherapy-induced nausea and vomiting (CINV) in hospice patients. ABH PLO gel is widely used for this purpose due to its low cost and presumed efficacy. However, previous studies, including one conducted by the authors, have reported insufficient drug absorption from the ABH PLO gel. Here we hypothesized that the ABH Carbopol gel would provide superior percutaneous absorption of the drugs. ABH Carbopol gel was characterized for pH, viscosity, thermal properties, and infrared spectroscopy. The percutaneous absorption and skin retention of the gel was evaluated across porcine ear skin using Franz diffusion cells, and the drug concentrations were determined by high-performance liquid chromatography. The pH of the ABH Carbopol gel was found to be 6.80 ± 0.33, and the retention time of diphenhydramine, haloperidol, and lorazepam were 4.73, 7.11, and 18.69 minutes, respectively. The thermogram of the ABH Carbopol gel indicates the drugs were present in the dissolved state. Based on the flux data, the estimated steady-state concentration (C
    MeSH term(s) Swine ; Animals ; Skin Absorption ; Haloperidol ; Lorazepam ; Diphenhydramine
    Chemical Substances Haloperidol (J6292F8L3D) ; Lorazepam (O26FZP769L) ; carboxypolymethylene (0A5MM307FC) ; Diphenhydramine (8GTS82S83M)
    Language English
    Publishing date 2023-09-12
    Publishing country United States
    Document type Journal Article
    ZDB-ID 2052070-0
    ISSN 1530-9932 ; 1530-9932
    ISSN (online) 1530-9932
    ISSN 1530-9932
    DOI 10.1208/s12249-023-02608-6
    Database MEDical Literature Analysis and Retrieval System OnLINE

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