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  1. Article ; Online: Improved delivery of poorly soluble compounds using nanoparticle technology: a review.

    Kalepu, Sandeep / Nekkanti, Vijaykumar

    Drug delivery and translational research

    2016  Volume 6, Issue 3, Page(s) 319–332

    Abstract: Although a large number of new drug molecules with varied therapeutic potentials have been discovered in the recent decade, yet most of them are still in developmental process. This can be attributed to the limited aqueous solubility which governs the ... ...

    Abstract Although a large number of new drug molecules with varied therapeutic potentials have been discovered in the recent decade, yet most of them are still in developmental process. This can be attributed to the limited aqueous solubility which governs the bioavailability of such drug molecules. Hence, there is a requisite for a technology-based product (formulation) in order to overcome such issues without compromising on the therapeutic response. The purpose of this review is to provide an insight to the formulation of drug nanoparticles for enhancing solubility and dissolution velocity with concomitant enhancement in bioavailability. In the recent decade, nanonization has evolved from a concept to reality owing to its versatile applications, especially in the development of drugs having poor solubility. In this review, a relatively simple and scalable approach for the manufacture of drug nanoparticles and latest characterization techniques utilized to evaluate the drug nanoparticles are discussed. The drug nanoparticulate approach described herein provides a general applicability of the platform technology in designing a formulation for drugs associated with poor aqueous solubility.
    Language English
    Publishing date 2016-06
    Publishing country United States
    Document type Journal Article ; Review
    ZDB-ID 2590155-2
    ISSN 2190-3948 ; 2190-393X
    ISSN (online) 2190-3948
    ISSN 2190-393X
    DOI 10.1007/s13346-016-0283-1
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Insoluble drug delivery strategies: review of recent advances and business prospects.

    Kalepu, Sandeep / Nekkanti, Vijaykumar

    Acta pharmaceutica Sinica. B

    2015  Volume 5, Issue 5, Page(s) 442–453

    Abstract: The emerging trends in the combinatorial chemistry and drug design have led to the development of drug candidates with greater lipophilicity, high molecular weight and poor water solubility. Majority of the failures in new drug development have been ... ...

    Abstract The emerging trends in the combinatorial chemistry and drug design have led to the development of drug candidates with greater lipophilicity, high molecular weight and poor water solubility. Majority of the failures in new drug development have been attributed to poor water solubility of the drug. Issues associated with poor solubility can lead to low bioavailability resulting in suboptimal drug delivery. About 40% of drugs with market approval and nearly 90% of molecules in the discovery pipeline are poorly water-soluble. With the advent of various insoluble drug delivery technologies, the challenge to formulate poorly water soluble drugs could be achieved. Numerous drugs associated with poor solubility and low bioavailabilities have been formulated into successful drug products. Several marketed drugs were reformulated to improve efficacy, safety and patient compliance. In order to gain marketing exclusivity and patent protection for such products, revitalization of poorly soluble drugs using insoluble drug delivery technologies have been successfully adopted by many pharmaceutical companies. This review covers the recent advances in the field of insoluble drug delivery and business prospects.
    Language English
    Publishing date 2015-08-24
    Publishing country Netherlands
    Document type Journal Article ; Review
    ISSN 2211-3835
    ISSN 2211-3835
    DOI 10.1016/j.apsb.2015.07.003
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Insoluble drug delivery strategies

    Sandeep Kalepu / Vijaykumar Nekkanti

    Acta Pharmaceutica Sinica B, Vol 5, Iss 5, Pp 442-

    review of recent advances and business prospects

    2015  Volume 453

    Abstract: The emerging trends in the combinatorial chemistry and drug design have led to the development of drug candidates with greater lipophilicity, high molecular weight and poor water solubility. Majority of the failures in new drug development have been ... ...

    Abstract The emerging trends in the combinatorial chemistry and drug design have led to the development of drug candidates with greater lipophilicity, high molecular weight and poor water solubility. Majority of the failures in new drug development have been attributed to poor water solubility of the drug. Issues associated with poor solubility can lead to low bioavailability resulting in suboptimal drug delivery. About 40% of drugs with market approval and nearly 90% of molecules in the discovery pipeline are poorly water-soluble. With the advent of various insoluble drug delivery technologies, the challenge to formulate poorly water soluble drugs could be achieved. Numerous drugs associated with poor solubility and low bioavailabilities have been formulated into successful drug products. Several marketed drugs were reformulated to improve efficacy, safety and patient compliance. In order to gain marketing exclusivity and patent protection for such products, revitalization of poorly soluble drugs using insoluble drug delivery technologies have been successfully adopted by many pharmaceutical companies. This review covers the recent advances in the field of insoluble drug delivery and business prospects.
    Keywords Bioavailability ; Cocrystals ; Solubility ; Inclusion complexation ; Nanoparticles ; Self-emulsifying formulations ; Proliposomes ; Medicine ; R ; Therapeutics. Pharmacology ; RM1-950
    Subject code 660
    Publishing date 2015-09-01T00:00:00Z
    Publisher Elsevier
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  4. Article ; Online: DEVELOPMENT OF NOVEL LIPID BASED DRUG DELIVERY SYSTEM FOR RALOXIFENE HYDROCHLORIDE

    Vijaykumar Nekkanti / Sandeep Kalepu

    International Research Journal of Pharmacy, Vol 3, Iss 9, Pp 166-

    2012  Volume 173

    Abstract: Lipid-based delivery systems are becoming increasingly popular as carriers of drugs due to their ability to overcome barriers to oral absorption. The objective of the present study was to prepare novel lipid-based formulation of a sparingly soluble drug, ...

    Abstract Lipid-based delivery systems are becoming increasingly popular as carriers of drugs due to their ability to overcome barriers to oral absorption. The objective of the present study was to prepare novel lipid-based formulation of a sparingly soluble drug, Raloxifene hydrochloride (RLX) to increase its saturation solubility and dissolution velocity for enhancing bioavailability while reducing systemic variability. Lipid-based formulations were prepared using melt solubilization technique. The liquid formulations were converted into a solid intermediate by adsorbing onto an inert carrier and blended with excipients for encapsulation. The solid state properties, surface morphology and in-vitro release characteristics of the lipid formulations were investigated and compared with commercial formulation. The characterization of lipid formulations using Differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD) and Scanning electron microscopy (SEM) indicated that the drug is completely enveloped in the lipid core. The dissolution characteristics of lipid based formulation filled in hard gelatin capsules showed faster rate of drug dissolution as compared to commercial tablet formulation (Fiona®). The in-vitro release studies in fed state simulated intestinal fluid (FeSSIF) and fasted state simulated intestinal fluid (FaSSIF) media indicated that, the variability in fed and fasted conditions was significantly reduced with lipid based formulation. The results from this study suggest the potential use of lipid based formulation a means of improving solubility, dissolution and concomitantly the bioavailability of a sparingly soluble drug like RLX.
    Keywords Lipid based formulation ; Raloxifene hydrochloride ; Drug content ; Powder flow properties ; Food effect ; Stability study. ; Pharmacy and materia medica ; RS1-441 ; Medicine ; R ; DOAJ:Pharmacy and materia medica ; DOAJ:Medicine (General) ; DOAJ:Health Sciences
    Subject code 660
    Language English
    Publishing date 2012-09-01T00:00:00Z
    Publisher International Research Journal of Pharmacy
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  5. Article ; Online: Oral lipid-based drug delivery systems – an overview

    Sandeep Kalepu / Mohanvarma Manthina / Veerabhadhraswamy Padavala

    Acta Pharmaceutica Sinica B, Vol 3, Iss 6, Pp 361-

    2013  Volume 372

    Abstract: The formulation of drugs is carried out with the principle objective of enhancing their bioavailability. Poorly water soluble drugs are challenging for the formulation scientists with regard to solubility and bioavailability. Lipid-based drug delivery ... ...

    Abstract The formulation of drugs is carried out with the principle objective of enhancing their bioavailability. Poorly water soluble drugs are challenging for the formulation scientists with regard to solubility and bioavailability. Lipid-based drug delivery systems (LBDDS) are one of the emerging technologies designed to address such challenges. Encapsulating or solubilizing the drug in lipid excipients can lead to increased solubilization and absorption, resulting in enhanced bioavailability. Recent advances in these formulation technologies have led to the successful commercialization of lipid-based formulations. This review provides a comprehensive summary and characterization of lipid-based formulations, especially for oral delivery, from both physicochemical and biopharmaceutical perspectives. This review also focuses on the processing techniques necessary to obtain solid lipid-based formulations for oral delivery, along with a brief discussion of lipid excipients and their characterization.
    Keywords Lipid-based formulation ; Lipid excipient ; Solubilization ; Lymphatic absorption ; Medicine ; R ; Therapeutics. Pharmacology ; RM1-950
    Publishing date 2013-12-01T00:00:00Z
    Publisher Elsevier
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  6. Article ; Online: Liposomal drug delivery system - A Comprehensive Review

    SANDEEP KALEPU / SUNILKUMAR K T / SUDHEER BETHA / MOHANVARMA M

    International Journal of Drug Development & Research, Vol 5, Iss 4, Pp 62-

    2013  Volume 75

    Abstract: The role of bilayerd vesicles as efficient carriers for drugs, vaccines, diagnostic agents and other bioactive agents have led to a rapid advancement in the liposomal drug delivery system. Moreover, the site-avoidance and site-specific drug targeting ... ...

    Abstract The role of bilayerd vesicles as efficient carriers for drugs, vaccines, diagnostic agents and other bioactive agents have led to a rapid advancement in the liposomal drug delivery system. Moreover, the site-avoidance and site-specific drug targeting therapy could be achieved by formulating a liposomal product, so as to reduce the cytotoxicity of many potent therapeutic agents. This article is intended to provide an overview of liposomal drug delivery system. It has focused on the factorsaffecting the behavior of the liposomes in the biological environment. Various aspects related to mechanism of liposome formation, characterization and stability of the liposomal drug product were also discussed in the article. Liposomes can be used as a therapeutic tool inthe fields like tumor targeting, genetic transfer, immunomodulation, skin and topical therapy.
    Keywords Liposomal formulation ; bilayered vesicles ; percent drug encapsulation ; cytotoxic. ; Pharmacy and materia medica ; RS1-441 ; Medicine ; R
    Subject code 610
    Language English
    Publishing date 2013-12-01T00:00:00Z
    Publisher Chauhan Publishers
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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